In vitro and computational studies on the antiglycation activity of compounds isolated from antidiabetic Tetracera alnifolia stem bark.

The continuous search for new compounds in natural-based plants is a promising strategy for the prevention of diseases. This work examined antiglycation activity compounds isolated from the antidiabetic extract of T. alnifolia stem bark via in vitro and computational [molecular dynamics (MD)] approach. Phytochemical investigation of ethyl acetate fraction and the application of spectroscopic methods led to the isolation and elucidation of 3 compounds: quercetin (1), kaempferol (2), and gallic acid (3). Compounds 1, 2 and 3 were then screened for antioxidant and antiglycation activities. Results show that the ethanol extract of T. alnifolia demonstrated good antioxidant activity compared to the standard gallic acid. There was a significant reduction in fasting blood glucose level progressively in diabetic rats, for 21 days compared to diabetic control. Consequently, the antiglycation activity of ethyl acetate fraction had the highest antiglycation activities, followed by dichloromethane (DCM) fraction. Compounds isolated from ethyl acetate fraction, exhibited the highest antiglycation effect for kaempferol followed by quercetin, while gallic acid had the least antiglycation effect. The root mean square of deviation (RMSD) and MM/GBSA energies obtained from molecular dynamics agree with the in vitro antiglycation activity with the sequence of structural stability in the order; kaempferol > quercetin > gallic acid. Therefore, findings from these results suggest that compounds isolated from T. alnifolia possess antiglycation activity.Communicated by Ramaswamy H. Sarma.

Isolation, characterization, and hepatoprotective properties of betulinic acid and ricinine from Tetracarpidium conophorum seeds (Euphorbiaceae).

The present study is to isolate and characterize betulinic acid and ricinine from T. conophorum seeds. Phytochemical investigation on hexane fraction of T. conophorum seeds led to the isolation of two compounds, Betulinic acid (1), and Ricinine (2). Betulinic acid and ricinine were screened against HepG2 cells and tested in vivo in CCl4 -induced experimental rats model. Results from this study showed that the compounds had hepatoprotective and cytotoxic activities. It was observed that betulinic acid inhibited HepG2 cell with percentage inhibition of 54% compared with standard doxorubicin (64%), while ricinine was inactive against HepG2 cell lines. Furthermore, molecular docking was carried out on betulinic acids and ricinine, with binding energies of -11.2 kcal/mol and -5.4 kcal/mol, respectively, indicating strong binding sites and interactions with Hepatitis B Virus DNA polymerase. Therefore, findings from this study suggest that betulinic acid possess cytotoxic and hepatoprotective properties, while ricinine exhibited hepatoprotection in CCl4 -induced liver damage. PRACTICAL APPLICATIONS: Medicinal plants contain unrestricted ability to make compounds that intrigue researchers in the quest for novel phyto-therapeutic drugs. The continuous exploration of new compounds in the medicinal plant is an auspicious strategy for the prevention of diseases. Therefore, the purpose of this research is to evaluate the cytotoxic and hepatoprotective compounds (betulinic acid and ricinine) isolated from T. conophorum seeds.

Phytochemical screening and acute toxicity evaluation of Telfairia occidentalis aqueous extracts on rats.

The phytochemical composition and acute toxicity of Telfairia occidentalis aqueous extracts were investigated in this study. Phytochemical screening was carried out on the pulverized leaf, root, pod and stem samples. Proximate analysis was also conducted for the root to ascertain the effect of drying procedures on its composition. Fifty-six (56) Wister albino rats, male and female were divided into two broad groups of 28 animals per group. The first group was randomly separated into seven (7) groups of four (4) animals per group. The control group received distilled water alone while the other groups received varied doses (1500mg/kg, 2250mg/kg and 3000mg/kg) of the Soluble and Insoluble Tefairia occidentalis root fraction. The second group of 28 animals was also distributed into 7 groups of 4 animals per group. Six test groups received varied doses (1500mg/kg, 2250mg/kg and 3000mg/kg) of Telfairia occidentalis fruit and stem extracts. The animals were observed for the first 12hr for any toxic symptoms and for 48 hr for mortality rate. Surviving animals were sacrificed after 48 hours. Phytochemical screening results reveal the presence of tannins, flavonoid, steroid, terpenoids, saponin, alkaloid, glycosides, proteins and carbohydrates. Flavonoid and saponin was not detected in stem sample; alkaloid is present in all samples except pod; and cyanogenic glycoside was found in both root and pod samples. Except for the fibre content, the method of preparation of the root had no significant effect on the proximate composition of the sample. The root extracts cause insignificant reduction in Alanine aminotransferase (ALT) and Aspartate aminotransferase (AST) activities, except for the significant reduction in ALT activity at highest dose. The pod extract significantly increased the ALT and AST activities, which is dose dependent, while the stem extract only caused increased activity of ALT, but not AST. None of the extracts administered had any significant effect on the levels of serum creatinine and urea. Thus, while the root extract may exhibit some hepatoprotective effect (or nephrotoxic due to cyanogenic glycoside) and its proximate composition, not affected by heat treatment, the pod and stem extracts of Telfairia occidentalis may have some effects on rat hepatocytes.

Differential Effects of Continuous and Interval Exercise Training on the Atherogenic Index of Plasma in the Non-Obese Young Male.

BACKGROUND: The process of atherogenicity is known to be influenced by exercise. However, appropriate exercise stimulus necessary to generate the response and adaptation in sedentary non-obese individuals has not yet been investigated. The purpose of the present study was to compare the effects of an 8-week continuous training and corresponding interval training on the atherogenic index of plasma in sedentary Nigerian males. METHODS: Overall, there were 54 male university students that participated in our study, which used a pretest- posttest control group design. Participants (18 males per group) were assigned into continuous, interval and control groups respectively. During the first two weeks, training was done 3 times weekly for 30 minutes each day, and was increased by 5 minutes every 2 weeks. Continuous training was done at 70-84% of heart rate reserve. Interval training was done at 70-84%/30-39% heart rate reserve in 1:2 minutes work/rest intervals, respectively. The control group did not participate in the training. Data collected were analysed using descriptive, paired t-test, analysis of covariance and Bonferroni post-hoc analysis. RESULTS: Young sedentary non-obese males were at high risk (atherogenic index of plasma > 0.24) of cardiovascular diseases/conditions. However, continuous training led to significant reductions (p = 0.002) in the atherogenic index of plasma. In contrast, non-significant increase (p = 0.084) followed interval training. After controlling for baseline values, only continuous training still had significant effects on atherogenic index of plasma when compared with other groups. CONCLUSIONS: Continuous training of vigorous intensity is better than a corresponding interval training protocol as a natural anti-atherogenic method of reducing risk of cardiovascular event in sedentary non-obese males. KEY WORDS: Atherogenicity; Cholesterol; Exercise; Training; Vigorous.