Swertiamarin and quercetin combination ameliorates hyperglycemia, hyperlipidemia and oxidative stress in streptozotocin-induced type 2 diabetes mellitus in wistar rats.

ETHNOPHARMACOLOGICAL RELEVANCE: Swertiamarin (Sw) and quercetin (Qu) have been isolated from different plants and are reported for their antidiabetic activities. The plants from which swertiamarin and quercetin were isolated are also traditionally used in the treatment of diabetes mellitus. AIM OF THE STUDY: The present study is aimed to evaluate the synergistic effect of a combination of swertiamarin and quercetin (CSQ) on α-amylase in vitro and on streptozotocin (STZ) induced diabetes mellitus in vivo. METHODS: Swertiamarin was isolated from the plant Enicostemma axillare and quercetin was procured in its pure form. Sw, Qu and CSQ were evaluated for in vitro α-amylase inhibitory activity. Based on the in vitro study results, CSQ was assessed for in vivo streptozotocin induced diabetes mellitus in Wistar rats. The effect of CSQ on blood glucose levels, body weight, serum biochemical parameters and antioxidant enzymes such as glutathione (GSH), superoxide dismutase (SOD), catalase, glutathione peroxidase (GPx) and lipid peroxide levels were estimated. The histopathological observations of pancreatic tissues were also made. RESULTS: The purity of swertiamarin was confirmed by HPLC. The results showed that CSQ was found to possess high percentage of inhibition in an in vitro α-amylase inhibitory study. In a STZ-induced type 2 diabetes mellitus (T2DM), body weight of rats in CSQ treated and control groups were unaltered. A marked reduction in the blood glucose levels was observed in the CSQ treated groups on 14th and 28th day. Decrease in the levels of low-density lipoprotein (LDL), triglycerides, total cholesterol and an increase in high-density lipoprotein (HDL) cholesterol level was observed in a dose dependant in CSQ treated groups. However, CSQ treated groups could significantly improve antioxidant protection by increasing the levels of serum GSH, SOD, Catalase and GPx and decreasing the levels of lipid peroxide (p < 0.05). In the histopathological study, the pancreatic islets of Langerhans and vacuolization have shown significant increase in both the treated groups. CONCLUSIONS: The combination of swertiamarin and quercetin (CSQ) has proven a preventive and therapeutic effect against T2DM and suggests that this is a potential combination of phytoconstituents for excellent hypoglycemic activity in T2DM.

SYNTHESIS AND BIOLOGICAL EVALUATION OF NOVEL COUMARIN DERIVATIVES AS ANTIOXIDANT AGENTS.

Coumarins have been isolated from plants and reported for antioxidant properties. In the present study, we report synthesis of new coumarin derivatives as prospective therapeutic agents and investigate their antioxidant properties.

Nanotechnology: A Revolution in Cancer Diagnosis.

Nanotechnology has brought revolution in cancer detection and treatment. It has capability to detect even a single cancerous cell in vivo and deliver the highly toxic drugs to the cancerous cells. Nanoshells, carbon nanotubes, quantum dots, supermagnetic nanoparticles, nano wires, nanodiamonds, dandrimers, and recently synthesized nanosponges are some of the materials used for cancer detection. Using specific cross linkers, such as specific antibodies against cancer cells individual cancer cells can be located. With the aid of a novel set of lipid-coated, targeted quantum dots a method for quantifying multiple specific biomarkers on the surfaces of individual cancer cells was also developed. This approach to quantitative biomarker detection stands to improve the histopathology methods used to diagnosis pancreatic and other cancers and enable the development of methods to spot cancer cells circulating in the blood stream. Certain nano materials can also deliver cancer drugs at the site so the drug toxicity can also be reduced.

Antioxidant and hepatoprotective effect of swertiamarin from Enicostemma axillare against D-galactosamine induced acute liver damage in rats.

ETHNOPHARMACOLOGICAL RELEVANCE: The whole plant of Enicostemma axillare Raynal (Family: Gentianaceae) is used in variety of diseases in traditional Indian system of medicine including hepatic ailments. AIM OF THE STUDY: Swertiamarin isolated from Enicostemma axillare Raynal was evaluated for antioxidant and hepatoprotective activity. MATERIALS AND METHODS: Swertiamarin was isolated from successive ethyl acetate extract of the plant Enicostemma axillare belongs to the family Gentianaceae. The concentration of swertiamarin was determined by high performance thin layer chromatography (HPTLC). The hepatoprotective and antioxidant activity of swertiamarin (100 and 200mg/kg body weight) was carried out against d-Galactosamine (d-GalN) (200mg/kg body weight intraperitoneally i.p.) induced liver injury in rats. RESULTS: Swertiamarin a secoiridoid glycoside was found to contain a major constituent of the extract. d-GalN caused significant hepatotoxicity by alteration of several hepatic parameters. It also caused significant lipid peroxidation and reduced the levels of antioxidant defense mechanisms. The treatment with swertiamarin at 100 and 200mg/kg body weight when administered orally for 8 days prior to d-GalN caused a significant restoration of all the altered biochemical parameters due to d-GalN towards the normal, indicating the potent antioxidant and hepatoprotective nature of swertiamarin. CONCLUSIONS: Swertiamarin isolated from Enicostemma axillare possesses significant antioxidant and hepatoprotective properties against d-GalN induced hepatotoxicity given at 100 and 200mg/kg body weight orally for 8 days, which might be due to its in vitro antioxidant activity.

Antioxidant and hepatoprotective effect of the ethyl acetate extract of Enicostemma axillare (Lam). Raynal against CCL4-induced liver injury in rats.

Enicostemma axillare is used in Indian traditional medicine as a liver tonic. Its ethyl acetate extract has shown potent in vitro antioxidant activity and found to contain 7.26% of a bitter secoiridoid glycoside, swertiamarin. Hence, in the present study the ethyl acetate extract was screened for hepatoprotective and antioxidant properties against CCl4 induced hepatic injury in rats. The hepatoprotection was assessed in terms of reduction in histological damage and changes in serum enzymes and metabolites. The pretreatment with the extract at 100 and 200 mg/kg body weight doses given orally for eight days prior to CCl4 caused significant restoration of altered biochemical changes due to CCl4 towards the normal in serum, liver and kidney. The extract treatment at 200 mg/kg body weight was found to be more potent than the standard silymarin at 100 mg/kg body weight in reversing most of the biochemical parameters. Histopathological studies complemented the results of biochemical estimations in providing a proof of hepatoprotective and antioxidant actions of the extract. The study provides a support to the ethnomedical use of E. axillare in India.

Antinociceptive activity of swertiamarin isolated from Enicostemma axillare.

Many traditional Indian medicinal plants which contain large quantity of a secoiridoid, swertiamarin are being used to relieve pain. Iridoids present in a wide variety of medicinal plants possess a large number of medicinal properties. In the present study in vivo antinociceptive activity of swertiamarin isolated from E. axillare was carried out using three different methods in mice. In the hot plate method, a significant increase in the latency period was observed for the treatment with swertiamarin at 100 and 200 mg/kg bw after 30 and 45 min. The percent protection observed after 45 min was 109.42, 147.42 and 157.14, respectively, for the standard paracetamol and swertiamarin at 100 and 200 mg/kg bw treatments. A significant increase in the tail withdrawal reflex was observed for the swertiamarin treatment at both the doses with percent protections of 150 and 200, respectively. In both these methods, swertiamarin produced potent activity than that of standard paracetamol. In the acetic acid induced writhing, swertiamarin at 100 and 200 mg/kg bw reduced the number of writhes significantly. Dose dependent results were observed in all the three methods and among the two doses, swertiamarin at 200 mg/kg bw showed potent activity. These results prove that swertiamarin possess both peripheral and central antinociceptive activity.