Anti-proliferative activities of Byrsocarpus coccineus Schum. and Thonn. (Connaraceae) using ovarian cancer cell lines.

BACKGROUND: Ovarian cancer (OvCa) is one of the most lethal tumors of gynecologic malignancies, due to lack of early detection, and a high rate of metastasis. The standard treatment for OvCa is surgery and cytotoxic chemotherapy. However, to overcome the high cost and side effects of these treatments, medicinal plants are widely used in developing countries to treat OvCa. Byrsocarpus coccineus plant preparation has been administered to patients traditionally in the management of tumors in Nigeria. In this study, we investigated the anti-proliferative effects of B. coccineus ethanol leaf extract against OVCAR-3 and SW 626 OvCa cell lines. After the treatment of the two cell lines with the extracts, analyses were carried out to determine inhibition of proliferation and expression of cell cycle markers, pro-apoptotic, and anti-apoptotic markers. RESULTS: Results showed that B. coccineus ethanol leaf extract, significantly inhibited cell migration and colony formation in OVCAR-3 and SW 626 treated cells in a dose-dependent manner. Results also show that B. coccineus ethanol leaf extract modulated the expression of tumor suppressor gene (p53), cell cycle progression, pro- and anti-apoptotic gene, and the pro-inflammatory cytokines. CONCLUSIONS: These results suggest that B. coccineus have anti-proliferative properties and could induce apoptosis. Further investigation will be carried out to isolate bioactive compounds for the treatment of ovarian cancer.

Hepatoprotective properties of aqueous leaf extract of Persea Americana, Mill (Lauraceae) 'avocado' against CCL4-induced damage in rats.

BACKGROUND: Natural products from plants have received considerable attention in recent years due to their diverse pharmacological properties, including antioxidants and hepatoprotective activities. The protective effects of aqueous extract of Persea americana (AEPA) against carbon tetrachloride (CCl4)-induced hepatotoxicity in male albino rats was investigated. MATERIALS AND METHODS: Liver damage was induced in rats by administering a 1:1 (v/v) mixture of CCl4 and olive oil [3 ml/kg, subcutaneously (sc)] after pre-treatment for 7 days with AEPA. Hepatoprotective effects of AEPA was evaluated by estimating the activities of alanine aminotransferase (ALT), aspartate aminotransferase (AST), alkaline phosphatase (ALP) and levels of total bilirubin (TBL). The effects of AEPA on biomarkers of oxidative damage (lipid peroxidation) and antioxidant enzymes namely, catalase (CAT), superoxide dismutase (SOD), glutathione peroxidase (GPx) and glutathione S-transferase (GST) were measured in liver post mitochondrial fraction. RESULTS: AEPA and Reducdyn® showed significant (p<0.05) hepatoprotective activity by decreasing the activities of ALT, AST, ALP and reducing the levels of TBL. The activities of antioxidant enzymes, levels of malondialdehyde and protein carbonyls were also decreased dose-dependently in the AEPA-treated rats. Pre-treatment with AEPA also decreased the serum levels of glutathione significantly. CONCLUSION: These data revealed that AEPA possesses significant hepatoprotective effects against CCl4-induced toxicity attributable to its constituent phytochemicals. The mechanism of hepatoprotection seems to be through modulation of antioxidant enzyme system.

Robustaside B and para­hydroxyphenol: phenolic and antioxidant compounds purified from Cnestis ferruginea D.C induced membrane permeability transition in rat liver mitochondria.

The antioxidant properties of robustaside B and para­hydroxyphenol isolated from Cnestis ferruginea were measured as the rate of inhibition of thiobarbituric acid reactive substance (TBARS) production in the Fe2+/ascorbate system. The modulatory effects of the compounds on mitochondrial membrane permeability transition (MMPT) were monitored spectrophotometrically as decreases in light scattering at 540 nm. The varying concentrations of robustaside B and para­hydroxyphenol (0.05, 0.1, 0.2, 0.25, 0.5, 0.75 and 1 mM) significantly reduced (P<0.05) the amount of TBARS generated by the Fe2+/ascorbate system by 85.3, 86.4, 86.0, 86.1, 86.0, 86.0 and 86.0% and 86.7, 81.3, 81.3, 80, 80, 82.6 and 83.1%, respectively. Similarly, quercetin, a standard antioxidant, was found to induce an 80% reduction in the amount of TBARS produced. The same IC50 value of 0.025 mM was observed for robustaside B, para­hydroxyphenol and quercetin. Pre­incubation of varying concentrations of robustaside B (0.125, 0.2, 0.5 and 1 mM) with succinate­energized mitochondria induced MMPT pore opening by 0, ­33.3, ­59.3 and ­218.5%, compared with control mitochondria. Para­hydroxyphenol at 0.1, 0.2, 0.25 and 0.5 mM induced MMPT pore opening in a concentration­dependent manner up to 0.25 mM by ­21, ­54.4 and ­107.0%, respectively. Quercetin at 0.05, 0.1, 0.25, 0.5, 0.75 and 1 mM also induced MMPT pore opening in the absence of calcium in a concentration­dependent manner by 5, 3.7, ­42.6, ­81.5, ­187 and ­161.1%, respectively. The current observations confirm the antioxidant properties of robustaside B and para­hydroxyphenol, and indicate a potential therapeutic use of the compounds for the treatment of diseases requiring the induction of cell death, including cancer.

Hypoglycemic activity of Buchholzia coriacea (Capparaceae) seeds in streptozotocin-induced diabetic rats and mice.

The present study evaluates the possible hypoglycemic activity and ameliorative effects of oral administration of ethanol extracts (EEBC) and butanol fraction (BFBC) of Buchholzia coriacea seeds, a plant in use traditionally for treating diabetes, hypertension, rheumatism, cold, cough and catarrh, in streptozotocin (STZ)-induced diabetic mice and rats. Fasting blood glucose (FBG) levels were evaluated before and after extracts administration. EEBC and BFBC significantly decreased (P<0.05) FBG in hyperglycemic mice and normoglycemic rats within 4 and 12 h, respectively after extract administration. The administration of EEBC, BFBC and glibenclamide (a standard antidiabetic drug) for 10 days significantly lowered (P<0.05) FBG level in STZ-induced diabetic rats by 55%, 64% and 56%, respectively. EEBC and BFBC significantly (P<0.05) decreased hepatic injury induced by STZ as evident in the decreased activity of serum alanine amino transferase and aspartate amino transferase compared to in the STZ-only treated group. Similarly, both extracts significantly decreased (P<0.05) the elevated levels of serum creatinine, urea, total cholesterol, triglyceride and thiobarbituric acid reactive species (TBARS) products in diabetic rats. Serum superoxide dismutase activity was significantly enhanced (P<0.05) by treatments with EEBC, BFBC and glibenclamide. Overall, the results suggest that B. coriacea seeds contain a potent hypoglycemic and antioxidant agent suggested to be a flavone glycoside concentrated in BFBC which may find clinical application in amelioration of diabetes-induced secondary complications.

Hypoglycaemic and biochemical properties of Cnestis ferruginea.

Increasing incidences of diabetes in Africa has prompted the search for safe and readily available alternative herbal remedies for the treatment of diabetes mellitus. Cnestis ferruginea was extracted with methanol and ethylacetate and the extracts obtained were tested for hypoglycaemic activities in streptozotocin (STZ)-induced diabetic rats and mice. The extracts (250 mg/kg body weight) were administered orally for 10 consecutive days to STZ-induced diabetic rats while a single dose (250 mg/kg body weight) of the extracts were administered to STZ-induced diabetic mice. Fasting blood glucose (FBG) levels were determined in the two groups of animals after extract administration. There was significant reduction in FBG (P< 0.005) by MCF and ECF within 4 hrs of extract administration in a time- dependent manner. Furthermore, administration of MCF and ECF for 10 days significantly lowered FBG in STZ diabetic rats (P<0.005) by 74% and 68%, respectively, whereas, glibenclamide - a standard antidiabetic drug reduced FBG by 60%. The levels of serum creatinine, urea, triglyceride, total cholesterol, total protein and level of lipid peroxidation were also evaluated. The extracts reduced significantly (P<0.005) the elevated levels of serum ALT and AST in diabetic treated rats. Similarly, both extracts significantly lowered (P<0.005) the levels of serum creatinine, urea, total cholesterol, triglyceride and thiobarbituric acid reactive species (TBARS).These results suggest that Cnestis ferruginea leaves contain a highly potent hypoglycaemic principle and could be a potential source for isolation of new orally active antihyperglycaemic compounds for attenuating secondary complications of diabetes such as atherosclerosis, liver and renal dysfunction.

Comprehensive assessment of the effect of Sphenocentrum jollyanum root extract on male reproductive activity in albino rats.

Aim: To evaluate the effect of methanol extract from the Sphenocentrum jollyanum root on male reproductive activity. Methods: Male albino rats were treated orally with distilled water (vehicle for the extract; control) and 50, 100 and 150 mg kg-1 body weight of Sphenocentrum jollyanum root extract for 8 weeks. Each group had its own recovery. Rats were killed 24 h after the last treatment. Caudal epididymal sperm count, motility, viability, morphology and organ weights were determined. Hematological indices, serum proteins, enzymes, testicular superoxide dismutase (SOD) activity, and testicular and epididymal histology were determined. Results: Compared with the control, the extract caused a dose dependent significant (P < 0.05) reduction in progressive motility of spermatozoa, viability and total sperm counts. The number of abnormal spermatozoa and epididymal volume were not statistically significant. There was a significant increase (P < 0.05) in serum testosterone levels in rats treated with 50 (P < 0.01) and 100 mg kg-1 (P < 0.05) of Sphenocentrum jollyanum. There was a significant (P < 0.05) increase in red blood cell count, packed cell volume and hemoglobin concentration, whereas there was no change in white blood cell count, mean total serum protein, albumin and globulin in the sera of Sphenocentrum jollyanum treated rats when compared with the control. The extract caused a significant decrease (P < 0.05) in serum aspartate and alanine aminotransferase activities with a significant increase (P < 0.05) in testicular SOD activity at a dose of 50 mg kg-1 bodyweight. Testicular cytoarchitecture of the extract treated rats showed degeneration of seminiferous tubules, whereas regeneration of germinal epithelium and restructuring of the germinal interstitium occurred in the recovery rats. No lesions were observed in the epididymis of the rats. Conclusion: The results suggest that methanol extract of the Sphenocentrum jollyanum root could produce harmful effects on reproductive functions in male albino rats which can be attributed to poor sperm quantity (epididymal sperm count), quality (sperm motility, viability and morphology) and testicular degeneration. The steroidogenic potential of the plant could explain its use as an aphrodisiac agent. (Reprod Med Biol 2006; 5: 283-292).