Gynostemma Extract targets endogenous metabolite pathways and acts as an antioxidant agent. It increases the activity and protein expression of antioxidant enzymes such as SOD and glutathione peroxidase. The extract reduces stress-induced c-fos expression, indicating its effects on stress-responsive signaling pathways. It also shows anxiolytic and antidiabetic effects in vivo, suggesting modulation of neurotransmitter systems and glucose metabolism. In liver injury models, Gynostemma Extract reduces the increase of SGOT and SGPT activities, indicating hepatoprotective effects. The extract's multiple targets and pathways contribute to its diverse pharmacological activities, including antioxidant, anxiolytic, antidiabetic, and hepatoprotective effects.

A short period of hypoxia/hypoglycaemia (oxygen and glucose deprivation, OGD) induced by perfusion with O(2)/glucose-free medium caused immediate loss and incomplete restoration of evoked field potentials in the CA1 region of transverse hippocampus slices. OGD-dependent decrease in evoked field potentials can be prevented by a proceeding short OGD event (preconditioning). We report about a study investigating the effect of an ethanolic Gynostemma pentaphyllum extract on evoked field potentials when administered before the OGD episode. Using this procedure, the extract completely protected the cells of the slices from functional injury. In an astroglia rich cell culture the ethanolic Gynostemma pentaphyllum extract caused within 48 h of cultivation increased protein and activity levels of the anti-oxidative enzymes manganese superoxide dismutase (Mn-SOD) and glutathione peroxidase (GPx). Consequently, the cellular H(2)O(2) concentration remained at a low level. These data suggest that the Gynostemma pentaphyllum-mediated increase in antioxidative enzyme activities may contribute to the protection of transverse hippocampus slices from OGD induced functional injury. Our results demonstrate that the prophylactic administration of the ethanolic extract from Gynostemma pentaphyllum has a high potential to protect from ischemia/reperfusion injury.[2]
In vitro studies have demonstrated that Gynostemma Extract has significant free radical-scavenging activity. It increases the activity and protein expression of SOD and glutathione peroxidase. The extract has been evaluated for its antioxidant, whitening, moisturizing, and antibacterial properties in vitro. Gynostemma Extract also reduces stress-induced c-fos expression in cell-based assays. Its antioxidant capacity has been compared between wild and artificially cultivated Gynostemma, with wild extract showing slightly higher activity. The extract is typically tested in various in vitro systems, including cell-free antioxidant assays (e.g., DPPH, ABTS) and cell-based assays (e.g., oxidative stress models), to evaluate its protective effects against oxidative damage.

In this study, the effects of herbal ethanol extracts of Gynostemma pentaphyllum (GP-EX), on chronic electric footshock (EF) stress-induced anxiety disorders were investigated in mice, which were orally treated with GP-EX (30 mg/kg and 50 mg/kg) once a day for 14 days, followed by exposure to EF stress (2 mA, with an interval and duration of 10 s for 3 min). After the final exposure to EF stress, the elevated plus-maze and marble burying tests were performed, and the levels of dopamine and serotonin in the brain, the serum levels of corticosterone, and the expression of c-Fos in the paraventricular nuclei (PVN) were determined. Treatment with GP-EX (30 mg/kg and 50 mg/kg) significantly recovered the number of entries into open arms and time spent on open arms, which was reduced by chronic EF stress. GP-EX (30 mg/kg and 50 mg/kg) also reduced the number of marbles buried, which was increased by chronic EF stress. In addition, electric EF stress significantly decreased the levels of dopamine and serotonin in the brain, which was recovered by treatment with GP-EX (30 mg/kg and 50 mg/kg). The serum levels of corticosterone, which were markedly increased by chronic EF stress, were reduced by treatment with GP-EX (30 mg/kg and 50 mg/kg). Chronic EF stress-induced increases in c-Fos expression were also markedly reduced by GP-EX (30 mg/kg and 50 mg/kg) in the PVN. These results suggest that GP-EX shows anxiolytic functions, determined by the elevated plus-maze and marble burying tests, which are mediated by modulating the activity of dopamine and serotonin neurons as well as the expression of c-Fos in the brain, and the serum levels of corticosterone. Clinical trials of herbal GP-EX and its bioactive components need further investigation.[1]
Gynostemma pentaphyllum (GP, Cucurbitaceae) has been used as an herbal tea containing various bioactive gypenoside derivatives and flavonoids, and has been found to have pharmacological functions against diabetes, fatigue, hyperlipidemia, immunity, oxidative stress and tumors . Recently, the ethanol extract from GP (GP-EX) has been reported to have anti-stress properties, by improving the loss of body weight and the reduction of grip strength which was induced by chronic EF stress as well as an immunomodulatory function in mice . [1]
In vivo studies have shown that Gynostemma Extract is an orally active antioxidant agent. It reduces stress-induced c-fos expression and shows anxiolytic and antidiabetic effects in vivo. In CCl4 liver injury models, treatment with Gypenoside significantly reduced the increase of SGOT and SGPT activities and elevated the A/G ratio. These findings indicate hepatoprotective effects of the extract. Gynostemma Extract has also been studied for its antidiabetic effects, though specific details are less extensively documented. The extract's in vivo activities support its traditional use as a health-promoting agent. Further studies are needed to fully characterize its mechanisms of action and therapeutic potential.

Non-cellular assays for Gynostemma Extract typically involve measuring its antioxidant activity using cell-free systems such as DPPH (2,2-diphenyl-1-picrylhydrazyl) radical scavenging, ABTS (2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid)) radical scavenging, and superoxide radical scavenging assays. The extract's ability to scavenge free radicals is measured spectrophotometrically by monitoring the reduction of absorbance at specific wavelengths. The extract is tested at various concentrations to determine its IC50 for radical scavenging. Enzyme activity assays for SOD and glutathione peroxidase may also be performed using purified enzymes or tissue homogenates to assess the extract's effects on these antioxidant enzymes. These assays provide a biochemical basis for the extract's antioxidant properties.

In vitro cell-based assays for Gynostemma Extract typically use various cell lines to assess its antioxidant, anti-inflammatory, and cytoprotective effects. Cells are cultured in appropriate media and treated with the extract at various concentrations. Oxidative stress is induced using agents such as H2O2 or CCl4, and the protective effects of the extract are assessed by measuring cell viability (MTT assay), reactive oxygen species (ROS) levels, and antioxidant enzyme activities (SOD, glutathione peroxidase). Stress-induced c-fos expression is measured by qRT-PCR or Western blotting to assess the extract's effects on stress-responsive signaling. The extract's whitening and moisturizing effects can also be evaluated in skin cell models. Gynostemma Extract is typically dissolved in DMSO or water and diluted in culture medium.

In vivo animal studies for Gynostemma Extract typically involve rodent models of oxidative stress, liver injury, diabetes, or anxiety. For liver injury studies, animals are treated with CCl4 to induce hepatotoxicity, and the protective effects of the extract are assessed by measuring serum SGOT and SGPT activities, as well as liver histology. For antidiabetic studies, diabetic animal models (e.g., streptozotocin-induced diabetic rats) are used, and blood glucose levels and insulin sensitivity are measured. For anxiolytic studies, behavioral tests such as elevated plus maze or open field test are used to assess anxiety-like behaviors. The extract is typically administered orally, and its effects are evaluated over a period of days to weeks. Body weight, food intake, and general health parameters are monitored throughout the study.

Pharmacokinetic data for Gynostemma Extract are limited. As a complex mixture of saponins, the extract's pharmacokinetic profile is expected to be complex, with multiple components having different absorption, distribution, metabolism, and excretion characteristics. The extract is orally active, indicating that its components are absorbed from the gastrointestinal tract. The molecular weight of the major component (Ginsenoside C-Mx1) is 917.13 g/mol. The extract is soluble in DMSO at 189 mg/mL (206.07 mM). However, detailed PK parameters such as half-life, Cmax, AUC, and bioavailability for individual components have not been extensively reported. Research-grade Gynostemma Extract is intended for laboratory use only.

Toxicological data for Gynostemma Extract suggest a favorable safety profile, consistent with its long history of use as a traditional herbal medicine. In animal studies, the extract has been shown to be well-tolerated at therapeutic doses. The extract's hepatoprotective effects indicate that it is not hepatotoxic; rather, it protects the liver from injury. However, comprehensive toxicological studies, including acute and chronic toxicity, genotoxicity, and reproductive toxicity assessments, are not extensively documented in publicly available sources. As with all herbal extracts, the safety profile may vary depending on the source, extraction method, and purity of the extract. Research-grade Gynostemma Extract is intended for laboratory use only.

Molecules.2013 Apr 12;18(4):4342-56;Phytomedicine.2012 Jun 15;19(8-9):812-8.

Reports have indicated that Panax notoginseng and ginseng contain notoginsenoside Fd, and relevant data is available for reference.
Gynostemma Extract (Ginsenoside C-Mx1) is a natural saponins extract derived from Gynostemma pentaphyllum. It has the molecular formula C47H80O17 and CAS number 80321-63-7. The extract is an orally active antioxidant agent that increases SOD and glutathione peroxidase activity and expression. It reduces stress-induced c-fos expression and shows anxiolytic and antidiabetic effects in vivo. In liver injury models, it reduces SGOT and SGPT elevations. Gynostemma Extract is not approved as a drug and is primarily used as a research compound and dietary supplement. Its molecular weight is 917.13 g/mol.

C48H82O18

917.13

916.54

80321-63-7

15574810

White to off-white solid powder

1.36

183 - 185 °C

0.612

11

17

12

64

1630

0

ZTQSADJAYQOCDD-UHFFFAOYSA-N

InChI=1S/C47H80O17/c1-22(2)10-9-14-47(8,64-42-39(58)36(55)34(53)27(62-42)21-60-40-37(56)32(51)25(50)20-59-40)23-11-16-46(7)31(23)24(49)18-29-44(5)15-13-30(43(3,4)28(44)12-17-45(29,46)6)63-41-38(57)35(54)33(52)26(19-48)61-41/h10,23-42,48-58H,9,11-21H2,1-8H3

2-(hydroxymethyl)-6-[[12-hydroxy-4,4,8,10,14-pentamethyl-17-[6-methyl-2-[3,4,5-trihydroxy-6-[(3,4,5-trihydroxyoxan-2-yl)oxymethyl]oxan-2-yl]oxyhept-5-en-2-yl]-2,3,5,6,7,9,11,12,13,15,16,17-dodecahydro-1H-cyclopenta[a]phenanthren-3-yl]oxy]oxane-3,4,5-triol

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Solubility in Formulation 1: 2.5 mg/mL (2.73 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

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Solubility in Formulation 2: ≥ 2.5 mg/mL (2.73 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

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Solubility in Formulation 3: ≥ 2.5 mg/mL (2.73 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.

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 (Please use freshly prepared in vivo formulations for optimal results.)