Search Results (25)

This study evaluates the antimicrobial activity of the glycolic extract of G. sylvestre against anaerobic pathogens, along with its cytotoxicity, genotoxicity, anti-inflammatory activity, antioxidant effects, and phytochemical composition. Phytochemical analysis was conducted using high-performance liquid chromatography and liquid chromatography–mass spectrometry, while the antioxidant effect was assessed through a DPPH assay. Antimicrobial action was tested on planktonic cultures and biofilms of Porphyromonas gingivalis, Porphyromonas endodontalis, Parvimonas micra, and Fusobacterium nucleatum. Cytotoxicity was evaluated using mouse macrophages (RAW 264.7), rat fibroblasts (L929), and human keratinocytes (HaCaT). Anti-inflammatory effects were measured by an immunoenzymatic assay (ELISA) on RAW 264.7 cells. Statistical analysis was performed using a one-way ANOVA and Tukey’s test. Phytochemical analysis revealed the presence of phenolic compounds and flavonoids. The extract demonstrated a reduction of over 95% in biofilms of P. gingivalis, P. micra, and F. nucleatum within 5 min of treatment. Cell viability (HaCaT) remained above 80%. Antioxidant activity showed an EC50 of 353.43 µg/mL, achieving a 50% reduction in free radicals. A significant decrease in TNF-α (a pro-inflammatory cytokine) and an increase in IL-10 (an anti-inflammatory cytokine) were observed. In conclusion, the extract of G. sylvestre exhibits promising potential as a therapeutic agent for treating anaerobic infections, inflammation, and oxidative stress. Full article

A study on 81 individuals (18–75 years old) with mildly impaired fasting blood glucose (FBG) concentrations (98–125 mg/dL) was undertaken to investigate the tolerability of a food supplement (FS) based on Zea mays and Gymnema sylvestre extracts, zinc, and chromium and its efficacy on glucose and lipid metabolism. The subjects were randomized into three groups (27 in each group) and supplemented with one or two tablet(s)/day of FS (groups 1 and 2, respectively), or two tablets/day of placebo (group 3). Blood sampling was carried out at baseline (t0) and after a 3-month treatment (t1), and biochemical parameters associated with glucose and lipid metabolism and kidney and liver toxicity were evaluated. Compared to the placebo, FBG and glycated haemoglobin (HbA1c) were significantly (p < 0.001) reduced in group 1 subjects. In contrast, at the doses of one and two tablet(s)/day, the FS exerted no effect on the other parameters examined. We conclude that in subjects with slightly impaired FBG, ingestion of a FS based on Z. mays and G. sylvestre extracts, zinc, and chromium over 3 months lowers FBG and modulates glucose homeostasis by improving glucose metabolism. These beneficial effects occur in the absence of biochemical evidence of kidney and liver toxicity. Full article

Gymnema sylvestre (GS) and berberine (BBR) are natural products that have demonstrated therapeutic potential for the management of obesity and its comorbidities, as effective and safe alternatives to synthetic drugs. Although their anti-obesogenic and antidiabetic properties have been widely studied, comparative research on their impact on the gene expression of adipokines, such as resistin (Res), omentin (Ome), visfatin (Vis) and apelin (Ap), has not been reported. Methodology: We performed a comparative study in 50 adult Mexican patients with obesity treated with GS or BBR for 3 months. The baseline and final biochemical parameters, body composition, blood pressure, gene expression of Res, Ome, Vis, and Ap, and safety parameters were evaluated. Results: BBR significantly decreased (p < 0.05) body weight, blood pressure and Vis and Ap gene expression and increased Ome, while GS decreased fasting glucose and Res gene expression (p < 0.05). A comparative analysis of the final measurements revealed a lower gene expression of Ap and Vis (p < 0.05) in patients treated with BBR than in those treated with GS. The most frequent adverse effects in both groups were gastrointestinal symptoms, which attenuated during the first month of treatment. Conclusion: In patients with obesity, BBR has a better effect on body composition, blood pressure, and the gene expression of adipokines related to metabolic risk, while GS has a better effect on fasting glucose and adipokines related to insulin resistance, with minimal side effects. Full article

The main objective of this research was to perform Gymnema sylvestre (Asclepiadaceae) extract’s phytochemical screening and identify its therapeutic potential. Using a Soxhlet apparatus, the powdered plant material was extracted using ethyl acetate. The preliminary phytochemical analysis confirmed the presence of alkaloids, flavonoids, phenols, glycosides, and steroids. Gas chromatography–mass spectroscopy analysis of the extract was performed and confirmed the presence of 11 compounds. As per the quantitative analysis, the extract exhibited a phenolic content of 948 µg gallic acid equivalent/g dry weight, a total flavonoid content of 398 µg quercetin equivalent/g dry weight, and an alkaloid content of 487 µg atropine equivalent/g dry weight. As per the in vitro cytotoxicity test using A549 cells, the IC₅₀ (half-maximal inhibitory concentration) value for the extract was found to be 76.06 ± 1.26 µg/mL, indicating its cytotoxic effect on the cells. The ethyl acetate extract showed significant antibacterial efficacy, as evidenced by a zone of clearance measuring 3 mm against Escherichia coli and 6 mm against Bacillus subtilis. For anthelmintic activity, the earthworm paralysis time induced by G. sylvestre extract (10 mg/mL) was 28.13 ± 0.8 min, and the time of death was 68.21 ± 1.72 min. In comparison, the reference drug, piperazine citrate (10 mg/mL), caused paralysis in 22.18 ± 1.02 min and resulted in death at 66.22 ± 2.35 min. Similarly, the coagulation time was notably prolonged, with blood clot formation observed at 1 min and 40 s, at a concentration of 1 mg/mL, which underscores the potential anticoagulant or hemostatic modulation properties of G. sylvestre extract. The test extract showed good inhibition of alpha-amylase activity and exhibited an IC₅₀ value of 15.59 µg/mL. The IC₅₀ value for DPPH (2,2-diphenyl-1-picrylhydrazyl)-scavenging activity for the extract was 19.19 µg/mL. Based on the GCMS results, the compound 2,7-dimethyl-undecane was selected for its anticancer potential. Docking studies were conducted with the epidermal growth factor receptor (EGFR) protein, specifically the 5WB7 variant associated with lung cancer. The docking score was −4.5, indicating a potential interaction. Key interaction residues such as ASN328, VAL350, and THR358 were identified. Overall, this research provides valuable insights into the phytochemical composition and diverse biological activities of G. sylvestre extract, offering a foundation for further exploration of its medicinal and pharmacological potential. Full article

Background: Folk medicines are attractive therapeutic agents for treating type 2 diabetes mellitus (T2DM). Most plant extracts that have been suggested to restore β-cells function were tested in vivo. Some only have been tested in vitro to determine whether they have a direct effect on β-cells islets of Langerhans. Currently, there are no defined criteria for screening of β-cell-directed plant-based remedies as potential antidiabetic agents. Summary: In this review, we have identified certain criteria/characteristics that can be used to generate a “screening portfolio” to identify plant extracts as potential β-cell-directed agents for the treatment of T2DM. To validate our screening method, we studied the potential therapeutic efficacy of a Gymnema sylvestre (GS) extract using the screening criteria detailed in the review. Six criteria have been identified and validated using OSA^®, a GS extract. By using this screening method, we show that OSA^® fulfilled most of the criteria identified for an effective β-cell-directed antidiabetic therapy, being an effective insulin-releasing agent at nontoxic concentrations; maintaining β-cell insulin content by stimulating a concomitant increase in insulin gene transcription; maintaining β-cell mass by protecting against apoptosis; and being effective at maintaining normoglycemia in vivo in a mouse model and a human cohort with T2DM. Key messages: The present review has highlighted the importance of having a screening portfolio for plant extracts that have potential antidiabetic effects in the treatment of T2DM. We propose that this screening method should be adopted for future studies to identify new β-cell-directed antidiabetic plant derived agents. Full article

Type 2 diabetes mellitus (T2DM) is characterized by high blood glucose levels and lipid alterations. Besides pharmacological treatment, lifestyle modifications and nutraceuticals can be used to manage glucose and lipid profiles, which is crucial for preventing, or avoiding, serious consequences associated with the condition. This randomized controlled clinical trial on 75 patients with T2DM evaluated the effects of a combination of myo-inositol and d-chiro-inositol (40:1), α-lactalbumin, Gymnema sylvestre, and zinc on glucose and lipid profile. The intention-to-treat analysis displayed no significant differences in glucose parameters between the groups; however, the study group displayed reduced levels of total cholesterol (p = 0.01) and LDL (p = 0.03) after 3 months of supplementation. A subgroup analysis involving patients who did not modify their antidiabetic therapy, after 6 months displayed improved levels of total cholesterol (p = 0.03) and LDL (p = 0.04) in the study group versus placebo, along with a greater body weight reduction (p = 0.03) after 3 months. Furthermore, within the study group, levels of HDL (p = 0.03) and triglycerides (p = 0.04) improved after 3 months. These findings support supplementation with myo-inositol and d-chiro-inositol (40:1), α-lactalbumin, Gymnema sylvestre, and zinc as an adjuvant and safe strategy to manage the lipid profiles of patients with T2DM. Full article

The primary control of dysmetabolic patients is extremely challenging worldwide, with inadequate dietary habits and sporadic physical activity among the key risk factors for metabolic syndrome onset. Nowadays, there is no exclusive treatment for this condition, and considering that preventive measures usually fail, new therapeutic approaches need to be proposed and investigated. This present pilot study compared the effects of diet alone and in association with a combination of myo-inositol and d-chiro-inositol in their 40:1 ratio, α-lactalbumin, and Gymnema sylvestre on different metabolic parameters in obese dysmetabolic patients. To this purpose, 37 patients with BMI between 30 and 40 and fasting blood glucose between 100 and 125 mg/dL were divided into two groups: (i) the control group followed a hypocaloric Mediterranean diet, (ii) while the study group was also supplemented with a daily dosage of two sachets, each one containing 1950 mg myo-inositol, 50 mg d-chiro-inositol, 50 mg α-lactalbumin, and 250 mg Gymnema Sylvestre. After a 6-month treatment, all parameters improved in both groups. Nevertheless, the treated group experienced a greater improvement, especially concerning the variation from the baseline of HOMA index, triglycerides, BMI, body weight, and waist circumference. These findings support the supplementation with myo-inositol and d-chiro-inositol in the 40:1 ratio, α-lactalbumin, and Gymnema sylvestre as a therapeutical strategy to potentiate the beneficial effects induced via dietary programs in dysmetabolic patients. Full article

Gymnema sylvestre is traditionally used as an herbal remedy for diabetes. The effect of Gymnema sylvestre supplementation on beta cell and hepatic activity was explored in an alloxan-induced hyperglycemic adult rat. Animals were made hyperglycemic via a single inj. (i.p) of Alloxan. Gymnema sylvestre was supplemented in diet @250 mg/kg and 500 mg/kg b.w. Animals were sacrificed, and blood and tissues (pancreas and liver) were collected for biochemical, expression, and histological analysis. Gymnema sylvestre significantly reduced blood glucose levels with a subsequent increase in plasma insulin levels in a dosage-dependent manner. Total oxidant status (TOS), malondialdehyde, LDL, VLDL, ALT, AST, triglyceride, total cholesterol, and total protein levels were reduced significantly. Significantly raised paraoxonase, arylesterase, albumin, and HDL levels were also observed in Gymnema sylvestre treated hyperglycemic rats. Increased mRNA expression of Ins-1, Ins-2, Gck, Pdx1, Mafa, and Pax6 was observed, while decreased expression of Cat, Sod1, Nrf2, and NF-kB was observed in the pancreas. However, increased mRNA expression of Gck, Irs1, SREBP1c, and Foxk1 and decreased expression of Irs2, ChREBP, Foxo1, and FoxA2 were observed in the liver. The current study indicates the potent effect of Gymnema sylvestre on the transcription modulation of the insulin gene in the alloxan-induced hyperglycemic rat model. Enhanced plasma insulin levels further help to improve hyperglycemia-induced dyslipidemia through transcriptional modulation of hepatocytes. Full article

The leaf extracts of Gymnema sylvestre consist of secondary metabolites which are well known for antioxidant activity. This study aimed to measure the drying characteristics of G. sylvestre leaves under far-infrared radiation (FIR) and to optimize the specific energy consumption for drying and antioxidant activity of ethanol-water extract of dried leaves. Fresh leaves were harvested and exposed to combinations of four different temperatures (125, 150, 175 and 200 °C) and exposure times (5, 10, 15 and 20 min). Drying kinetics, energy consumption, color changes, total phenolic content (TPC) and antioxidant activities were quantified. Both temperature and drying time have significant (p < 0.05) effects on drying characteristics and antioxidant activity. The equilibrium moisture content was achieved at 200 °C and 18 min. The specific energy decreased and total color changes increased with temperature. Under lower temperatures (125 and 150 °C), TPC and antioxidant activity increased with exposure time, whereas higher exposure time (20 min) with high temperatures (175 and 200 °C) significantly decreased TPC and antioxidant activity. The highest TPC of 30.5 mg TAE/g leaf-fresh weight was achieved at 200 °C and 15 min. The optimal drying conditions achieved from the dissimilarity function method were 200 °C and 8.4 min. Full article

The invention of an easy synthetic approach for extremely impactful nanomaterials (NMs) is one of the crucial research areas in modern science and engineering. In the present work, we describe a cost-effective, simple, rapid and environmentally gracious biogenic fabrication of nickel/nickel oxide nanoparticles (Ni/NiO NPs) using Gymnema sylvestre as a natural fuel. The textural characteristics of as-prepared Ni/NiO NPs were explored using X-ray diffraction (XRD), Fourier transform infrared spectroscopy (FTIR), diffuse reflectance spectra (DRS), photoluminescence spectroscopy (PL), field-emission scanning electron microscope (FESEM), energy dispersive X-ray analysis (EDX), and high-resolution transmission electron microscopy (HRTEM). XRD affirmed the crystalline nature and phase formation of Ni/NiO NPs. The FTIR spectrum ascertains the formation of Ni/NiO NPs, and the band gap of 4.29 eV is revealed from DRS studies. Ni/NiO NPs display an intense emission peak at 576.2 nm in their PL spectrum. The fabrication of pseudo-spherical Ni/NiO NPs was displayed by FESEM and HRTEM images. The particle size obtained from HRTEM was 21 nm, which resembles the median crystallite size ascertained from the XRD data. Additionally, the plausible mechanism for Ni/NiO NPs formation is illustrated. Moreover, as-synthesized Ni/NiO NPs displayed considerable antifungal potential against Candida albicans and Aspergillus niger. Results revealed that the Gymnema sylvestre leaves extract can synthesize Ni/NiO NPs with appealing biological effectiveness for application in the nanomedicine sector. Full article

Gymnema sylvestre (GS) is a perennial woody vine native to tropical Asia, China, the Arabian Peninsula, Africa and Australia. GS has been used as a medicinal plant with potential anti-microbial, anti-inflammatory and anti-oxidant properties. This study was conceptualized to evaluate the cytotoxicity potential of Gymnema sylvestre saponin rich fraction (GSSRF) on breast cancer cell lines (MCF-7 and MDA-MB-468) by SRB assay. The anti-tumor activity of GSSRF was assessed in tumor-bearing Elrich ascites carcinoma (EAC) and Dalton’s lymphoma ascites (DLA) mouse models. The anti-oxidant potential of GSSRF was assessed by DPPH radical scavenging assay. The acute toxicity of GSSRF was carried out according to OECD guideline 425. The yield of GSSRF was around 1.4% and the presence of saponin content in GSSRF was confirmed by qualitative and Fourier transform infrared spectroscopic (FTIR) analysis. The in vitro cytotoxic effects of GSSRF on breast cancer cell lines were promising and found to be dose-dependent. An acute toxicity study of GSSRF was found to be safe at 2000 mg/kg body weight. GSSRF treatment has shown a significant increase in the body weight and the life span of EAC-bearing mice in a dose-dependent manner when compared with the control group. In the solid tumor model, the doses of 100 and 200 mg/kg body weight per day have shown about 46.70% and 60.80% reduction in tumor weight and controlled the tumor weight until the 30th day when compared with the control group. The activity of GSSRF in both models was similar to the cisplatin, a standard anticancer agent used in the study. Together, these results open the door for detailed investigations of anti-tumor potentials of GSSRF in specific tumor models, mechanistic studies and clinical trials leading to promising novel therapeutics for cancer therapy. Full article

Gymnemic-acids (GA) block lingual sweet taste receptors, thereby reducing pleasantness and intake of sweet food. Objective: To examine whether a 14-day gymnema-based intervention can reduce sweet foods and discretionary sugar intake in free-living adults. Healthy adults (n = 58) were randomly allocated to either the intervention group (INT) or control group (CON). The intervention comprised of consuming 4 mg of Gymnema sylvestre containing 75% gymnema acids, a fibre and vitamin supplement, and an associated healthy-eating guide for 14 days; participants in the CON group followed the same protocol, replacing the GA with a placebo mint. Amount of chocolate bars eaten and sensory testing were conducted before and after the 14-day intervention (post-GA or placebo dosing on days zero and 15, respectively). Food frequency questionnaires were conducted on days zero, 15 and after a 28-day maintenance period to examine any changes in intake of sweet foods. A range of statistical procedures were used to analyse the data including Chi square, t-test and two-way analysis of variance. Post dosing, INT consumed fewer chocolates (2.65 ± 0.21 bars) at day zero than CON (3.15 ± 0.24 bars; p = 0.02); there were no differences between groups at day 15 (INT = 2.77 ± 0.22 bars; CON = 2.78 ± 0.22 bars; p = 0.81). At both visits, a small substantive effect (r < 0.3) was observed in the change in pleasantness and desire ratings, with INT showing a slight increase while CON showed a small decrease over the 14-day period. No differences were found in the intake of 9 food categories between groups at any timepoint. There were no differences in consumption of low sugar healthy foods between visits, or by group. The 14-day behavioural intervention reduced pleasantness and intake of chocolate in a laboratory setting. There was no habituation to the mint over the 14-day period. This study is the first to investigate the effect of longer-term gymnema acid consumption on sweet food consumption outside of a laboratory setting; further research is needed to assess how long the effect of the 14-day intervention persists. Full article

Diabetes represents a major health problem, involving a severe imbalance of blood sugar levels, which can disturb the nerves, eyes, kidneys, and other organs. Diabes management involves several synthetic drugs focused on improving insulin sensitivity, increasing insulin production, and decreasing blood glucose levels, but with unclear molecular mechanisms and severe side effects. Natural chemicals extracted from several plants such as Gymnema sylvestre, Momordica charantia or Ophiopogon planiscapus Niger have aroused great interest for their anti-diabetes activity, but also their hypolipidemic and anti-obesity activity. Here, we focused on the anti-diabetic activity of a few natural and synthetic compounds, in correlation with their pharmacokinetic/pharmacodynamic profiles, especially with their blood-brain barrier (BBB) permeability. We reviewed studies that used bioinformatics methods such as predicted BBB, molecular docking, molecular dynamics and quantitative structure-activity relationship (QSAR) to elucidate the proper action mechanisms of antidiabetic compounds. Currently, it is evident that BBB damage plays a significant role in diabetes disorders, but the molecular mechanisms are not clear. Here, we presented the efficacy of natural (gymnemic acids, quercetin, resveratrol) and synthetic (TAK-242, propofol, or APX3330) compounds in reducing diabetes symptoms and improving BBB dysfunctions. Bioinformatics tools can be helpful in the quest for chemical compounds with effective anti-diabetic activity that can enhance the druggability of molecular targets and provide a deeper understanding of diabetes mechanisms. Full article

Gymnema sylvestre (Retz.) Schult is a multi-purpose traditional medicine that has long been used for the treatment of various diseases. To discover the potential bioactive composition of G. sylvestre, a chemical investigation was thus performed. In this research, four new C₂₁ steroidal glycosides sylvepregosides A-D (1–4) were isolated along with four known compounds, gymnepregoside H (5), deacetylkidjoladinin (6), gymnepregoside G (7) and gymnepregoside I (8), from the ethyl acetate fraction of G. sylvestre. The structures of the new compounds were established by extensive 1D and 2D nuclear magnetic resonance (NMR) spectra with mass spectroscopy data. Compounds 1–6 promoted glucose uptake by the range of 1.10- to 2.37-fold, respectively. Compound 1 showed the most potent glucose uptake, with 1.37-fold enhancement. Further study showed that compounds 1 and 5 could promote GLUT-4 fusion with the plasma membrane in L6 cells. The result attained in this study indicated that the separation and characterization of these compounds play an important role in the research and development of new anti-diabetic drugs and pharmaceutical industry. Full article