Ninety-day oral toxicological profiling of Kolaviron (an extract of Garcinia kola) in male and female rats.

There remains an insufficiency of data on the long-term toxicological profile of Garcinia kola Heckel and its extract, Kolaviron (KV), despite several studies on its pharmacological effects. This research was designed to investigate the long-term histopathological, hematological, biochemical, hormonal, reproductive, and oxidative effects of 90 days administration of KV to male and female rats, as well as additional 30 days reversibility study to assess the potential for reversal of induced effects. Fifty-six male and female Wistar rats divided into four groups were treated orally with distilled water/propylene glycol, 20 mg/kg KV, 100 mg/kg KV, and 500 mg/kg KV for 90 days. At the end of 90 days and 30 additional days of reversibility study, 5 ml blood was collected from animals for relevant analyses. Vital organs were harvested for histopathological assessments. In this study, KV did not elicit any adverse effect on histopathological presentations of vital organs which were generally non-abnormal. There was significant increase (p < 0.05) in LEU, MON, EOS%, BAS%, HCT (male animals) and LYM%, EOS%, BAS%, RBC, hemoglobin and MCH (female animals). There was significant diminution (p < 0.05) in cholesterol, triglycerides, LDL, and VLDL levels, with significant increase (p < 0.05) in HDL level in both male and female animals. KV elicited a non-significant increase in sperm count accompanied by a significant increase (p < 0.05) in levels of Follicle stimulating hormone (FSH) and testosterone in male rats. Furthermore, KV elicited significant (p < 0.001-0.05) elevation in the levels of GSH, SOD and CAT, and diminution in the level of MDA. The findings in this study suggest that long-term administration of KV is considerably safe with some variations in response between male and female animals. The possible sustenance of observed effects after cessation of KV administration, lipid lowering, erythropoiesis inducing, and immune system boosting activities of KV were confirmed in this study.

Ameliorative effect of Kolaviron, an extract of Garcinia kola seeds, on induced hypertension.

OBJECTIVES: Early diagnosis and management of known cardiovascular disease risk attributes such as hypertension lessens morbidity and mortality as well as increase quality of life of patients. This present study was modelled to investigate the ameliorative effect of Kolaviron, an extract of Garcinia kola Heckel seeds, in ethanol- and sucrose-induced hypertension. METHODS: Test animals were divided into six groups of six animals each for each hypertensive model. Animals were treated daily with distilled water (10 ml/kg); 35% ethanol (3 g/kg) or sucrose (5-7%); Kolaviron (50, 100 and 200 mg/kg) separately plus ethanol or sucrose and Amlodipine (0.14 mg/kg) separately plus ethanol or sucrose for 8 weeks. Systolic, diastolic and mean arterial pressures were determined using non-invasive BP system after 8 weeks. Blood was obtained for the assessment of biochemical parameters, lipid profile and antioxidant indices. Vital organs were collected for approximation of tissue antioxidant levels. RESULTS: Results show that Kolaviron at various doses and Amlodipine significantly reduced (p<0.05-0.001) the elevated systolic, diastolic, and mean arterial pressures produced by ethanol and sucrose administration. Additionally, Kolaviron and Amlodipine significantly overturned (p<0.05-0.001) the reduction in GSH, SOD and CAT, and elevation in MDA levels elicited by ethanol and sucrose. Furthermore, Kolaviron and Amlodipine produced significant reduction (p<0.001) in levels of cholesterol, triglycerides and low-density lipoproteins, as well as significant increase (p<0.01-0.001) in levels of high-density lipoproteins. CONCLUSIONS: Results from this study demonstrate that Kolaviron possibly possesses significant antihypertensive effect which may possibly be attributed to its antioxidant effects and relative improvement of lipid profile.

COVID-19 Pandemic: A Case for Phytomedicines.

Coronavirus disease 2019 (COVID-19) is an infection caused by a newly discovered coronavirus which was identified in Wuhan, China. The race is on globally to repurpose drugs for COVID-19 and develop a safe and effective vaccine against the disease. There is an urgent need to search for effective remedies against COVID-19 from the rich and extensive flora of Africa and the world. A literature search was conducted to obtain information on drugs with the potential for effectiveness in the treatment of COVID-19 based mostly on outcomes of preclinical studies and a few clinical investigations. This was considered important to this perspective as some of the identified mechanisms of action may be related to potential anti-COVID-19 actions of phytomedicines. The findings from the literature search were also used to establish the need for exploration of phytomedicines in the fight against COVID-19. This perspective identifies the need to preserve the rich tradition of herbal medicine in Africa, repositioning it by inculcating all aspects of discovery, development, and chemical evaluation of pharmaceuticals from medicinal plants for effective management of prevalent diseases. The identified mechanisms of action of current drugs under consideration for the treatment of COVID-19 include preventing fusion of SARS-CoV-2 with human cells; decrease acidity in endosomes, cell membrane-derived vesicles for transportation of the virus within the host cell and within which the virus can replicate; and blockade of the production of proinflammatory cytokines. Phytomedicines may possibly elicit either one or a combination of these effects. The case for the exploration of phytomedicines against COVID-19 is strengthened by the emergence of a number of conventional drugs from medicinal plants and the emergence of botanicals with proven efficacy for some medical conditions. Caution against indiscriminate use of medicinal plants in the guise of treating COVID-19 has been highlighted and the need for reliable preclinical and clinical studies.

Anxiolytic- and antidepressant-like activities of hydroethanol leaf extract of Newbouldia laevis (P.Beauv.) Seem. (Bignoniaceae) in mice.

ETHNOPHARMACOLOGICAL RELEVANCE: Newbouldia laevis (Bignoniaceae) is a woody tropical plant commonly found in southwest Nigeria. Ethnobotanical survey and literature revealed its application in the management of CNS disorders e.g. psychosis, insomnia, convulsions and associated anxiety and depression. This study evaluated the anxiolytic and antidepressant activities of the hydroethanol leaf extract of N. laevis in mice. MATERIALS AND METHODS: The hole-board (HBT), elevated plus maze (EPMT), light/dark exploration (LDET), open field (OFT), social interaction (SIT) (anxiolytic activity), forced swim (FST) and tail suspension (TST) (antidepressant property) tests were employed in this investigation. Mice randomly allotted to different groups were treated orally with distilled water (10 ml/kg), diazepam (1 and 3 mg/kg), imipramine (20 mg/kg) and N. laevis (25-200 mg/kg). The mice were subjected to the various tests 60 min post-treatment. RESULTS: In the HBT, N. laevis (25 and 100 mg/kg) increased the number of sectional crossings significantly (p < 0.05). In the OFT, N. laevis (25-200 mg/kg) increased the number of general square crossings, centre square crossings, rearings and assisted rearings (p < 0.05). In the EPMT, the extract (25 and 50 mg/kg) increased the open arms time spent, number of head dips and entry (p < 0.05). In the LDET, N. laevis increased the number of transitions at 100 and 200 mg/kg (p < 0.05). For the SIT, N. laevis (25 and 200 mg/kg) increased the frequency and duration of interaction respectively (p < 0.05). In the FST and TST, N. laevis (25-200 mg/kg) increased the latency and reduced the total duration of immobility (p < 0.05). The effect of the extract on duration of immobility was significantly reversed by sulpiride (Dopamine D2 receptor antagonist). CONCLUSION: The hydroethanol leaf extract of N. laevis possesses anxiolytic- and antidepressant-like activities, the later possibly mediated by dopaminergic enhancement(s).

Investigation of Antidepressant, Anxiolytic and Sedative Activities of the Aqueous Leaf Extract of Musa sapientum Linn. (Banana; Musaceae).

BACKGROUND: Musa sapientum Linn. (Musaceae) is used in traditional African medicine in the management of mental disorders. This study was conducted to evaluate the central nervous system activities of the aqueous leaf extract of M. sapientum (MS). MATERIALS AND METHODS: MS (50, 100 and 200 mg/kg, p.o.) was administered to separate groups of mice 1 h before behavioural studies. The antidepressant effect was studied using the forced swimming test (FST) and tail suspension test (TST) while the elevated plus maze (EPM) and the hole-board tests were used to evaluate the anxiolytic effect. The probable mechanism of antidepressant-like effect was also investigated. RESULTS: MS (50, 100 and 200 mg/kg) produced significant (P<0.0001) reduction in the duration of immobility with peak effect at 200 mg/kg (79.6%) in FST and 66.9 % in TST respectively when compared with control. The pre-treatment of mice with prazosin (α1-adrenoceptor antagonist, 62.5 µg/kg, i.p.) and sulpiride (dopamine D2 receptor antagonist, 50 mg/kg, i.p.) significantly prevented the antidepressant effect produced by MS in FST. However, pre-treatment of mice with metergoline (5-HT2 receptor antagonist, 4 mg/kg, i.p.) and yohimbine (α2-adrenoceptor antagonist, 1 mg/kg, i.p.) did not prevent the antidepressant effect of MS. In the EPM test, MS did not significantly increase open arm exploration. It also did not significantly increase the number of head dips in the hole-board test. CONCLUSIONS: Results showed that MS had antidepressant activity possibly mediated through α1-adrenergic and D2 dopaminergic receptors, without significant anxiolytic effect.

Antidiarrhoeal activity of aqueous leaf extract of Caladium bicolor (Araceae) and its possible mechanisms of action.

ETHNOPHARMACOLOGICAL RELEVANCE: Caladium bicolor (Araceae) is a horticulture plant also used by some traditional medicine practitioners in the treatment of diarrhoea and other gastrointestinal disorders. This study was conducted to evaluate the antidiarrhoeal activity of the aqueous leaf extract of C. bicolor and its possible mechanisms of action in rodents. MATERIALS AND METHODS: Normal and castor oil-induced intestinal transit and castor oil-induced diarrhoea tests were carried out in mice while gastric emptying and enteropooling tests were conducted in rats following the administration of distilled water (10 ml/kg, p.o.), C. bicolor extract (1-50mg/kg, p.o.) and loperamide (5mg/kg, p.o.). The probable mechanisms of action of C. bicolor was investigated following pre-treatment with yohimbine (10mg/kg, s.c.; α2-adrenoceptor antagonist), pilocarpine (1mg/kg, s.c.; non-selective muscarinic receptor agonist), prazosin (1mg/kg, s.c.; α1-adrenoceptor antagonist) and propranolol (1mg/kg, i.p.; non-selective ß-adrenoceptor antagonist) 15 min prior to administration of C. bicolor extract (50mg/kg, p.o.). After 30 min of pre-treatment with these drugs, the mice were subjected to the castor oil-induced intestinal transit test. RESULTS: C. bicolor extract did not produce significant (p>0.05) effect on normal intestinal transit unlike loperamide which caused significant (p<0.001) inhibition (61.57%). The extract caused significant (p<0.001) dose-dependent inhibition of castor oil-induced intestinal transit with peak effect, 100% inhibition, elicited at the dose of 50mg/kg compared to 86.97% inhibition for loperamide. Yohimbine and pilocarpine most significantly (p<0.001) reversed this effect of the extract. In the castor oil-induced diarrhoea test, the extract (1mg/kg) and loperamide significantly (p<0.05, 0.01) delayed the onset of diarrhoea. For diarrhoea score, the extract (1 and 50mg/kg) inhibited diarrhoea development (47.53% and 43.83% inhibition, respectively) like loperamide (5mg/kg; 54.94%). The in vivo antidiarrhoeal index of the extract at 1 and 50mg/kg was 50.07% and 42.81% respectively compared to 58.15% for loperamide. CONCLUSIONS: The results obtained in this study suggest that the aqueous leaf extract of C. bicolor possess antidiarrhoeal activity due to its anti-motility effect possibly via antagonist action on intestinal muscarinic receptors and agonist action on intestinal α2-adrenoceptors. This justifies the use of the extract in traditional medicine for the treatment of diarrhoea.

In Vitro and In Vivo Anticancer Activity of Root Extracts of Sansevieria liberica Gerome and Labroy (Agavaceae).

Introduction. Sansevieria liberica Gerome and Labroy (Agavaceae) is a perennial plant widely distributed in tropical Africa. Preparations of the plant are commonly used across Nigeria for the treatment of inflammatory conditions. Based on the fact that herbal medicine is a strong component of integrative medicine, this study was conducted to evaluate the anticancer activity of root extracts of Sansevieria liberica. Methods. Sulforhodamine B (SRB) in vitro cytotoxicity assay, Sarcoma-180 (S-180) ascites and solid tumor, and L1210 lymphoid leukemia in vivo models were used in this study. Results. SL-A002 (IC50 23 µg/mL with HeLa), SL-A003 (IC50 22 µg/mL with HCT-116), and SL-A004 (IC50 23 and 18 µg/mL with A549 and THP-1, resp.) demonstrated significant activity in the SRB cytotoxicity assay. Potency was highest with the following pairs of extract : cancer cell line: SL-A002 : HeLa (IC50 23 µg/mL), SL-A003 : HCT-116 (IC50 22 µg/mL), and SL-A004 : THP-1 (IC50 18 µg/mL). SL-A002 demonstrated significant dose-dependent antitumor activity in the Sarcoma-180 (S-180) ascites model with peak effect produced at the dose of 120 mg/kg (i.p.) with inhibition of 89.36% compared to 97.96% for 5-FU (20 mg/kg i.p.). The inhibition of tumor growth by SL-A002 in the S-180 solid tumor model was 47.40% compared to a value of 50.18% for 5-FU. SL-A002 was also significantly active in the L1210 lymphoid leukemia model with 158.33% increase in mean survival time, the same value for 5-FU. Conclusions. The hydroethanolic extract of Sansevieria liberica, SL-A002, possesses significant anticancer activity to warrant further extensive study to identify, isolate, and characterize the specific bioactive molecules responsible for the observed antitumor activity and the precise mechanism(s) of action.

90 Days toxicological assessment of hydroethanolic leaf extract of Ipomoea asarifolia (Desr.) Roem. and Schult. (Convolvulaceae) in rats.

ETHNOPHARMACOLOGICAL RELEVANCE: Ipomoea asarifolia (Convolvulacae), commonly known as "morning glory" is found across West Africa. Preparations of the plant are used traditionally for the treatment of diverse ailments including diabetes, neuralgia, arthritic pain and stomach ache. This study was designed to assess the safety profile of the hydroethanolic leaf extract of I. asarifolia through a 90-day subchronic toxicity study in rats. MATERIALS AND METHODS: I. asarifolia was administered p.o. at doses of 40, 200 and 1000mg/kg to separate groups of rats for 90 days. Distilled water was given p.o. to rats in the control group. Some set of rats in each group were left for additional 30 days without administration of the extract for reversibility study. Animals were weighed weekly and relevant parameters were assayed at the end of the main and reversibility study periods. RESULTS: There was no significant change (p>0.05) in the body weight of rats, and food and water intake in I. asarifolia treated groups compared with control. I. asarifolia (40-1000 mg/kg) significantly but reversibly reduced (p<0.05, 0.001) sperm motility and count. The extract did not generally cause significant change (p>0.05) in the weight of vital organs and haematological parameters except in the case of reversible reduction in the level of haemoglobin and red blood cell count (p<0.01; 40 mg/kg). The level of biochemical parameters and electrolytes were not significantly changed (p>0.05) except for the reversible reduction in the level of aspartate aminotransferase (AST; p<0.0001; 200 and 1000 mg/kg) and increase in the level of Na(+) (p<0.01; 200 mg/kg). The level of kidney reduced glutathione (GSH) was reversibly increased (p<0.01; 1000 mg/kg) while the level of enzymatic and non-enzymatic in vivo antioxidants was generally comparable and not significantly different (p>0.05) from control in respect of all other vital organs. Histological presentations were generally normal in respect of the liver, kidneys, brain, heart, lungs, pancreas, spleen and testes. CONCLUSIONS: The findings in this study suggest that the hydroethanolic leaf extract of I. asarifolia is relatively safe administered orally for an extended period with potential renal in vivo antioxidant activities. However, the extract may cause reversible male sterility, anaemia and hypernatraemia.

Anticancer activity of the phytomedicine DAS-77.

This study was designed to investigate the anticancer activity of extracts of the phytomedicine DAS-77. The sulforhodamine B (SRB) in vitro cytotoxicity assay, Sarcoma-180 (S-180) ascites and solid tumor, and L1210 lymphoid leukemia in vivo models were employed. DAS-A001 (ethanol extract, IC50 12 and 13 µg/mL with HCT-116 and PC3, respectively); DAS-A002 (hydroethanol extract, IC50 <5 and 13 µg/mL with HCT-116 and PC3, respectively); DAS-A003 (aqueous extract, IC50 <5 µg/mL with THP-1); and DAS-A004 (dichloromethane:methanol extract; IC50 <5 and 17 µg/mL with HCT-116 and PC3, respectively) demonstrated significant activity in vitro. DAS-A002 and DAS-A003 (80-120 mg/kg) elicited significant (P < .05-.001) dose-dependent inhibition of tumor growth in the S-180 ascites model. Peak effects were produced at the highest dose of 120 mg/kg with inhibition values of 87.50% and 89.23% for DAS-A002 and DAS-A003, respectively, compared with a value of 97.27% for 5-FU (20 mg/kg). As regards the S-180 solid tumor model, inhibition of tumor growth was found to be 52.56% and 37.95%, respectively, for DAS-A002 and DAS-A003. The effect of DAS-A002 was comparable and not significantly different (P > .05) from that of 5-FU (20 mg/kg; 50.18% inhibition). DAS-A003 but not DAS-A002 showed significant activity in the leukemia model with 177.78% increase in mean survival time relative to 211.11% for 5-FU. Findings in this study suggest that the hydroethanol and aqueous extracts of DAS-77 possess significant anticancer activity.

Evaluation of neuropharmacological effects of aqueous leaf extract of Albizia glaberrima (Leguminosae) in mice.

ETHNOPHARMACOLOGICAL RELEVANCE: Albizia glaberrima is a shrub found in the deciduous forest and jungle of the coastal plain of West Africa. Preparations of the plant are used traditionally in the treatment of fever, pain and central nervous system disorders, including epilepsy. This study was conducted to investigate the neuropharmacological effects of the aqueous leaf extract of Albizia glaberrima in mice. MATERIALS AND METHODS: The hole-board, elevated plus-maze, thiopentone-induced sleep (anxiolytic/sedative-hypnotic), traction, climbing, inclined screen (muscle relaxant), strychnine-, picrotoxin- and pentylenetetrazole (PTZ)-induced convulsion (anticonvulsant) tests were employed in this study. RESULTS: Albizia glaberrima extract at 200mg/kg significantly increased the duration of head dips (p<0.05) and number of open arms entry (p<0.01) compared with control in the hole-board and elevated plus-maze tests, respectively. At 400mg/kg, Albizia glaberrima extract significantly reduced the number of sectional crossings relative to control. The extract at 400mg/kg significantly (p<0.05) increased the duration of sleep compared with control in the thiopentone-induced hypnosis test. Albizia glaberrima extract at 200mg/kg and diazepam (5mg/kg) significantly (p<0.05, 0.01) increased the post-treatment climbing time and reduced the latency to slide down in the climbing and inclined screen tests, respectively. The extract was not effective in the strychnine-induced seizure model, while in the picrotoxin test Albizia glaberrima extract at 100mg/kg significantly (p<0.05) reduced the duration of convulsion while reducing mortality at 400mg/kg, as was the case with diazepam (2mg/kg). The extract and diazepam significantly (p<0.01, 0.001) increased onset and reduced duration of convulsion, with significant level of protection against convulsion and reduction in mortality in the PTZ-induced seizure model. Preliminary phytochemical screening of the extract revealed the presence of phenols>tannins>saponins>flavonoids. The extract was found to be relatively non-toxic when administered p.o. up to 5000mg/kg and the LD50 was 398.11mg/kg when administered i.p. CONCLUSIONS: The aqueous leaf extract of Albizia glaberrima possesses dose-dependent anxiolytic/muscle relaxant (low dose) and sedative-hypnotic/anticonvulsant (high dose) activities possibly mediated via enhancement of GABAergic inhibitory actions.

Ameliorative Effect of Hydroethanolic Leaf Extract of Byrsocarpus coccineus in Alcohol- and Sucrose-Induced Hypertension in Rats.

Hypertension remains a major health problem worldwide considering the prevalence of morbidity and mortality. Plants remain a reliable source of efficacious and better tolerated drugs and botanicals. This study was designed to investigate the effect of the chemo-profiled hydroethanolic leaf extract of Byrsocarpus coccineus in ethanol- and sucrose-induced hypertension. Groups of rats were treated orally (p.o.) with distilled water (10 ml/kg), ethanol (35%; 3 g/kg), sucrose (5-7%), and B. coccineus (100, 200, and 400 mg/kg), and nifedipine together with ethanol and sucrose separately for 8 weeks. At the end of the treatment period, blood pressure and heart rate of rats were determined. Blood was collected for serum biochemical parameters and lipid profile assessment, and the liver, aorta, kidney, and heart were harvested for estimation of in vivo antioxidants and malondialdehyde (MDA). Results obtained in this study showed that B. coccineus at the various doses administered reduced the systolic, diastolic, and arterial blood pressure elevated by ethanol and sucrose. Also, the extract reversed the reduction in catalase (CAT), reduced glutathione (GSH), glutathione peroxidase (GPx), and superoxide dismutase (SOD) induced by ethanol and sucrose. The level of MDA was reduced compared to the ethanol- and sucrose-induced hypertensive group. With respect to lipid profile, administration of B. coccineus at the various doses reduced the levels of triglycerides, low-density lipoprotein (LDL), cholesterol, and atherogenic indices, compared to the ethanol and sucrose groups. In conclusion the hydroethanolic leaf extract of B. coccineus exerted significant antihypertensive effect and this is probably related to the antioxidant property and improvement of lipid profile observed in this study.

Hepatoprotective and in vivo antioxidant activities of the hydroethanolic leaf extract of Mucuna pruriens (Fabaceae) in antitubercular drugs and alcohol models.

AIM: Hepatotoxicity is a significantly increasing health problem worldwide, and the extent of the problem has stimulated interest in the search for hepatotherapeutic agents from plants. This study investigated the hepatoprotective and in vivo antioxidant activities of the hydroethanolic extract of Mucuna pruriens leaves in antitubercular and alcohol-induced hepatotoxicity assays in rats. METHOD: In each of the models used, seven groups were allotted. The different groups received normal saline (10 mL·kg(-1), p.o.); hepatotoxicant (isoniazid-rifampicin, INH-RIF, 100 mg·kg(-1), i.p. or 20% ethanol 5 g·kg(-1), p.o.) and normal saline (10 mL·kg(-1), p.o.); hepatotoxicant and extract at doses of 100, 200, and 400 mg·kg(-1) p.o.; hepatotoxicant and silymarin 50 mg·kg(-1) p.o.; and extract at 400 mg·kg(-1) p.o. On the 21(st) day of treatment, blood was collected for assessment of serum biochemical parameters and harvested liver samples were assessed for antioxidants. RESULTS: The hepatotoxicants significantly (P < 0.05-0.001) increased the levels of alanine transaminase (ALT), aspartate transaminase (AST), alkaline phosphatase (ALP), bilirubin, and malondialdehyde (MDA); and reduced the levels of catalase (CAT), superoxide dismutase (SOD), glutathione peroxidase (GPx), and reduced glutathione GSH compared to control. M. pruriens significantly reversed (P < 0.05-0.001) the elevation in the level of ALT, AST, ALP, and bilirubin caused by the hepatotoxicants. The extract (200 and 400 mg·kg(-1)) significantly reversed (P < 0.05) the diminution in the level of in vivo antioxidants and increased the level of MDA produced by INH-RIF. M. pruriens (100-400 mg·kg(-1)) elicited significant reduction (P < 0.001) in the level of MDA compared to the alcohol group. Silymarin also reversed the deleterious effects of the hepatotoxicants. CONCLUSION: The hydroethanolic extract of Mucuna pruriens leaves possesses hepatoprotective activity with enhancement of in vivo antioxidants as a possible mechanism of action.

Hypoglycemic and antioxidant activities of the hydroethanolic leaf extract of Byrsocarpus coccineus Schumach. & Thonn. (Connaraceae).

AIM: Diabetes Mellitus is associated with significant morbidity and mortality worldwide. The need for enhanced efficacy and safety, and cheaper and more readily available new drugs has increased the search for new antidiabetic drugs from plants. This study was conducted to investigate the antidiabetic activity of the hydroethanolic leaf extract of B. coccineus in rats. METHODS: The effect of B. coccineus extract (100-800 mg · kg(-1), p.o.) on blood glucose levels in normal and glucose loaded rats, and alloxan-induced diabetic rats was determined. After 10 days of treatment, blood samples were collected from rats for lipid and insulin profiling. Animals were thereafter sacrificed and the kidneys, heart, and liver were harvested for antioxidant indices assay. RESULTS: In normal rats, B. coccineus did not cause significant reduction in blood glucose. At the dose of 800 mg · kg(-1), significant increase in blood glucose level was not observed 30 min. after glucose load. B. coccineus administered acutely did not generally produce significant reduction in blood glucose level in diabetic rats. Administered subacutely, the extract significantly reduced blood glucose level in diabetic rats from the 3(rd) day with peak effect observed at the dose of 800 mg · kg(-1) on the 10(th) day. The extract generally preserved in vivo antioxidant levels in the kidneys, heart, and liver, increased the level of high density lipoprotein and insulin, and reduced the level of triglycerides and low density lipoprotein compared to diabetic control. CONCLUSION: The findings in this study suggest that the hydroethanolic leaf extract Byrsocarpus coccineus possesses antidiabetic activity possibly mediated through inhibition of intestinal glucose absorption, in vivo antioxidant activity, and enhancement of regeneration of beta cells of the pancreas and insulin secretion.

Effects of Telfairia occidentalis (fluted pumpkin; Cucurbitaceae) in mouse models of convulsion, muscle relaxation, and depression.

Telfairia occidentalis (Cucurbitaceae) is a leafy vegetable used in soup and folk medicine in southern Nigeria. Ethnobotanical survey revealed that preparations of the plant are used in the treatment of central nervous system-related disorders including convulsion. This study was conducted to investigate the effect of the hydroethanolic leaf extract of T. occidentalis in mouse models of convulsion, muscle relaxation, and depression. The strychnine and isoniazid convulsion, traction and climbing muscle relaxation, and forced swim and tail suspension depression tests were used in this study. The extract was administered orally (p.o.) at dose range of 25-800 mg/kg while distilled water (10 mL/kg p.o.) served as negative control. Diazepam (5 mg/kg p.o.) was used as positive control in the convulsion and muscle relaxation models while imipramine (64 mg/kg p.o.) served the same purpose in the depression tests. T. occidentalis significantly increased the onset (P<.001) and reduced the duration of convulsion (P<.05, .01) in the strychnine test and increased the time to death (P<.05, .01, .001) in the isoniazid model. The extract insignificantly increased the reaction time in the traction test while it significantly increased the time in the climbing test (P<.001). In the forced swim and tail suspension models, T. occidentalis significantly (P<.001) and dose-dependently increased the duration of immobility. The results obtained in this study suggest that the hydroethanolic leaf extract of T. occidentalis possesses anticonvulsant and muscle relaxant properties, thus justifying its folkloric use.

Anxiolytic and sedative properties of hydroethanolic extract of Telfairia occidentalis leaves in mice

Telfairia occidentalis Hook. f., Cucurbitaceae, is a leafy vegetable used in soup and folk medicine in southern Nigeria. This study was conducted to investigate the anxiolytic and sedative activities of the hydroethanolic extract of the leaves of T. occidentalis in mice. The hole-board, elevated plus maze, open-field, light-dark, and social interaction tests were used in this study. T. occidentalis (50-400 mg/kg) and diazepam (1 mg/kg) were administered p.o. to different groups of mice and appropriate observations were made. T. occidentalis increased the number of sectional crossings (p<0.01) and duration of head dips (p<0.05) at doses of 50 and 100 mg/kg respectively; increased number of entries into open arms (p<0.01) at the dose of 100 mg/kg; increased number of central squares crossed (p<0.01) at the dose of 50 mg/kg; and increased number of social interactions (p<0.001) at doses of 50 and 100 mg/kg. At the dose of 400 mg/kg, T. occidentalis reduced number of head dips and sectional crossings (p<0.01); reduced time spent in open arms and increased time spent in closed arms (p<0.01, 0.001) at doses of 200 and 400 mg/kg; reduced number of assisted rearings (p<0.001) at doses of 200 and 400 mg/kg; increased latency of entry into and time spent in dark box (p<0.01, 0.001) at doses of 200 and 400 mg/kg; and reduced number of social interactions (p<0.001) at the dose of 400 mg/kg. The findings in this study suggest that T. occidentalis possess anxiolytic property at doses of 50 and 100 mg/kg, and sedative activity at doses of 200 and 400 mg/kg.

Effect of Flabellaria paniculata Cav. extracts on gastric ulcer in rats.

BACKGROUND: The leaves and root of Flabellaria paniculata (Malpighiaceae) are frequently used in the treatment of wounds and ulcers in Nigerian folk medicine. The purpose of this study was to compare the effect of ethanolic extracts from the leaves (FPL) and root (FPR) of F. paniculata on gastric ulcers in rats. METHODS: The effect of FPL and FPR (100, 200 and 400 mg/kg) was evaluated in ethanol and indomethacin gastric ulcer models. Control groups for FPL and FPR were orally treated with 3% Tween 20 and distilled water respectively. FPL was further investigated in pylorus ligation model. Misoprostol and cimetidine were used as reference. RESULTS: FPL significantly (P < 0.05) reduced gastric lesions by 82.22% and 67.32% in ethanol and indomethacin induced ulcer models at 100 mg/kg respectively while FPR (100, 200 and 400 mg/kg) did not exert significant effect in the two models. In pylorus ligation model, FPL exerted a significant preventive antiulcer effect as indicated by reduction in gastric volume at 200 and 400 mg/kg doses. Only 400 mg/kg of the extract exerted a significant reduction in ulcer index when compared with the control group. The oral route LD50 of FPL was estimated to be 4570 mg/kg while that of FPR was 2754 mg/kg. The LD50 in intraperitoneal injection was estimated to be 1202.26 and 1380.38 mg/kg for FPL and FPR respectively. The phytochemical investigation showed that both extracts possess triterpenoids and saponin, while the presence of flavonoid was detected only in FPL. CONCLUSIONS: The results of this study indicated that FPL and not FPR is effective against experimentally induced gastric ulcers. The presence of varied phytochemical constituents probably influenced the pharmacological differences between the two extracts.

A 90 day chronic toxicity study of Nigerian herbal preparation DAS-77 in rats.

BACKGROUND: The herbal preparation DAS-77, used for the treatment of various ailments in Nigeria, contains the milled bark of Mangifera indica L. and root of Carica papaya L. Toxicological assessment of the preparation was carried out in this study. METHODS: In the acute toxicity study, DAS-77 was administered to mice p.o. up to 20 g/kg in divided doses and i.p. at 250-3000 mg/kg. Mortality within 24 h was recorded. In the chronic toxicity study, rats were treated p.o. for 90 days at doses of 80, 400 (therapeutic dose, TD) and 2000 mg/kg. By 90 days, animals were sacrificed and blood samples collected for hematological and biochemical analysis. Organs were harvested for weight determination, antioxidants and histopathological assessments. RESULTS: DAS-77 did not produce any lethality administered p.o. up to 20 g/kg in divided doses but the i.p. LD50 was 1122.0 mg/kg. At TD, DAS-77 produced significant (p < 0.05) reductions in body weight, food intake and K+, and increases in ovary weight, neutrophils and HDL, which were reversible. Histopathological presentations were generally normal. Effects at the other doses were comparable to those at TD except for reversible increases in antioxidants in the liver, kidney and testes, and sperm abnormality, and reductions in liver enzymes, sperm motility and count. CONCLUSIONS: Findings in this study revealed that DAS-77 is relatively safe with the potential for enhancing in vivo antioxidant activity. However, possibly reversible side-effects include electrolyte imbalance and sterility in males.

Sub-chronic toxicity study of the methanol root extract of Cnestis ferruginea.

CONTEXT: Cnestis ferruginea (CF) Vahl ex DC (Connaraceae) is a shrub abundant in West Africa. Root preparations are used in traditional medicine to treat diverse conditions. OBJECTIVE: To evaluate the sub-chronic toxicological effects of the methanol root extract of CF. MATERIALS AND METHODS: Groups of adult rats of both sexes were treated daily with distilled water (DW) and CF at doses of 80 (sub-therapeutic dose), 400 (therapeutic dose), and 1000 (supra-therapeutic dose) mg/kg orally for 90 days. Animals were weighed weekly and observed for behavioral and morphological changes. At the end, rats were sacrificed and blood samples collected for hematological and biochemical analysis. Vital organs were harvested, weighed, and assessed for in vivo antioxidants and histopathological changes. Sperm analysis and reversibility study were done, and mortality was recorded. RESULTS: CF at the therapeutic dose did not produce any significant irreversible deleterious effects on the weight of animals and vital organs, in vivo antioxidants, histopathological presentation, hematological, biochemical, and sperm parameters. Platelet anomaly was elicited as a delayed effect. Effects at the sub- and supra-therapeutic doses were similar but with delayed anemia in females and weight reduction and sterility in males as possible side effects. CF generally showed a potential to induce in vivo antioxidants. DISCUSSION AND CONCLUSION: Findings suggest that CF given over an extended period possess the potential to cause induction of in vivo antioxidants especially in the ovary. Possible side effects identified with CF, which necessitate caution, include delayed platelet anomaly and anemia in females, weight reduction, and sterility in males.

Effects of the hydroethanolic extract of Mucuna pruriens (L.) DC (Fabaceae) on haematological profile in normal and haloperidol treated rats.

BACKGROUND: Mucuna pruriens (L.) DC (Fabaceae) is a climbing plant claimed in traditional medicine to possess anti-anaemic effect. OBJECTIVE: The study is to investigate the effects of the hydroethanolic extract of M. pruriens (MP) on haematological profile in normal and haloperidol treated rats. METHODS: MP was administered p.o. at doses of 50, 100, 200, and 400 mg/kg to groups of rats daily for 28 days. Control animals received distilled water. Rats were sacrificed on the 28th day and blood samples collected for evaluation of haematological parameters and serum iron. Another set of animals received MP p.o. at same doses but along with haloperidol (0.2 mg/kg, i.p.) daily for 4 days. Three other groups of rats received distilled water, haloperidol, and MP at 400 mg/kg alone. Haematological parameters and serum iron were determined. Extract iron content, phytochemical analysis and acute toxicity studies were also carried out. RESULTS: MP administered to normal rats for 28 days significantly (p < 0.05) reduced the number of platelets and proportion of neutrophils. In haloperidol treated rats, MP significantly reversed the reduction in mean corpuscular haemoglobin (MCH) and mean corpuscular haemoglobin concentration (MCHC) values and increased the red blood cell (RBC) count and packed cell volume (PCV). MP also caused significant reduction in the number of platelets and proportion of neutrophils. Administered alone, MP caused a significant increase in the concentration of haemoglobin. The iron content of MP was found to be 61.20 mg/100 g and it was found to contain alkaloids, cardiac glycosides, saponins and tannins. Given up to 10 g/kg p.o., no deaths and visible signs of toxicity were observed while the LD50 for the i.p. route was estimated to be 1509.46 mg/kg. CONCLUSION: The findings in the study suggest that the hydroethanolic extract of Mucuna pruriens possibly possess beneficial effects in anaemic conditions especially associated with iron deficiency.