[English Name] | Fiveleaf Gynostemma Herb | |
[Chinese Name] | 绞股蓝 | |
[Pinying Name] | Jiaogulan | |
[Latin Name] | Gynostemmatis Herba | |
[Genera] | Cucurbitaceae | |
[Efficacy] | buyao | |
[Pictures] | Plant picture | Drug picture |
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[Characteristics] | ||
[Ecology] | It grows in valley dense forest、hillside open forest or bushes at the altitude between 100 to 3200 metres.It avoids straight sunshine ,poorly cold resistance,prefers dank、loose and fertile soil. | |
[Chemical composition] | This plant contains sterols: cucurbita-5,24-dienol, 24,24-dimethyl-5α-cholest-8-en-3β-ol, (24R)-5α-stigmast-7-en-22-yn-3β-ol, 24,24-dimethyl-5α- cholest-7-en-22-yn-3β-ol, 24,24-dimethyl-5α-cholest- 7,25-dien-22-yn-3β-ol, spinasterol, 24,24-dimethyl- 5α-cholest-7-en-3β-ol, 14α-methyl-5α-erg osta-9(11),24(28)-dien-3β-ol, 24α-ethyl-5α-cholestan-3β-ol, 14α-methyl-5α-ergost-9(11)-en-3β-ol, 4α,14α-dimethyl-5α-ergosta-7,9(11),24(28)-trien-3β-ol, isofucosterol, β-sitosterol)[1]. The aerial part contains dammaranetetracyclic triterpenoids: gynosaponin TN-1[1,2], gynosaponin TN-2, gypenoside I→LXXIX(totally 79), 6′′-malonylgensenoside-Rb1, 6′′-malonylgensenoside-Rd, 6′′-malonylgypenosideV; aglycone: panaxadiol, 2α-hydroxypanaxadiol, (20R,25S)-12β,25-epoxy-20,26-cyclodammaran-3β-ol, (20R,25S)-12β,25-epoxy-20,26-cyclodammaran-2α,3β-diol, gynogeninⅡ;(20S)3β,20,23ζ-trihydroxydamm ar-24-en-21-oicacid-21,23-lactone-3-O-[β-D-glucopyranosyl(1→2)-α-L-arabinopyranosyl]-20-O-β-D-rhamnopyranoside, (20S)-dammar-23ζ-ene-3β,20,25,26-tetrol-3-O-[β-D-glucopyranosyl(1→2)-α-L-arabinopyranosyl]- 20-O-β-D-rhamnopyranosyl-26-O-glucopyranoside, (20R)-dammar-25-en-3β,20,21,24ζ-tetrol-3-O-[β-D-glucopyranosyl-(1→2)-α-L-arabinopyranosyl]-21-O-β-D-glucopyranosyl-24-O-rhamnopyranoside}[2]. |
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[Pharmacological activities] |
1. Impact on immune function: Mice fed the Gynostemma decoction 10g/kg or 30g/kg, and even served 10 days, can significantly increase the spleen weight, promote the monocyte-macrophage cell system of blood colloidal carbon clearance rate and increase the phagocytic function of monocytes 30g/kg also can increase thymus weight [1]. Mice fed Gynostemma decoction and alcohol precipitation water extract of 0.5g/kg ,lg / kg and 2g/kg, and even served 5 days, increase the thymus weight,when with 1.0g / kg and 2.0g/kg it can increase spleen weight [ 3]. Normal mice fed with gypenosides (GPs) 5mg/kg, and even served 10 days, showed a biphasic regulatory role of spleen weight, that is, for these spleen weight is less than the median it can make increase, while make it decrease tothose greater than the median spleen weight; And it can significantly reduce the thymus weight to those are greater than the median. Mice fed GPs200mg/kg or 400mg/kg, for 10 days can significantly antagonize cyclophosphamide-induced thymus and spleen weight reduction.Mice fed GPs400mg/kg, for five consecutive days, to the lymph node weight induced by cyclophosphamide in the thymus, spleen and mesenteric mitigate showed significant antagonism [4]. Mice fed the GPs30Dmg/kg for 7 days, can be significantly enhanced peritoneal macrophage phagocytic function [5]. Fed 3% Gynostemma extract suspension, and even served 50 days, can make the percentage of the D-lactose-induced mice subacute aging model significantly increased the total number of white blood cells, lymphocytes decreased; and the percentage of the reduced neutrophil increased; As to the model group, showed the atrophy of thymus, and spleen weight increased. The thymus index of recovery after treatment, and more than the control group, the spleen index returned to normal; levels of serum lysozyme levels were significantly lower, suggesting that the organism decline in anti-infectious, the lysozyme content of the treated group increased significantly more than control group [6]. Mice fedGPs60mg/kg or 100mg/kg for 7 days can significantly increase the number of peripheral blood leukocytes, and enhanced chemiluminescence engulfed yeast polysaccharide peak, while light-emitting index luminescence peak (white blood cell count) also increased significantly; Fed the mice with acetate prednisone-induced immune suppression GPs80mg/kg or 120mg/kg, and even served seven days, the white blood cell count, peak luminous and luminous index improved more significantly, to prompt GPs can not only increase the normal animal white blood cell count ,but also make the white blood cell count of some animals with low white blood cell count recovery, and enhance normal or low leukocyte phagocytosis [7].Daily service with Gynostemma decoction feed 20g/kg in rats, and even served 15 days,it shows that pulmonary macrophage phagocytic function was significantly inhibited [8]. The water extract o Gynostemma decoction and alcohol precipatation on 10μg/ml, l00μg/ml and 1000μg/ml can enhance ConcanavalinA (ConA) and lipopolysaccharide ( LPS)-induced mouse spleen lymphocyte proliferation response [3]. 10-200μg/ml can stimulate rat and mouse spleen lymphocytes of spontaneous [3H] thymidine nucleoside [3HTdR] infiltrate and incorporate with the appropriate amount of ConA Sub compatibility, may be synergistic stimulation of mouse spleen lymphocytes mixed;In vitro,it also stimulated rat spleen lymphocytes spontaneously secrete white interleukin 2 (IL-2) [9] . GPs small dose 2.5-20μg/m1 of promoting splenic T and B lymphocytes, enhance the DNA polymerase II activity to promote lymphocyte deoxyribonucleic acid (DNA) synthesis, but large doses of GPs showed the opposite effect [10]. The GPs40 and 80μg/ml play a obvious role to ConA, LPS and plant hemagglutinin (PHA)-induced mouse spleen cell proliferative response, but also enhanced the rat spleen cells of IL-2 secretion [11]. Normal mice were injected subcutaneously, 10mg / kg or 30mg/kg, 7 days in a row, both enhance the ConA and LPS-induced splenic T and B lymphocyte proliferation response as the role of l0mg/kg group are more significant, but also improve the spleen cells from IL -2 generation, while the more obvious role is 30mg/kg group. Inject the subcutaneousGPs10m/kg or 20mg/kg into the mice which are induced by cyclophosphamide in immunocompromised,for seven days, the above three indicators were significantly higher, but IL-2 increased the earliest ,T-cellproliferative response enhancement appear late , the 20mg/kg group is more significant. Intraperitoneally inject into mouse with GPs14mg/kg or 24mg/kg for 7days, spleen cells to ConA-induced proliferative response was significantly enhanced [12]. The result of high performance liquid chromatography of monoamine neurotransmitters, shows that hypothalamic norepinephrine content decreased, and spleen were significantly decreased ,proliferative response was negatively correlated with spleen cells; In addition,the plasma corticosterone levels also decreased. The results suggest that, the influence of GPs on the immune response is closely related to the role of neuroendocrine regulatory network, and then play to the immune enhancement [13]. GPs10-80μg/m1 can synergisticly increase ConAnormal mouse spleen cells to produce IL-2 significantly, normal mice abdominal plastic injection GPs144-200mg/kg, for five days, can also be collaborative to make ConA spleen cells to produce IL-2 significantly increased ; rhubarb-induced mouse spleen deficiency syndrome IL-2 activity was significantly lower than normal mice, GPs can be synergistic with ConA and make low IL-2activity to improve both in vitro \ vivo ,and returned to near normal levels [14]. In vitro,GPs10μg/ml to PHA-induced elderly lymphocyte proliferative responses were significantly enhance. To the PHA-induced proliferative response sensitivity the concentration increase or decrease take a anti inhibition, so that GPs have a biphasic regulatory role, elderly lymphocyteis lower than young people lymphocyte, GPs have enhanced the role of lymphocytes when PHA proliferation response is low, when the strong lymphocyte proliferation response to PHA, GPs,compared with inhibition [15,16]. Mice fed the the Gynostemma decoction l0g/kg or 50g/kg, even serving eight days, can significantly increase the serum of sheep red blood cells (SRBC) specific antibodies of hemolysin content [1]. Mice fed Gynostemma decoction and alcohol precipitation water extract of 0.5g / kg, the l.0g/kg or 2.0g/kg, and even served five days, can promote the formation of spleen antibody-secreting cells (PFC) to SRBC immunized mice the 2.0g/kg can promote the formation of hemolysin. Mice fed GPs100mg/kg for 10 days showed a biphasic regulation of SRBC in mice immunized with hemolysin levels ,and a antigonism to the hemolysin levels decrease induced by antagonism [2]. Mice fedGPs400mg/kg even served 5 days, low immune function of tumor-bearing mice or dexamethasone-induced rats produced hemolysin and PFCreduction in irrigation service, GPs showed a significant protective effect. Mice fed GPs300mg/kg for 7 days can significantly increase the serumIgG concentration the Gps separated from the Gynostemma which are producted from another area of Guangxi can make a significantly elevated both in the IgG and 1gM content were significantly elevate [5]. Mice fed Gynostemma decoction 29g/kg, and even served 25 days. Can reduce the number of spleen antibody-forming cells, and the mouse peripheral blood anti-SRBC antibody titers [8]; Mice fed Gynostemma decoction 10, 30g/kg, and even served 12 days shows a significant enhancement of dinitrochlorobenzene (DNCB ) caused [1] by T cell-mediated delayed-type skin hypersensitivity. Mice the gavage GPs200mg/kg or 400mg/kg even served 10 days showed a obvious antagonism to the cyclophosphamide-induced E-rosette formation rate of reduction, and make it returned to normal levels, fed GPs50mg/kg, even for l0 days, showed a biphasic regulation [2] of E-rosette formation rate in normal mice. Tumor-bearing (sarcoma 180) Mice fed GPs400mg/kg, and even served 12 days that dexamethasone-induced immune dysfunction in rats fed with GPs150mg/kgor 300mg/kg, and even served 15 days, to the SRBC immune spleen cells in specific roses formed cells to reduce a significant protective effect[6]. D-galactose subacute aging model mice fed 3% Gynostemma extract suspension 5ml / only for 50 days, allows peripheral blood lymphocytes reduced naphthyl acetate esterase (ANAE)-positive rate improved significantly, and make the DNCB-induced delayed type hypersensitivity was significantly enhanced. Stress (anesthesia, surgery, cardiopulmonary bypass), rheumatic heart disease and congenital heart disease during cardiopulmonary bypass surgery patients with T-cell subsets CD3 +, of CD4 + cells lower, while the CD8 + cells were increased and B cells is also reduced, the difference was very significantly [17]. Reduced in vitro by the GPs after CD3 +, CD4 + cells and B cells were significantly increased. Elevated B-cells decreased significantly, suggesting that GPs have anti-stress effect, have aregutation to the immune suppression moderating role of stress; GPs100μg/m1, 200μg/m1 can strengthen the role of the human peripheral blood NK cell activity, but the 400μg/m1 showed the anti inhibition.Mice fed GPs400mg/kg, and even served 12 days, a significant antagonism [18] to the NK cell activity induced by cyclophosphamide. 2. Anti-tumor: Mice fed GPs50mg / kg of for 7 days, 40% inhibition on murine sarcoma S180 [19]. Mice fed Gynostemma Decoction 1.0g/kg, 2.0g/kg,and even served for 10-12 days, the S180 homogenate inoculated into the mice right axillary tumor growth was significantly inhibited, inhibition rates were 28.9% and 38.1%; To the tumor growth of S180 plug transplants, only exsist weak inhibition, when 7.5g/kg showed significantly inhibited.Leukemia L615 tumor strains of mice were inoculated intraperitoneally 2g/kg of gavage for 7 days, the life prolongation rate is 37.4% the one use the homogenate inoculation,the one use insert block method is up to 66.6%. Increase the dose to 7.5g/kg cann’t extend the life prolong rate but decreased to 29.6% [20]. Inoculated intraperitoneally with S180 mice fed GPs3m / only, and even servedseven days per lml ascites tumor cells was significantly lower than the control group, cells in dividing also decreased significantly, in treatment group the percentage of cells which is in DNA synthesis early (G1) was significantly higher, while cells in the DNA synthesis phase (S phase) were significantly lower than the control group, suggesting that GPs could significantly inhibit tumor cell DNA synthesis. GPs on the S180mice significantly increased the spleen index, but no significant effect on the thymus index, the total number of peripheral blood cells, Thcells, the total number B cells, , of IgM, IgG were significantly higher, suggesting that GPs can not only improve cellular immune function, but also enhance humoral immunity [21]. The anti-tumor effect of GPs require appropriate dose, such as mice fed with GPs10 days, 30mg/kg, on S180tumor inhibition rate of 87.1%, 300mg/kg when the inhibition rate of 61.1%. The 600mg/kg tumor inhibition rate 21.1%. In vitro, GPs, S180cells incubated together for 5 hours, remove and use eosin staining (stained red for dead cells), the GPs concentration of 0.38%, the red dye uptake by 54%;concentration of 0.55%, red dye was 82.7% ; concentration of 0.75%, the red dye was 87.5%, suggesting that GPs S180 cells also have a direct role in the killing [22]. Ehrlich ascites carcinoma in mice were fed with the Gynostemma aerial parts decoction and fresh grain stocks blue callus organizations and water mashed filter (FGP, lg / ml) 0.3ml / ascites gavage 15 days, the entity filling eye 30 days, the ascites type mice, the NGP and FGP can extend its life rate to 40.7% and 46.6% respectively; entity type mice, inhibition rates were 33.1% and 36.2%[23]. Tumor-bearing (Ehrlich ascites carcinoma) mouse peripheral blood acid naphthyl acetate esterase (ANAE) positive cells in phytohemagglutinin (PHA), non-specific conversion rate is lower than normal mice, serving the above-mentioned dose of FGA or NGP Ehrlich carcinoma in mice is significantly higher in these two indicators mouse spleen lymphocytes which applicate the ANAE positive rate of 5 - fluorouracil or cyclophosphamide, decrease the non-specific conversion of PHA and NIC cell is toxic to cancer cells, Ehrlich reduced taking FGP or NCPmice, the above three indicators were significantly increased [24]. In vitro, GPs0.5g/ml, 1.0mg/ml, 2.0mg/ml is inhibited to human hepatoma SMMC-7721 cell’s growth, and concentration; And inhibited the incoporation of 3H-thymidine, 3H-uracil nucleosides and 3H-leucine's; cancer cells, DNA, RNA content reduced when the concentration is lmg / ml, the 2mg/ml, suggesting that the Gpsis inhibited on the cancer cell DNA, RNA and protein synthesis [25]. The Gynostemma decoction drunk Shen extract 5mg (crude drug) / ml allows cultured human hepatoma cell line SMMC-7721 cells rounded, thickened membrane, and shedding the suspended [26]. Hepatic precancerous lesion rats fed with GPs feed (feed the GPsconcentration of 1.5 or 0.48g/kg) serving 14 days, the occurrence of diethylnitrosamine (DEN) induced liver cancer is inhibited [27]. Inhibition of lung cancer cell lines A549, Calu, 592/9 GPs in vitro 1-10g/ml is significantly stronger than the cervical cancer Hela S3 and colon adenocarcinoma Co1o205 while the same concentration of GPs had no inhibitory effect on the normal mixed lymphocyte , but promotion to cell proliferation [28]. Gynostemma extract 1.0g (crude drug) / ml containing saponins 6.44mg/ml, polysaccharide 10.697mg/ml in 1-20μl/ml showed ihibition to human colorectal cancer ( HCe8693) DNA synthesis with dose-related, but at higher concentrations, also inhibited the normal fibroblasts, when the concentration is lower than 10μg/ml, colon cancer cells inhibited the normal fibroblasts fine run without adverse effects [29]. Any C20 or C21 on the dammarane skeleton with free hydroxyl saponins have inhibitory effects on cultured lung cancer, uterine cancer, melanoma tumor cells, while no adverse effects on the proliferation of normal cells [30]. 3. Aging: the Gynostemma significantly extend the cell culture passage algebra. Human skin cells cultured in vitro,with GPs200μg/ml culture medium can increase cells passaged for 27 generations, while the control group can only be passaged for 22 generations. Human fetal lung diploid fibroblast subculture to be similar to the results that transmitted to the control group on behalf of 51, GPs group can be transmitted on behalf of 59 [30]. 0.5% and 1.0% Gynostemma extract solution to drink eclosion the housefly, shows that male and female housefly half survival time, the average life expectancy and the highest life expectancy are extended the role of l% with the Gynostemma group can make the housefly brain superoxide dismutase enzyme (SOD) activity significantly increased, malondialdehyde (MDA), significantly reducted [31].Drosophila medium containing 0.5% and 1% Gynostemma extract extended the average life expectancy of the male flies were 11.8% and 12.2%;concentration of 0.25% on the average life expectancy of male and female flies were extended by 18.5% and 24.1%. 5% grain stocks blue extract in the incubation period the eggs began to administration, the average life expectancy was significantly longer than adults (30 days old) administration, extend the percentage of the former was 53.3% (males), 46.1% (females) ,those for the 14.4% (males), 9.7% [females).Gynostemma extract can promote the growth and development of the Drosophila larvae, but have no impact on the Drosophila life [32]. 5-month-old mice was containing Gynostemma the decoction feed (2.5g basal diet containing 0.1g crude drug) for four monthes the survival is 50%,while 0% survival of control group. Feeding of 2 to increase SOD activity in mice [33]. D-half of the lactose-induced mice subacute aging model, such as intraperitoneal injection of Gynostemma extract suspension 15mg / only for 40 days, can significantly combat aging mice induced by learning initiative to avoid the decline of the ability to respond to the brain monoamine oxidase increase set for the abnormal elevation of enzyme activity and brain lipofuscin, atrophy of the thymus in aging model mice returned to normal levels, and enlarged spleen also returned to normal levels [34]. Young rats fed with Gynostemma aqueous extract of dry extract feed 200mg/kg for three months, can enable the brain, heart tissue lipofuscin content decreased, although lipofuscin content in the liver has no significant differences with the control group, but also lower than the control group.Aged rats fed with 0.5% and 0.25% Jiaogulan aqueous extract of dry extract for 2.5 monthes, heart, liver and brain tissues through lipid peroxidation(LPO) have significantly reduced [35] and 0.5% concentrations to serum and liver total cholesterol, triglycerides have significantly decreased; in vitro, 250μg/1.5m1 and 500μg/1.5m1 of concentration on the rat heart, brain, liver tissue content of LPO were significantly reduced.Mice fed 2 months with GPs80mg/kg, plasma liver and brain LPO levels were significantly reduced, and the activity of the liver and brain SOD were increased, it can also reduce the mouse skin hydroxyproline content, suggesting that GPs have antioxidant and anti-aging [36]. 4. Impact on lipid metabolism: the intake of high sugar high fat diet-induced hyperlipidemic rats significantly increased serum neutral fat. LPO increased in blood, if service GPs500mg/kg, l00mg/kg (taking mixed in feed) 7 weeks, the serum neutral fat, total cholesterol level decreased significantly, the increase in liver LPO can be inhibited [37]. Rabbits with Experimental hyperlipidemia fed with GPs100mg/kg four weeks, the total cholesterol (TC) can be significantly increased, does not seem to impact on triglyceride (TG) and high-density lipoprotein cholesterol (HDLc). Currently advocating the use As, I (atherosclerosis index) = (TC-HDLc) / HDLc, HDLc / TC to measure the susceptibility of the individual As calculations show that GPs can significantly reduce the AsI improve the HDLc / TC, undoubtedly it’s a positive significance to preventive As. Macromolecules in the form of As plaques of cholesterol low-density lipoprotein (LPL) deposition in the arterial wall induce wall smooth muscle cell proliferation, vascular endothelial cells, calculations show that, GPs can significantly lower LDL levels, and prevent As with good. Qualitative content of hyperlipidemia rabbit serum LPO and myocardial lipofuscinosis were significantly higher than normal rabbits, suggesting that GPs can significantly reduce serum LPO and myocardial lipid lipofuscin (Lf), showed that GPs can against with oxygen free radicals and protect the role of the intima [38]; hyperlipidemia rats fed GPs 100mg/kg, 300mg/kg 15 days, can make blood TC, TG and LDLlower the HDL / LDL ratio was significantly increased. Mice to drinking GPs300mp/kg four months, can inhibit or clear the L1 formation of the myocardium [39], intraperitoneal injection of fresh egg yellow latex-induced hyperlipidemic mice, gavage GPs200mg/kg, 7 days can significantly reduce blood TC concentration; the high fat diet in hyperlipidemic rats fed with GPs200mg/kg 7 days, can significantly reduce the content of TC, LDL and very low density lipoprotein (VLDL), increased HDL and HDL / LDL rate [40], patients with hyperlipidemia takingGPs can also reduce blood TC, TG, LDLc [41-43]. Service GPs40mg 30 days in patients with hyperlipidemia, can significantly lower the content of serum apolipoprotein (apoB100) and lipoprotein [Lp (a)] that has an important significance to improve the blood supply to body tissue, prevent atherosclerosis, while it has no significant effect on serum HDLc, LDLc and VLDL and TC, TG content [44]. The mice were free to drink the Gynostemma alcohol extract of 13 days, can not only improve the liver SOD activity, but also enhance the SOD heat-resistant acid resistance, since the protection of SOD [45]. In vitro, GPs can significantly inhibite the formation of gavageGPs0.25/kg, 8 days in the ozone cabinet and continue administration of l0 days, can the liver and plasma LPO content significantly lower than controls, erythrocyte SOD activity was also significantly higher. Aged rats (26 months), water service GPs0.05g/kg 80 days, can also significantly reduce liver LPO content, enhance erythrocyte SOD activity [46]. In vitro when in GPs2.5-160μg/ml the D-cysteine, vitamin C-NADPH, and carbon tetrachloride-induced rat liver microsomal MDA formation and spontaneous MDA production were inhibited, and in The dose-effect relationship. Dose compared the efficacy of the GPs was significantly higher than the total ginseng soap into. Fe2 + cysteine-induced injury of rat liver microsomal and mitochondrial membrane emblem viscosity is significantly increased, indicating that the membrane fluidity, such at the same time joining GPs2.5-150μg/ml it can against the decreasing of membrane fluidity, but has no influence on intact normal liver microsomes, the mitochondrial membrane fluidity [47]. Guinea pig papillary muscle oxygen free radicals induced by xanthine - xanthine oxidase (X-XOD) system, in the X-XODrole of papillary ,muscle contractile force first increased and then decreased, the function should not be shortened, excitatory improve, the self-regulation of the adrenaline-induced increase,and in myocardial ,the SOD activity decreased, while MDA content increased. If give GPs50μg/ml first,and then giveX--of XOD, the papillary muscle contraction peak will be postpone, and inhibit its negative inotropic effect, at the same time,change the reversal of theX-XOD due to papillary muscle refractory period, excitability and self-discipline MDA content in the myocardial tissue to recover, suggesting that GPs have a protective effect on the guinea pig myocardial oxidative damage [48]. Electrolytic the Kreh liquid and get oxygen free radicals (OFR) it can allow acetylcholine (Ach)-induced rabbit aortic annulus percentage significantly reduce. GPs25μg / m1, 50μg / m1 is,the 100μg/ml can protect endothelial from OFR injury, GPs50μg / ml the role can be blocked by indomethacin (INDO) X-XOD also reduce vascular ring diastolic function, GPs100μg/ml can against the X-XOD injury [49]. GPs100μg/ml also against vascular ring diastolic dysfunction due to methylene blue (Mb) . Vascular endothelial can release prostacyclin (PGI2) and endothelium-derived relaxation factor (EDRF) to regulate vascular tone and enhance their own ability to damage resistance, the OFR in induced vasodilation reduced ability will reduce the endothelial release of EDRF, GPs can confront Mb inhibition of EDRF induced vasodilation decreased, GPs may protect EDRF activity. The role of GPs can INDOblocked, indicating that the GPs role in the release of PGI2 and then anti-membrane lipid peroxidation [49], can reduce superoxide anion and hydrogen peroxide content in human neutrophils by promoting organization; on human monocyte giant cells and mouse macrophages, GPs can reduce the chemiluminescent oxidative burst triggered by the yeast polysaccharide; Fe2 + cysteine, ascorbic acid-NADPH or over the hydrogen peroxide of LPO in liver microsomes and vascular endothelial cells to increase, GPs can inhibit the role of oxidative damage and reduced liver microsomal and light mitochondrial membrane fluidity, GPs can be reversed to increase the activity of mitochondrial enzyme of vascular endothelial cells. Reduce lactate dehydrogenase leakage in these cells, suggesting that GPs can protect the biofilm from oxidative damage and hardening the GPs extensive antioxidant effect of a variety of diseases such as atherosclerosis Cheung, prevention and treatment of liver disease and inflammation can be pricing. It was noted that changes in the composition of lipid oxidation allows a higher lipid content of the biofilm, and makes the DNA, RNA structure be damaged, causing cross-linking of protein molecules, leading to cell aging and the Gynostemma significantly reduce the role of LPO noteworthy [50]. Gynostemma can inhibit fat cells to produce free fatty acids and synthesis of neutral fat. Preparation of rat epididymal adipose tissue fat cells were cultured in culture medium plus ACTH or epinephrine may cause the fat cells break down and produce free fatty acids, such as add GPs to reduce the generation of free fatty acids amounted to 28%. Counts per minute (CPM) to fat cells and tracer compounds 14C-glucose at 37 ℃ for co-cultivation for 30 minutes, the determination of fat cells as the glucose into the cells to synthesize neutral refers to the anti-index, add medium GPs per gram the number of fat cells measured CPM is only about 50% of the non-plus GPs [50]. 5. The role of the cardiovascular system : The low concentration of GPs have excitatory effects on isolated frog heart, t when2.4mg/ml showed he strongest effect, when 4mg/ml Showed inhibition Anesthetized rabbits intravenously GPs 8mg/kg, significantly higher blood pressure, 16mg/kg when blood pressure was significantly reduced, and antagonized the effect of pituitrin caused by myocardial ischemic T-wave height and ST segment depression [51]. Anesthetized dogs to intravenous GPs8mg/kg or 10mg/kg, it can reduce the dog blood pressure and total peripheral resistance, cerebrovascular and coronary vascular resistance and increase coronary blood flow, heart rate, decrease cardiac tension - time index (indirectly reflect myocardial reduce oxygen consumption), while had no significant effect on myocardial contractility and heart function, slightly stronger than the same amount of total ginsenoside role [52]. Intravenous GPs 1 mg / kg can improve systolic and diastolic blood pressure, significantly improved myocardial systolic and diastolic performance, enhanced myocardial contractility. When the left ventricular systolicin speed, peripheral resistance does not increase, thereby increasing the heart minute volume. Arterial diastolic blood pressure can increase coronary blood flow and improve heart and blood circulation, but the intravenous GPs20mg/kg,the blood pressure, heart rate, left ventricular systolic pressure and its maximal rate, cardiac index, all significantly decreased, heart rate and heart index decreased at the same time, showed that the cardiac minute output is reduced, the small-dose GPs can enhance intravenous cardiac function, and large doses will make cardiac function inhibition [53]. Ligation of the coronary artery for 40 minutes, lifting ligation to restore blood flow and with 20 minutes reperfusion, intravenousGPs20mg/kg can significantly improve the myocardial tissue glutathione peroxidase (GSH-px) activity and reduce the MDA content restore the reduced mitochondrial membrane fluidity, reduce the damage of myocardial ultrastructural leaded by reperfusion, suggesting that GPs have a protective effect on myocardial ischemia reperfusion injury, the mechanism is related to antioxidant effect [54]. Stop filling in isolated rat hearts for 30 minutes and reperfusion for 20 minutes, GPs30μg/ml and 50μg/ml can significantly reduce the irreversible ventricular fibrillation incidence, 50μg/ml can significantly inhibitthe release of myocardial lactate dehydrogenase, GPs can also improve ischemia and reperfusion myocardial SOD activity,and significantly reduced MDA levels,and make protective effect on myocardial ischemia-reperfusion injury [55]. Ligating rats with acute myocardial infarction caused by Coronary artery , in the first three minutes of ligation and after ligation immediately do intraperitoneal injection of GPs25mg/kg enable ischemia 24 hours of myocardial infarct size significantly reduced and ischemia 6 hours and l0-hour serum creatine phosphate kinase [CPK) and lactate dehydrogenase (LDH) significantly reduced 30 minutes after the ischemic border zone in the ischemic myocardial ultrastructural injury significantly reduced. In vitro, GPs50μg/ml, 100μg/ml and 200μg/ml can reduce cultured rat myocardial cells of oxygen and glucose deprivation injury, inhibite the release of OGD 6 hours of myocardial cells,.Anesthetized rats the of intravenous GPs10mg/kg or 20mg/kg, 30 minutes, heart rate, blood pressure, left ventricular systolic and diastolic blood pressure, left ventricular pressure change in the maximum, cardiac index and other hemodynamic parameters had no obvious changes [56] .Do ligation in rabbits with the left coronary artery ligation caused myocardial infarction produce I, 30 minutes before surgery,and do intraperitoneal injection of GPs 100mg/kg reduce ΣSC (chest lead ECG St segment elevation the total mV) and NST (number of ECG ST-segment elevation), shows no significant difference in statistics ,but significant reduction to the total ginsenoside (GS) when in 50mg/kg, GPs100mg/kg can significantly reduce the elevation of infarction, serum free fatty acid (FFA). It can significantly reduced myocardial infarct size, but weaker than the GS role. Ligating left coronary artery in left ventricular branch of the rat myocardial infarction, preoperative intraperitoneal injection of 100mg/kg, GPs andFGNG (non-ginsenoside part) could significantly inhibit the MDA increased after myocardial infarction, infarct FGNG can then make the decreased SOD activity increased, GPs and GS, also have the tend to increase the SOD activity and myocardial infarction caused by CPK activity was significantly increased made by the GS ,GPs and GS also allows the rise, but close to statistically significant [57]. GPs on endotoxin shock in rabbits within the obvious anti-shock and prevention of secondary disseminated intravascular coagulation [58]. Intraperitoneal injection GPs40mg/kg can significantly prolong lidocaine poisoning survival time of mice intraperitoneally GPs80m/kg can significantly increase the tolerance dose of lidocaine [59]. In vitro, GPs 2μg/ml can significantly extend the guinea pig atrial functional refractory period (FRP), a concentration-dependent 0.01-1μg/ml can lower self-regulation of isolated guinea pig right atrium, and have no significant effect on right atrial muscle contractility [60]. Static anesthetized cats to GPs50mg/kg, blood pressure decreased by 40.7%, to maintain more than 30 minutes, heart rate did not change the pulse pressure increases, Pu Cai lol hydrochloride (propranolol) does not block the antihypertensive effect [60]. 6. On blood coagulation and platelet aggregation: in vitro, GPs 0.25-1.0mg/ml can promote platelet depolymerizationof the free arachidonic acid (AA) induced platelet aggregation, on collagen-induced platelet aggregation,it can make aggregation curve slope became smaller and smaller, incubation period gradually extended, indicating that it can slow down the rate of platelet aggregation, rabbits intravenously GPs 40mg/kg, it can significantly inhibite platelet aggregation induced by ADP, AA and collagen, which lasted about 60 minutes , and show the strongest inhibitory effect at the fifth minutes,.In vitro, GPs can significantly inhibit the release of collagen-induced platelet 5hydroxytryptamine (5-HT), in the inhibition of platelet aggregation concentration, and elevated AMP levels in platelets, and the effect of dose [61]. Subcutaneous injection of GPs 50mg/kg, can inhibit platelet thrombosis and venous thrombosis. 6 - keto-prostaglandin F10 in vitro 0.25-1.0mg/ml the platelet thromboxane B2 (TXB2) and aortic (The formation of 6-keto-PGF10) was inhibited by the IC50 of 1.03mg/ml and l.15 mg of / ml. That GPs can inhibit AA metabolism, may be one of the mechanisms if inhibiting platelet aggregation and experimental thrombosis of [62]. In vitro, Gynostemma decoction and alcohol precipitation extract 0.25-2g / L can significantly inhibited rabbit platelet aggregation induced by AA and TXB2 release the EC500 inhibition of TXB2 is 28mg/ml. Extract of rabbit intravenous 35mg/kg at 10 minutes and 20 minutes, the AA-induced platelet aggregation was significantly inhibited, during 10-40 minutes the platelet release of TXB2 was significantly reduced. In vitro 0.25-4mg/ml had no effect on rabbit thoracic aorta release 6-keto-PGF10 and it showed that the extract play a better role [6to reduce TXA2 / prostacyclin ratio 3]. The vitro studies carried out by the employing blood show that Gynostemma decoction 0.25mg/ml significantly inhibited ADP complex inducer (by the same amount of ADP, epinephrine and acid mucopolysaccharide composition) induced platelet 1 minute and 5 minutes maximum aggregation rate, and promote depolymerization occurred, also significantly inhibited thrombus formation in vitro. The mix of Decoction and platelet-poor plasma, can still inhibit the activity of clotting factors [64], kaolin partial thromboplastin enzyme time (KPTT), prothrombin time (PT), thrombin time (TT), the venom of Agkistrodon time (SAT), viper venom, the recalcification time (RVV-RT}, viper venom the phospholipid time coagulation test time [65,66]. 7. The role of the central nervous system: Gynostemma extract of mice by intraperitoneal injection of 100mg/kg, 200mg/kg, it can significantly prolong pentobarbital sleep time [65]. Mice fed Gynostemma extract (including GPs about 20%) at 450mg/kg can significantly reduc spontaneous locomotor activity in mice [67], indicating that the Gynostemma or contained was of significant sedation. Mice fed cream 450mg/kg, hot plate method proved to be a significant analgesic effect of short-term increase in normal mice body temperature, and significantly enhanced in mice hypoxia tolerance effect. The swimming test has significant anti-fatigue effects, and significant high-temperature effects [67]. Mice fed the GPs150mg/kg and continued for 3 days, can prolong the swimming time, also significantly prolong the climbing pole time; the abdominal the injection GPs200mg/kg significantly extend the hypoxia tolerance time. Blood in the rat after a long swim pond level and muscle glycogen content was significantly decreased,after a long swim the gavage Gynostemma extract 200m/kg for total of 14 days, then can make the long swim rats to maintain a high blood sugar levels, reduce the loss of muscle glycogen [68]. GPs can also reduce the number of hinf limb caused by scratch intramuscular injection of mescaline, reducing the mice writhing number caused by the intraperitoneal injection of acetic acid . Also indicated that the sedative and analgesic effects of GPs [50]. Mice were injected three extracts of subcutaneously Gynostemma (water, 20% ethanol and 95% B drunk extract) 3g/kg 4-5 days in a row, can improve learning acquisition impairment caused by the anisodine; Gynostemma 20% ethanol extract consolidate the bad and 20% ethanol-induced memory retrieval obstacles have antagonistic effects on memory caused by protein synthesis inhibitors (imide ring, chloramphenicol) [69]. Total of five days in mice by intraperitoneal injection of reserpine 0.25m/kg ,it can make weight, body temperature, spontaneous activity was significantly decreased, and cause ptosis, arched back bending, diarrhea, body hair, dull, and so on .gavageGPs50mg/kg, 100mg / kg, 200mg/kg, for 10 days. Can significantly improve the reserpine-induced body weight, body temperature and spontaneous activity decreased, while making the diarrhea Ptosis, arched back bending, body Maolong Guang Ze improved. GPs can improve Reserpine depletion of monoamine transmitters, but had no significant effect on the normal mouse brain monoamine neurotransmitters and some metabolites , does not cause obvious signs of change [70]. Cerebral ischemia and reperfusion brain injury model coefficients (brain weight / body weight) are higher than control group, injected intraperitoneally 15 minutes before ischemia with GPs100mg/kg will enable the brain factor, brain water content, brain tissueMDA levels, reduce, [71] showed that the GPs have apparent protective effect on ischemia reperfusion injury. Close bilateral common carotid arteries in rabbits, while the low voltage and low-irrigation causes an acute incomplete cerebral ischemia, the intravenous GPs50mg/kg can significantly improve the EEG changes after cerebral ischemia of 60 minutes, reduce the cerebral venous blood lactate dehydrogenase ( LDH)and creatine phosphokinase (CPK) activity, improve the morphological changes of the brain following cerebral ischemia, suggesting thatGPs have a protective effect against cerebral ischemia [72]. 8. Glucose metabolism: mice fed Gynostemma extract 100mg/kg, 200mg/kg. 3 days, shows a significant hypoglycemic effect in alloxan diabetes model; and significantly improved the lower of blood glucose tolerance in aged rats [78]; It was found that the gypenosides can stimulate islet cells release insulin, and dose-dependent manner. A new saponin, named phanoside. the separation and purification of Gynostemma The in vitro experiments, different concentrations of the Gynostemma ethanol extract in glucose concentration of 3.3, 16.7 mmol / L can promote normal male Wistar rats release insulin from rat pancreatic islet cells, dose a dependent manner. When The glucose concentration was 3.3 mmol / Lconcentration of insulin release in the control group was (12.1 ± 1.8) u / (islet hours), 2, 4 mg / mL insulin release concentration of Gynostemma pentaphyllum ethanol extract is (63.4 ± 5.0) and (103.0 +15.4) / (islet · h) and showed significantly different compared with the control group. When the Glucose concentration was 16.7 mmol / L, control group, the release of insulin concentration was (29.2 ± 6.5) / (islet · hours), insulin release concentration of 2 mg / ml Gynostemma ethanol extract is (42.4 ± 4.0) / (islet · h ), insulin release concentration of 4 mg / ml Gynostemma ethanol extract of (94.8 ± 9.8) u / (is1et · h) compared with the control group it was a significant difference. Purified compounds phanosidealso can significantly increase insulin release, and shows a certain dose-response relationship, the largest administered concentration, 5 mmol / Lof the compound in 3.3 mmol / L and 16.7 mmol / L glucose concentration of insulin The release of insulin are 10 times before dosing, respectively, and nearly four times, and several times the maximum effective amount of the urea glibenclamide role. In animal experiments, normal male Wistar rats were given DMSO (2.5% of 1 ml/l00 g body weight) gavage administration groups containing phanoside40 and 810 mg / kg of body weight, the control group to 2.5%After the Sulfoxide orally administered 90 minutes then intraperitoneal injection of glucose and plasma insulin levels, after more 30 minutes the drug group were significantly higher than that. The Gynostemma polysaccharide has a strong inhibitory effect on amylase in vitro, and showed a dose dependent manner, the inhibition rate is equivalent to about 50% of the same concentration of acarbose inhibition. By comparison to Gynostemma polysaccharide dose-response curves, the aging curve, he result suggesting that its inhibition might be reversible, and there may be time dependent, that is, there is an optimal duration of amylase. In vitro experiments showed that Gynostemma can effectively inhibit a-glucosidase activity, compared with acarbose (IC50: 53.9μg/ml) and its 50% effective inhibition concentration is lower(IC50: 42.8μg/ml) [84]. 9. Others: Intraperitoneal injection of GPs 10mg/kg 10 days to prevent dexamethasone-induced adrenal and thymic atrophy and the reduction of plasma cortisol content [73,74], fed GPs70mg/kg 350mg/kg, a total of 6 days can prevent dexamethasone-induced adrenal atrophy, and enable increased adrenal vitamin C content decreased [75], suggesting that GPs can be tested in drugs of anti-glucocorticoid side effects. Mice fed extracts of 20days, can significantly increase the weight of the male testicles, seminal vesicle, prostate and female sub-officer, suggesting that it had male and female hormone-like effects [76]. Injected subcutaneously GPs50ms/kg six days, could significantly inhibit the carbon tetrachloride-induced serum alanine aminotransferase (ALT), elevated dynamic, biopsy revealed vacuolar degeneration of liver cells, inflammatory not Run necrosis etc. improved markedly. Removal of 70% of the liver in rats surgery, will enable the number of fission of the residual liver increased significantly. Liver regeneration was significantly higher, indicate that it can promote the regeneration of liver cells [77]. GPs has protective effects on stress ulcer caused by the flooding in rats. GPs100m/kg five days in a row, have a therapeutic effect on the rat acetic acid-induced gastric ulcer. High glucose and fat-induced hyperlipemia often accompanied by liver injury, serum ALT rose GPs100mg/kg 500mg/kg added to the feed to take seven weeks, and allows elevated ALT decreased significantly, suggesting that GPs have hepatoprotective effect [80], but Mice fed GPs250mg/kg 500mg/kg, morning and afternoon 1 the next day afternoon intraperitoneal injection can cause liver injury in carbon tetrachloride, the first three days measured the ALT ,the results shows that GPs has no hepatoprotective effect. Gynostemma decoction of mice fed 10g/kg, 30g/kg, for7 days were significantly inhibited auricular inflammation caused by topical application of xylene, also markedly inhibited by intraperitoneal injection of acetic acid-induced capillary permeability increased. 5g/kg of rats fed with a total of 7 days can significantly inhibite the carrageenin-induced ankle swelling, although gavage the 15g/kg ankle swelling suppression but exsist no statistically significant.Significantly inhibited the rat granuloma While to tht 5g/kg and 15g/kg suppression strength is close. Indicate that Gynostemma inhibit exudative inflammation and proliferative inflammation. Mice fed Gynostemma decoction 0.06 / 0.12g / only a total of 10 days, and take sister chromatid exchange as an indicator, there is no mutagenic effect, can make the cyclophosphamide-induced mutations significantly reduced. Take the Cyclophosphamide induced micronucleus, chromosomal aberrations and sperm abnormality as an indicator, GPs have anti-mutagenic effects [81]. Take A flat, daunorubicin, azides sodium, mitomycin C, respectively, as the strains of Salmonella mutagenicity, TA98, TA100, and TA102 as the mutagenic factors, the decline in the number of revertant colonies as an indicator, GPs in vitro can antagonize the above four kinds of the mutagenic effect of mutagenic factors and dose-response relationship [82]. 10. Pharmacokinetics: rabbits intramuscularly GPs300mg/kg, absorbed quickly, widely distributed, slow excretion, 24-hour total urine emissions equivalent to about 10% of the total dose, plasma concentration also appeared bimodal, suggesting that GPs maytake the exsist of enterohepatic circulation. The GPs kinetics of the two compartment model, the main pharmacokinetic parameters are as follows: absorption half-life of 0.289hours, eliminating the half-life of 16.440 hours, blood drug peak 163.598μg/ml [83]. |
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[Clinical trial] | 1. Hyperlipidemia:Gypenosides tablet on treating hyperlipidemia in clinical observation in 112cases, Orally,3 tablets per time, 3 times per day. Results: Treatment for 40 days ,that TCdecreased 18.20%, the total effective rate was 81.52%, TG decreased by an average of 31.60%,the total effective rate was 83.58%, LDL-C decreased by an average of 25.59%,the total effective rate was 73.08%,HDL-C increased by 4.89%, the total effective rate was 47.83% 2.anti-aging: Treatment of Jiaogulan capsule for 100cases of aging, 3 capsules per time, 3 times per day, a course per 2 months.Results: 12 symptom integral average value decreased, the comparison of beforeand after treatment, the result was significant(P<0.01) [2]. 3. vascularheadache: Jiaogulan 20 g, boiling in water as tea drink, an agent per day, threemonths as one course of treatment. If the effect was not good person can take 1 couse again, better or cure,consolidate the treatment for half a year. results showed that 32 cases hadcured in 46 cases of treatment (69.6%),10 cases were effective (21.7%), 4 caseswere invalid (8.7%), and the total effective rate were 91.3% [3]. 4.Coronary heart disease, angina: Gypenosides tablet, 3 tablet per time, 3 timesper day, 4 months as one course of treatment. 80 cases were treated, 13 caseswere cure. accounting for 16.25%, 35 cases were markedly improved, accountingfor 43.75%, 25 cases were improve, accounting for 31.25% ,7 cases were invalid,accounting for 8.75%, the total effective rate was 91.25%[4]. 5. Leukopenia: Jiaogulankoufuye(Each l0ml,contains ginseng saponins 20 mg), 2 bottles per time,3 times per day,15 days asone course of treatment,39 cases were treated for 2 courses ,result showed that21 cases were markedly improved, 15 cases were effective , 3 cases were invalid, thetotal effective rate was 92.31%[5]. 6. Hepatitis B:Hangshanjiaogulanchongji,2 times per day, 25 g per time,6months as one courseof treatment,200 cases were treated , Ⅰ level curative effect in 52 cases (26%); Ⅱ level curative effect 139 cases (69.5%); Ⅲ level curative effect in 9 cases (4.5%); I+Ⅱlevel curativeeffect was 95.5%[6]. 7. Sebaceousglands disease: Jiaogulan totalglucoside capsule ,40mg per time,3 times per day, 15 days as one course oftreatment,88 cases were treated for 2 courses,38 cases were cured , 43 caseswere powerfully and effective, the total effective rate was 92.0%[7]. 8. Psoriasisvulgaris: Jiaogulan total glucosidecapsule,2 capsules per time,3 times per day, 30 days as one course oftreatment,120 cases were treated for 2 courses to judge curative effect, thetotal effective rate was 85.92% for course above 1 years of the patient, 10years or more effective rate was 74.61%[8]. 9.Brotherstinea: Fresh leaf of Jiaogulan stem 30 ~ 90 g, dip juice besmear brushrepeatedly affected part, 3 to 5 times per day, to treat for 5 ~ 7,. Treatmentof 100 patients were all recovered[9]. 10. Chronicbronchitis: Jiaogulan bag tea agent,2 times per day, 1 bag per time, Treatmentin 86 cases were treated, 12 cases were cured, 23 cases were powerfully, 45cases were better, 6 cases were invalid, the total effective rate was 93.02%[10]. 11. Chronicatrophic gastritis: Jiaogulanchongji,10 g per time,3 times per day,3months as 1 courses of treatment, after1 course, 28 cases were improved, 57cases were for better and 58 cases were invalid, 8 cases were aggravated, thetotal effective rate was 56.26%[11] . |
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[Properties] | ||
[Medical and other Uses] | ||
[Dosage] | ||
[Cautions] | ||
[Traditional usage] |
1. Chronic bronchitis 2. Strain, nocturnal emission |
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[Toxicological studies] | ||
[Pharmaceutical preparations] |
1. QuanfukangOral Liquid:milkvetchroot, coastal glehnia root, cochinchinese asparagus root, ophiopogon root,glossy privet fruit(processing with wine), dogwood fruit, epimedium, faenumgraecum(stir-frying with salt water), gynostemma pentaphylla, doederlein’s spikemossherb, all-grass of Chinese sage, paris root. |
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[References] |
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