The LD(50) of roselle calyx extract and its effect on blood pressure were determined. The LD(50) was found to be above 5000 mg kg(-1). Roselle calyx infusion was found to lower significantly (p<0.05) both systolic and diastolic pressure in spontaneously hypertensive and normotensive Wistar-Kyoto rats at tested doses of 500 and 1000 mg kg(-1) body weight. The reduction in blood pressure in both groups was positively correlated with weight. Continuous consumption of the infusion at 1000 mg kg(-1) was discovered to lead to sudden death in spontaneously hypertensive rats but not in Wistar-Kyoto rats. Water intake was not significantly different (p>0.05) in the control groups of the two strains of rats used, neither was there a significant difference in their urine output. The water intake in the treated spontaneously hypertensive and normotensive rats was not different from the corresponding control groups. However the urine output of the treated spontaneously hypertensive rats was significantly higher. A significant decrease in serum creatinine, cholesterol, and glucose in the treated rats compared with the control as well as a significant increase in serum uric acid was observed. The serum proteins (albumin and total protein) in the treated rats when compared with the control groups was not changed significantly.
Aqueous, ethanolic and hexane extracts of the leaves of Nauclea latifolia (Rubiaceae) were assessed for their fasting blood glucose lowering effect in normoglycaemic and streptozotocin -diabetic rats. Wistar strain albino rats were given different doses of the extracts after 18 hrs fast and their blood glucose measured at 0,1,2,4 and 6 hours after treatment. The aqueous and ethanolic extracts significantly lowered the fasting blood glucose levels of the STZ-diabetic rats in a dose-dependent manner. The highest dose administered (400mg/kg) lowered the fasting blood glucose of the diabetic rats by 31.7% (aqueous) and 36.1% (ethanolic) extracts. The aqueous extract did not significantly lower the glucose levels of normoglycaemic rats (maximum 6.6%), nor was any significant decrease seen in the rats administered with the hexane (maximum of 4.0% for normoglycaemic and 2.4% for diabetics) extract. The hypoglycaemic and antihyperglycaemic potentials of the aqueous and ethanolic extracts were comparable to that of glibenclamide (1mg/kg).These results further support the traditional use of the plant in the treatment of diabetes mellitus.
Searching for new compounds against pathogenic trypanosomes has been substantially accelerated by the development of in vitro screening assays. In an attempt to explore the chemotherapeutic potential of organotin compounds and to broaden the search for newer trypanocides, fatty acid derivatives of dibutyltin dichloride were synthesized and their in vitro trypanocidal profiles studied on Trypanosoma brucei brucei, Trypanosoma brucei gambiense and Trypanosoma brucei rhodesiense. A 24-h time course experiment was conducted with various concentrations of the compounds using a 24-well microtiter plate technique. The compounds tested were trypanocidal in a dose-dependent fashion: inhibiting survival and growth, resulting in irreversible morphological deformation and the eventual death of the parasites. The minimum inhibitory concentrations of the tested diorganotins are at low micromolar ranges: from 0.15-0.75 microM for T. b. brucei, T. b. gambiense and T. b. rhodesiense. These observations suggest that organotin has chemotherapeutic potential.
Background: Garcinia kola is used in traditional medicine in various parts of Africa including Nigeria for the amelioration of hypertension, cough, diabetes, sickle cell anemia, bacterial and fungal infections amongst others. The prophylactic and therapeutic efficacy of Garcinia kola biflavonoid fractions (GKBF); root bark (RBBF), stem bark (SBBF) and seed (SBF)) on the lipid profile and kidney function of Poloxamer 407 (P407) induced hyperlipidemic rats were determined.
Activity and kinetics of phospholipase A2 (PLA2) from Trypanosoma brucei gambiense (Wellcome strain) and Trypanosoma brucei brucei (GUTat 3.1) were examined using two different fluorescent substrates. The activity in the supernatants of sonicated parasites was Ca2+-independent, strongly stimulated by Triton X-100 with optimum activity at 37 degrees C and pH 6.5-8.5. To encourage a possible interaction between the parasite enzyme and organotin compounds, fatty acid derivatives of dibutyltin dichloride were synthesized and evaluated as potential inhibitors of PLA2. The enzyme from the two-trypanosome species differ with respect to kinetic parameters and are noncompetitively inhibited by the organotin compounds. The Michaelis constant (KM) for PLA2 from T. b. brucei is 63.87 and 30.90 microM while for T. b. gambiense it is 119.64 and 32.91 microM for the substrates 1,2-bis-(1-pyrenebutanoyl)-sn-glycero-3-phosphocholine (PBGPC) and 2-(12-(7-nitrobenz-2-oxa-1,3-diazol-4-yl)amino)dodecanoyl-1-hexadecanoyl-sn-glycero-3-phosphocholine (NBDC12-HPC), respectively.
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