Assessment of the antidiabetic potential of Pterocarpus santalinoides extract in alloxan-induced diabetic rats

Purpose: To establish the pharmacological basis for the antidiabetic use of Pterocarpus santalinoides.Methods: Alloxan-induced diabetic rats were given graded doses (50, 100 and 200 mg/kg) of P. santalinoides extract (PSE) for 21 days. The fasting blood glucose (FBG), body weight, in vivo antioxidant assay, and lipid profile were determined.Results: Pterocarpus santalinoides extract at all doses tested caused significant (p < 0.05) reduction in FBG and significant (p < 0.05) increase in body weight of treated rats when compared with the control. There were significant (p < 0.05) increases in the activities of antioxidant enzymes and high-density lipoprotein, while the levels of total cholesterol, triglycerides and low-density lipoprotein were significantly (p < 0.05) reduced in PSE-treated rats.Conclusion: These results demonstrate the significant antidiabetic activity of P. santalinoides extract in albino Wistar rats, thus suggesting its potential application for the management of diabetes in humans, Furthermore, the findings may explain its use in ethnomedicine as an antidiabetic regimen.&nbsp

Potential antidiabetic and antioxidant activities of a heliangolide sesquiterpene lactone isolated from Helianthus annuus L. Leaves

Heliangolide is a naturally occurring sesquiterpene lactone and its derivatives are biologically active compounds present in most medicinal plants. This study evaluated the antioxidant and antidiabetic properties of a heliangolide sesquiterpene lactone isolated from Helianthus annuus L. leaves. The heliangolide sesquiterpene lactone was isolated through combination of solvent-solvent partitioning, column chromatography, thin layer chromatography and high performance-liquid chromatography techniques. The antioxidant activity of the compound was evaluated using 2,2-diphenyl-1-picrylhydrazyl (DPPH) and nitric oxide radical scavenging assays while the antidiabetic effects were investigated in alloxan-induced diabetic rats. The heliangolide derivative at 954.2 µmol L–1 showed 23.7 % DPPH and 26 % nitric oxide radical inhibitions compared with 96.6 and 50.9 %, resp., displayed by the controls (2,271.2 µmol L–1). It also reduced the fasting blood glucose (FBG) levels in a time-dependent manner. The highest activity was recorded within 6 h post-treatment at 0.2 mmol kg–1 bm. The heliangolide derivative exhibited significant (p < 0.05) antioxidant and antidiabetic properties and provides basis for further development of constituents of Helianthus annuus leaves for the management of such diseases

Vitamin D supplementation attenuated carageenan-induced paw edema and formalin-induced nociception in indomethacin-treated rats

Background: This work evaluated the effect of vitamin D supplementation on carrageenan-induced paw edema and formalin-induced nociception in indomethacin treated rats.Methods: Rats were grouped into six (A – F) of 5 each. Groups (C – F) were pretreated for 14 days with vitamin D; 250, 500, 1000 and 1000 iu/day respectively. On day 15, they were treated as follows: group A (10 ml/kg distilled water), B; (10 mg/kg indomethacin), C – E; (10 mg/kg indomethacin) F (1000 iu/day vitamin D alone). One hour later 50 1% carrageenan or 25 5% formalin was injected into the sub-plantal surface of left hind paw. For carageenan-induced paw edema, paw sizes were measured 1 h later, then every hour for 5h. For formalin-induced nociception, number of paw licking/lifting was counted for each rat from 0 – 5 min (first phase) and 25 – 30 min (second phase) post-formalin injection.Results: Paw sizes were significantly (P<0.05) lower from 2 – 5 h post-carageenan injection in the 250 iu/day vitamin D + 10 mg/kg indomethacin group when compared with both controls. In the formalin-induced nociception, the 250 iu/day vitamin D + 10 mg/kg indomethacin, 500 iu/day vitamin D + 10 mg/kg indomethacin and the 1000 iu/day vitamin D alone groups produced significantly (p<0.05) lower number of paw lifting when compared with both controls in both phases.Conclusion: These findings suggest that vitamin D exerts antiinflammatory and antinociceptive responses that could be relevant for clinical application

Hypoglycemic, antidyslipidemic, hepatoprotective and antilipid peroxidation activities of hydromethanol leaf extract of Helianthus annuus in alloxan-induced diabetic rats

Purpose: To investigate the hypoglycemic, antidyslipidemic, hepatoprotective and anti-lipid peroxidation effects of hydromethanol leaf extract of Helianthus annuus (HLEHA) in alloxan-induced diabetic rats.Methods: The extract was administered once daily at 150, 300 and 600 mg/kg for 21 consecutive days. Glibenclamide (GLB) 2 mg/kg was used as a reference drug (positive control) and 5 % Tween-20 solution in water was used as negative control. The fasting blood glucose (FBG) and body weights were measured on days 7, 14 and 21 while glycosylated haemoglobin concentration (HbA1c), serum markers of liver function, lipid profile, antioxidant status, histopathological changes in pancreas and liver were determined 24 h after the last dosing on day 21.Results: The GLB and HLEHA caused significant (p &lt; 0.05) time-dependent weight gains in the treated rats when compared with 5 % Tween-20 treated rats. The HLEHA and GLB caused significant (p &lt; 0.05) decreases in FBG, HbA1c, malondialdehyde, and lipid profile levels in the treated rats when compared with rats in 5% tween-20 treated group. Alloxan-induced pancreatic and hepatic degeneration were reversed in GLB- and HLEHA-treated rats.Conclusion:  Helianthus annuus demonstrates potent antidiabetic, antioxidant and antidyslipidemic activities in rats.Keywords: Antidiabetic, Antidyslipidemic, Helianthus annuus, Medicinal plant, Traditional medicin

ANTI-ULCEROGENIC ACTIVITY OF THE METHANOL ROOT BARK EXTRACT OF COCHLOSPERMUM PLANCHONII (HOOK f)

Cochlospermum planchonii (Hook f) is a common medicinal plant used in Nigeria traditional medicine for treatment of different ailments including ulcers. The anti ulcer activity of the root bark methanol extract of Cochlospermum planchonii was evaluated using different [ethanol, acetylsalicylic acid (aspirin), cold/restraint stress and pyloric ligation/histamine – induced ulcers and acid production] ulcerogenic models in rats at the doses of 250, 500, and 1000 mg/kg body weight using cimetidine (100 mg/kg) as a standard reference drug. The different doses of the extract and the reference drug significantly (p < 0.01) decreased all the ulcer parameters in a dose dependent manner in all the models used. The total number of ulcers were significantly (p < 0.05) decreased. The ulcer index was significantly (p < 0.004) reduced by the extract. Similarly, the percentage ulcer preventive index was also increased from 0% in the negative control up to 93.2% at the dose of 1000 mg/kg, while the percentage ulcer severity was dose dependently reduced by the extract. Furthermore, the extract significantly (p < 0.02) decreased free gastric HCl and total gastric acid. In conclusion, Cochlospermum planchonii methanolic root bark extract showed significant antiulcer activity in this study which may be as a result of its cytoprotective, antioxidant or antisecretory properties

Chronic toxicity study of Pterocarpus santalinoides leaf extract in albino rats

Purpose: To investigate the possible toxic effects associated with prolonged use of Pterocarpus santalinoides leaf extract.Methods: Methanol leaf extract of Pterocarpus santalinoides (MEPS) was incorporated in rat feed at different doses (2.5, 5.0 and 10.0 mg/kg) for 90 days. On days 30, 60 and 90, blood was collected from the retro-orbital plexus of four rats that were randomly selected from each group (n = 14). Full blood count was done using an auto hematological analyzer, liver marker enzymes (AST, ALT and ALP) and kidney function parameters (serum urea and creatinine) were determined following standard methods as contained in Randox® test kits. The histopathological examination of the liver, kidney, lung and heart was also carried out.Results: MEPS did not cause significant (p &gt; 0.05) changes in the body weight, relative organ weights and hematological indices of treated rats when compared with control. The extract (5.0 and 10.0 mg/kg) significantly (p &lt; 0.05) increased the AST activity of the rats on day 90. Total bilirubin concentration was significantly (p &lt; 0.05) reduced by all doses of MEPS, while serum urea and creatinine were significantly (p &lt; 0.05) increased. Degeneration of hepatocytes and tubular epithelial cells of the kidney were observed in rats treated with MEPS at a dose of 10.0 mg/kg on days 60 and 90 of the study.Conclusion: MEPS does not cause significant toxicity in albino rats, when administered for a short duration. However, long term therapy with the extract precipitates liver and kidney damage

Hepatoprotective and antioxidant properties of the methanol leaf extract of Diaphananthe bidens in acetaminophen-induced hepatotoxicity in rats

Purpose: To investigate the hepatoprotective and antioxidant properties of the methanol extract of Diaphananthe bidens leaf using acetaminophen-induced hepatotoxicity rat model. Methods: Thirty albino Wistar rats, randomly assigned into 6 groups (A - F, n = 5), were used for the study. Groups A and B received distilled water (10 ml/kg), group C received silymarin (0.10 g/kg) while groups D - F received D. bidens extract 0.15, 0.30 and 0.60 g/kg, respectively, for 7 days. On day 8, groups B - F rats received acetaminophen (2 g/kg) orally. About 48 h later, pentobarbitone sodium (0.035 g/kg) was injected intraperitoneally for sleeping time studies. The time of sleep, time of awake and the duration of sleep were recorded. On awakening, blood samples were collected for evaluation of serum biochemical parameters and antioxidant profile. Thereafter, the rats were humanely euthanized and the liver excised for histopathological evaluation. In vitro antioxidant activity of the extract was evaluated using ferric reducing antioxidant power and 2,2-diphenyl-1-picrylhydrazine (DPPH) scavenging assay. Results: Treatment of the rats with D. bidens decreased (p &lt; 0.05) malondialdehyde values and activities of ALT, AST and ALP, but increased glutathione levels and catalase activities when compared to negative control group. The extract significantly (p &lt; 0.05) decreased sodium pentobarbitone-induced sleeping time relative to the negative control group and produced concentration-dependent increase in antioxidant activities in vitro. The extract protected the hepatocyte against acetaminophen-induced damage. Conclusion: D. bidens extract elicits antioxidant activities in vitro and in vivo and thus, protects rat liver against acetaminophen-induced damage. Therefore, the extract can potentially be developed as a hepatoprotective agent for the clinical management of liver damage

Anti-trypanosomal activity of secnidazole in vitro and in vivo

Purpose: To evaluate the anti-trypanosomal effect of secnidazole (SEC) in vitro and in vivo. Methods: The dose-response effect of SEC in Trypanosoma b. brucei infected rats was evaluated in five groups of rats (n = 5). Group A was infected but untreated; B was given diminazene aceturate (DA) (3.5 mg/kg) intraperitoneally, while groups C, D and E received orally 400, 800 and 1600 mg/kg of SEC, respectively. The effect of a combination therapy of SEC and DA was studied in 7 groups of rats (n =5). Group 1 was infected but untreated; groups 2 – 7 were treated with DA (3.5 mg/kg), while groups 3 – 7 received in addition to DA, increasing double doses of SEC (50 – 800 mg/kg).Results: The MIC of SEC and DA were 1.4 and 0.0021 mg/ml respectively. SEC dose-dependently and significantly (p &lt; 0.05) lowered parasitemia from day 2 post-treatment (PT) compared with infected untreated rats. Parasitemia was cleared 3 days PT in all combination groups and 5 days PT in DA group. Relapse of infection occurred in Group 2, 13 days PT, and 16 and 27 days PT in Groups 3 and 4 respectively. There was no relapse of infection in Groups 5 – 7 up to 70 days PT.Conclusion: These results suggest that SEC possesses some degree of  anti-trypanosomal effect, and that combination therapy of SEC and DA was superior to DA alone.Keywords: Trypanosoma, Secnidazole, Diminazene aceturate, Anti-trypanosomal, Combination therap

Antioxidant, anti-inflammatory and anti-nociceptive properties of hydro-methanol extract of Eremomastax speciosa (Hochst.) cufod leaf

Background: Eremomastax speciosa (Hochst.) Cufod is a perennial herb found in Africa along the rainforest zone and occurs as weed. It is cultivated in Cameroon and Akwa-Ibom in Nigeria due to its medicinal values. This study investigated the antioxidant, anti-inflammatory and antinociceptive properties of hydromethanol extract of Eremomastax speciosa (Hochst.) Cufod leaf in rat model.Materials and Methods: The plant material was extracted using cold maceration method in 80% hydromethanol. The acute oral toxicity test was performed using Up and Down method with limit dose of 2000 mg/kg. The in vitro antioxidant property was evaluated with 2,2-diphenyl-1-picrylhydrazyl and ferric reducing antioxidant power photometric assays. The anti-inflammatory potential was investigated in egg-albumin and carrageenan induced paw edema models while the antinociceptive activity was determined using acetic acid induced writhing reflex and tail immersion tests at the doses of 50, 100 and 200 mg/kg. The negative control group (group A) received distilled water (vehicle) at 5 ml/kg while acetyl salicylic acid (200 mg/kg) was used as the reference drug for the anti-inflammatory models and acetic acid induced writhing reflex model while pentazocine (5 mg/kg) was used as the reference drug for tail immersion test.Results: The LD50 of the extract was greater than 2000 mg/kg. The extract (25 to 400 μg/ml) demonstrated potent antioxidant activities in both the 2,2-diphenyl-1-picrylhydrazyl and ferric reducing antioxidant power assays. The E. speciosa extract caused significant (P &lt; 0.05) anti-inflammatory and antinociceptive activities in the extract treated groups when compared to rats that received distilled water. The optimal activities of the extract were produced at the dose of 100 mg/kg.Conclusion: The study supports the folkloric use of Eremomastax speciosa leaf in the management of pain and inflammatory conditions in traditional medicine.Keywords: Acetic acid, anti-inflammatory, antinociceptive, antioxidant, carrageenan, Eremomastax specios

Disposition kinetics of ceftriaxone and determination of its therapeutic dose in dogs

Purpose: To evaluate the disposition kinetics of ceftriaxone (CFZ) in dogs with a view to determining its therapeutic dose and dosing frequency.Methods: Twelve (12) Basenji dogs (n = 4), divided into 3 groups (A, B and C), were used for the study. Ceftriaxone was administered intramuscularly at doses of 12.5, 25, and 50 mg/kg once to groups A, B and C respectively. Plasma CFZ concentration was determined by agar well diffusion assay at 0.25, 0.5, 1, 2, 3, 4, 6, 8, 10, 12, and 24 h post-treatment, and the pharmacokinetic parameters were determined.Results: Intramuscular injection of CFZ to dogs resulted in rapid absorption, distribution and elimination (p &lt; 0.05). The elimination half-life was short and did not change significantly with increase in dose. Serum concentration of CFZ changed significantly (p &lt; 0.05) with increase in dose of CFZ. The maximum serum concentration (Cmax, 15.00 ± 1.18, 141.37 ± 15.87 and 259 ± 5.21 μg/mL) for groups A, B and C respectively were significantly (p &lt; 0.05) different. The steady state CFZ concentrations; 0.94, 8.81 and 16.19 μg/mL for groups A, B and C, respectively, were significantly (p &lt; 0.05) different. However, there was no significant difference in the time to reach steady state concentrations (Tmax, 00±0.021, 4.00±0.10 and 4.30±0.12 for groups A, B and C respectively). The therapeutic dose of CFZ was therefore determined to be 25 – 50 mg/kg every 4 h.Conclusion: Ceftriaxone undergoes rapid elimination in dogs with a short elimination half-life, thus making it an inconvenient prescription for out-patients in veterinary clinics. Keywords: Ceftriaxone, Pharmacokinetic profile, Dogs, Therapeutic dose, Veterinary clini