RESUMEN
BACKGROUND: The incidence of pain and inflammation in West Africa and in fact globally, continues to increase at an alarming rate. This research was conducted to investigate the analgesic and anti-inflammatory activities of leaf extracts of Chasmanthera dependens and Chenopodium ambrosioides; formulate and evaluate polyherbal gels from their combination in a bid to providing topical therapeutic solutions to pain and inflammation. METHODS: Pre-formulation studies (phytochemical analysis, in vitro analgesic and anti-inflammatory activities) were conducted on the methanol leaf extracts of Chasmanthera dependens and Chenopodium ambrosioides. Individual and polyherbal gels were prepared using polymer carbopol 940 (1%) at combination ratios of 0:100, 25:75, 50:50, 75:25 and 100:0 Chasmanthera:Chenopodium. These herbal gels were evaluated for physical parameters, pH, viscosity, extrudability and spreadability. Analgesic and anti-inflammatory activities of herbal gels were evaluated by their inhibitory activities (percentage inhibition) against COX-2, TNF-α, IL-10, PGE-2 and compared with commercial diclofenac gel. RESULTS: The phytochemicals of the two extracts detected gave varied contents of major classes of secondary metabolites. The pre formulation inhibitory studies of the two extracts exhibited dose dependent inhibitory activities against COX-2, TNF-α, IL-10, PGE-2. The physical appearance, homogeneity, and consistency of the herbal formulations were good. The herbal gels were spreadable with good extrudability. The pH of the herbal gels ranged from 4.5 ± 0.4 to 5.2 ± 0.4. The viscosity of the herbal gels ranged between 4.3 ± 0.2 and 4.7 ± 0.4 Pas. The herbal gels exhibited significant differences in inhibitory activities against COX-2, TNF-α, IL-10, PGE-2 when compared with control commercial diclofenac gel. CONCLUSION: The outcomes, including the inhibition of mediators COX-2, TNF-α, IL-10, PGE-2, confirm the use of the plant extracts under study, the individual and polyherbal gels formulated for the potential topical therapeutic treatment of pain and inflammation.
RESUMEN
BACKGROUND: Food and herbal usage of Hibiscus sabdariffa (HS) is attaining improved global relevance and acceptance without recourse to its potential toxic effects. This study investigated the safety profile of acute, sub-acute, sub-chronic administrations and diuretic potential of aqueous extract of Hibiscus sabdariffa calyces (AEHSC). METHOD: Acute oral toxicity, sub-acute and sub-chronic toxicity as well as diuretic studies were carried out on HS. A total of 20 Wistar rats were used for each toxicity study and assigned into four groups of five rats. The extract was administered as a single daily dose of 125, 250 and 500 mg/kg body weight (bwt) for 28 and 90 days respectively. To evaluate diuretic activity, 25 rats were divided into five groups of five rats and administered normal saline, hydrochlorothiazide 10 mg/kg, AEHSC 67.5, 125 and 250 mg/kg via the oral route. Urine sample was collected after 18 h, volume measured and concentration of electrolytes analyzed. The hematological and biochemical parameters were evaluated as well as the histopathology of kidney and liver. RESULTS: The acute oral toxicity was found to be >2000 mg/kg. AEHSC did not alter concentration of WBC, MCV, MCHC, lymphocyte as well as total and direct bilirubin in the sub-acute study. However, AEHSC significantly (p < 0.05) increased total protein, albumin, globulin, Na+, Cl-, HCO3 - and platelet levels, while levels of uric acid, creatinine, K+, RBC, Hb, total cholesterol, triglycerides, LDL-C, HDL-C and atherogenic index were decreased significantly (p < 0.05). In the sub-chronic study, AEHSC significantly (p < 0.05) increased the levels of globulin, urea, creatinine, MCH and atherogenic index. The concentrations of uric acid, WBC, platelets and HDL-C were significantly (p < 0.05) decreased. In both the sub-acute and sub-chronic studies, activities of ALP, ALT, AST, GGT and LDH in selected organs were altered without significant increase (P < 0.05) in activity of these enzymes in the serum. The AEHSC at all the doses showed remarkable diuretic activity during 18 h period comparable to hydrochlorothiazide. The extract also showed a non-dose-dependent increase in excretion of electrolytes. Histological analysis of sections of the liver and kidney for both sub-acute and sub-chronic studies showed normal histology comparable to the control group. CONCLUSION: This study revealed AEHSC has some toxic effects in rats on sub-chronic administration. In addition, the extracts produced a significant diuretic activity. Hence, prolonged oral consumption of the extract may not be recommended.