OBJECTIVETo study the antidiabetic activity of Gynura procumbens (G. procumbens) used in the traditional management of diabetes in Southern Asia.

METHODSG. procumbens leaves were extracted sequentially with graded percentage of ethanol in water (95%, 75%, 50%, 25% and 0%), and the extracts were tested for antidiabetic activity using acute (7 h), subcutaneous glucose tolerance test and sub-chronic (14 d) test in non-diabetic and streptozotocin-induced diabetic rats. The extracts were further subjected to phytochemical studies.

RESULTSIn acute dose (1 g/kg), the extracts significantly lowered fasting blood glucose (FBG) in streptozotocin-induced diabetic rats (P<0.05). However, the FBG-lowering effect of the 25% extract compared to the other extracts, was rapid (47% after 2 h) and the highest: 53%, 53% and 60% in the 3rd, 5th, and 7th h, respectively (P<0.05), comparable only to the effect of metformin. Furthermore, the extracts suppressed peak FBG in subcutaneous glucose tolerance test, but only the 0% and 25% extracts, and metformin sustained the decrease until the 90th min (P<0.05). Moreover, in the 14 days study, the 25% extract exerted the highest FBG-lowering effect, namely 49.38% and 65.43% on days 7 and 14, respectively (P<0.05), similar to the effect of metformin (46.26% and 65.42%). Total flavanoid and phenolic contents in the extracts were found to decrease with increase in polarity of extraction solvents. The composition of reference compounds (chlorogenic acid, rutin, astragalin and kaempferol-3-O-rutinoside) followed a similar trend.

CONCLUSIONSG. procumbens contains antidiabetic principles, most extracted in 25% ethanol. Interaction among active components appears to determine the antidiabetic efficacy, achieved likely by a metformin-like mechanism.

Animals ; Asteraceae ; chemistry ; Blood Glucose ; drug effects ; Body Weight ; drug effects ; Diabetes Mellitus, Experimental ; chemically induced ; drug therapy ; Flavonoids ; chemistry ; Glucose Tolerance Test ; Hypoglycemic Agents ; administration & dosage ; chemistry ; pharmacology ; Metformin ; administration & dosage ; pharmacology ; Phenols ; chemistry ; Phytochemicals ; chemistry ; Plant Extracts ; administration & dosage ; chemistry ; pharmacology ; Plant Leaves ; chemistry ; Rats

Aims: Hepatotoxicity is a serious health risk and treatment options are inadequate. Polygonum minus Huds. (Family: Polygonaceae) is an antioxidant rich, commonly available plant in Malaysia and used in the Malay folk medicine. The leaves are also considered as one of the salad plants and flavouring agent for food delicacies. The present study evaluates the hepatoprotective activity of methanol extract of P. minus leaves on carbon tetrachloride (CCl4) and paracetamol-induced hepatotoxicity in Sprague Dawley rats. Methodology and results: Methanol extract of P. minus (MEPM) was prepared by maceration method. The standard drug and MEPM treated groups of rats were administered with silymarin (50 mg/kg) or MEPM (200 mg/kg or 400 mg/kg), respectively for 14 days in both experimental models. All the animals in the CCl4-induced model were administered CCl4 and paracetamol in the other model except to respective normal control group to induce liver toxicity. Estimation of body weight and liver weight, biochemical parameters including total protein, aspartate aminotransferase, alanine aminotransferase, alkaline phosphatase and total bilirubin levels and histopathological studies were conducted. The MEPM was found to have significant hepatoprotective activity in rats with CCl4 and paracetamol-induced liver damage as noted from the analysis of body weight, serum marker enzyme activity and histopathology. Conclusion, significance and impact study: The MEPM possesses significant hepatoprotective activity while the activity is increased with dose in both experimental models. Inclusion of P. minus leaves in the food may be recommended as it may help to counteract different types of chemical-induced liver damage.

The present study was undertaken to investigate the isolated compounds from the stem bark of Garcinia atroviridis as potential cholinesterase inhibitors and the ligand-enzyme interactions of selected bioactive compounds in silico. The in vitro cholinesterase results showed that quercetin (3) was the most active AChE inhibitor (12.65 ± 1.57 µg/ml) while garcinexanthone G (6) was the most active BChE inhibitor (18.86 ± 2.41 µg/ml). It is noteworthy to note that compound 6 was a selective inhibitor with the selectivity index of 11.82. Molecular insight from docking interaction further substantiate that orientation of compound 6 in the catalytic site which enhanced its binding affinity as compared to other xanthones. The nature of protein-ligand interactions of compound 6 is mainly hydrogen bonding, and the hydroxyl group of compound 6 at C-10 is vital in BChE inhibition activity. Therefore, compound 6 is a notable lead for further drug design and development of BChE selective inhibitor.
Butyrylcholinesterase ; Catalytic Domain ; Cholinesterase Inhibitors ; Cholinesterases ; Computer Simulation ; Drug Design ; Garcinia ; Hydrogen Bonding ; In Vitro Techniques ; Quercetin ; Xanthones

Objective To investigate the antidiabetic activity of Ocimum tenuiflorum L. (O. tenuiflorum) leaves used in the traditional medicine management of diabetes in Malaysia. Methods O. tenuiflorum leaves were extracted sequentially with hexane, chloroform, ethyl acetate, methanol, and water. The extracts were evaluated in terms of antidiabetic activity by using acute, subcutaneous glucose tolerance, and sub-chronic tests in streptozotocin-induced diabetic rats. The extracts were also subjected to phytochemical analyses. Results With an acute dose (1 g/kg), the methanol extracts showed significant reduction (31%) in fasting blood glucose (FBG) of the streptozotocin-induced diabetic rats. The FBG-decreasing effect of ethyl acetate extract was more rapid than that of the other extracts; the decreasing rates were 20% after 2 h, 21% after 3 h, and 8% after 5 and 7 h. After 7 h (31%), the effect of methanol extract on FBG was significantly lower than that of metformin. In the subcutaneous glucose tolerance test, only methanol and hexane extracts showed the similarity of metformin in diabetic rats. After 14 days, the effects of these extracts were similar to those of metformin (63.33%). The total flavonoid and phenolic contents of extracts decreased as the polarity of the extraction solvent increased. Conclusions The results obtained provide support for a possible use of O. tenuiflorum leaves in managing hyperglycemia and preventing the complications associated with it in type 2 diabetic.

Introduction: Kratom or (Mitragyna speciosa) leaves are consumed as a folk remedy and opioid substitute in the Southeast Asian region. There is still a lack of information about the long-term or toxic-causing effects of kratom use. Methods: A total of thirteen regular kratom users, with long-term (>20 twenty years) kratom use history were recruited for this cross-sectional pilot study. Respondents were required to undergo a blood-test and laboratory anaysis was conducted to determine the mitragynine content in an acquired street sample of kratom. Results: The regular, longterm consumption of brewed kratom decoction did not cause any significant alterations in haematological, kidney, liver, thyroid, inflammatory and gastrointestinal analytes in a cohort of kratom users who had no history of substance misuse. However, those who had a higher intake (>3 glasses per day) of kratom exhibited higher lipid values (except for HDL-cholesterol), and a moderate elevation of homocysteine level. Conclusion: Long-term (>20 years with a daily intake of ≥87.54mg of mitragynine) kratom consumption was not associated with altered biochemical levels, although prolonged and heavy use (>3 glasses daily) may result in cardiovascular risks. The latter finding, however, requires further investigation.