HEMATOLOGICAL PARAMETERS OF ALLOXAN-INDUCED DIABETIC RATS TREATED WITH ETHANOL EXTRACTS AND FRACTIONS OF NAUCLEA LAFILOIA LEAF

Hematological parameters which have been implicated in diabetes mellitus were investigated in this study. N-hexane, ethyl acetate, butanol and methanol fractions of the ethanolic leaf extract of Nauclea latifolia were orally administered once daily for 2 weeks to diabetic rats. The levels of RBC, Hb, HCT, MCV, MCH, MCHC, PLT, PCT, MPV, PDW, WBC, lymphocyte and granulocyte were evaluated in blood. There was significant reduction (P < 0.05) in RBC and HCT levels in the treatment groups of ethyl acetate fraction (250 mg/kg) and ethanol extract (250 mg/kg) with significant increases (P < 0.05) in their MCV and MCH levels when compared with the diabetic control group. Significant increases (P < 0.05) in PLT levels of the treatment groups of ethanol extracts, n-hexane fractions and ethyl acetate fraction (100 mg/kg); PCT levels of ethanol extracts group and MPV levels of ethyl acetate fractions treatment groups was high. The treatment groups of glibenclamide, butanol, methanol, n-hexane, ethyl acetate fractions and ethanol extract (250 mg/kg) showed significant reduction (P < 0.05) in their WBC and lymphocyte levels while significant increase (P < 0.05) in granulocyte levels was noted in the treatment group of ethanol extract (100 mg/kg) when compared with diabetic control group. In conclusion, the ethanol extract proved to have anti-infective property. Some fractions, showed capabilities to boost the immune system

Synthesis and in vitro antidiabetic activity of some alkyl carbazole compounds

Purpose: To synthesize some alkyl derivatives of carbazole and evaluate their in vitro inhibitory effect on alpha amylase and alpha glucosidase.Methods: Synthesis of methylcarbazole, ethylcarbazole, propylcarbazole and butylcarbazole was carried out using acid-catalysed alkylation method while in vitro inhibitory assay on alpha amylase and alpha glucosidase enzymes on the  synthesized compounds was evaluated using standard procedures. Acarbose was used as the reference compound.Results: For carbazole, methylcarbazole, ethylcarbazole, propylcarbazole and butylcarbazole, the IC50 values of alpha amylase inhibitory assay were 87.47,  50.23, 47.20, 42.36 and 42.11 μg/mL respectively. IC50 values of alpha  glucosidase inhibitory assay for ethylcarbazole, propylcarbazole and butylcarbazole were 205.30, 153.93 and 152.90 μg/mL, respectively. Carbazole and  methylcarbazole had no inhibitory effect on this enzyme but the reference drug  (acarbose) had a better inhibitory effect towards the two enzymes than the synthesized products.Conclusion: Some alkyl-carbazoles with anti-diabetic effect have been successfully synthesised. Alkylation of carbazole increased the alpha amylase inhibitory effect of carbazole. The inhibitory effect is directly proportional to the chain length of the alkyl group.Keywords: Alkyl carbazole, alpha amylase, alpha glucosidase, synthesi

Evaluation of the antimicrobial and anticancer properties of the fruits of Synsepalum dulcificum (Sapotaceae)

Purpose: To evaluate the antimicrobial and anticancer activities of the fruit of Synsepalum dulcificum (Sapotaceae) against six bacterial strains and on two different colorectal cancer cell lines, respectively.Methods: The dried fruit of the plant was extracted in a Soxhlet apparatus successively with petroleum ether and ethanol, and concentrated in a rotary evaporator to obtain petroleum ether and ethanol extract, respectively. Phytochemical screening was done on the two extracts. The antimicrobial effects of the extracts against Bacillus subtilis, Staphylococcus aureus, Streptococcus pyogene, Pseudomonas aeruginosa, Klebsiella pneumoniae and Proteus vulgaris were evaluated using agar well diffusiontechnique while the anticancer effect of the ethanol extract was assessed on HCT-116 and primary colon epithelial (PCE) cell lines by MTT assay.Results: The results indicate that the petroleum ether extract of Synsepalum dulcificum fruits exerted stronger antimicrobial activity than the ethanol extract. The ethanol extract also showed significant anticancer activity (p < 0.05). The calculated half-maximal concentration (IC50) of the extract on HCT- 116 cells at 24, 48, and 72 h are 14.99, 8.97, and 8.54 μg/mL, respectively, while the IC50 of the extract on PCE cell lines at 24, 48, and 72 h are 236.25, 206.09, and 196.72 μg/mL, respectively. The extract was more toxic to cancer cells than to normal cells.Conclusion: The results of this study lend some justification for the use of the fruits of Synsepalum dulcificum as an antibacterial and anticancer agent

Isolation of a pentacyclic triterpenoid from the antiplasmodial bioactive fraction of Nauclea latifolia (Sm) roots

Purpose: To research the antiplasmodial property of aqueous extract, fractions, and residue of Nauclea latifolia roots and to isolate the components responsible for the antiplasmodial activity.Methods: Roots of N. latifolia were macerated with distilled water; the extract was obtained, successively partitioned with ethyl acetate and butanol. The extract, fractions, and the residue obtained were evaluated for their in vivo antiplasmodial activity and compared with amodiaquine and artesunate. The residue (which exhibited the best therapeutic index) was subjected to column and thin layer chromatography to isolate its components. Purification led to the isolation of betulinic acid, which was characterized with the aid of spectroscopic techniques (1H, 13C NMR, and EI-MS).Results: The residue significantly inhibited parasite growth from 42.8 % (D2) to 77.6 % (D5). Therefore, residue exhibited the highest therapeutic index against Plasmodium berghei in the three in vivo antiplasmodial (prophylactic, suppressive, and curative) models and it compared favourably with amodiaquine (80.5 %) and artesunate (85.9 %). The major component of the residue was betulinic acid.Conclusion: The results validate the antiplasmodial claims of the roots of N. latifolia in folkloric medicine, and demonstrated that the isolate has a high therapeutic index in this regard. Further investigations, however, are required to determine the clinical efficacy and safety of the compound/isolate

Isolation and characterization of antioxidant constituents of the fruit of Telfairia occidentalis Hook F (Cucurbitaceae)

Purpose: To evaluate the antioxidant property of the fruit of Telfairia occidentalis and isolate the components responsible for the antioxidant activity.Methods: The fruit pericarp was macerated with methanol and the extract obtained successively partitioned with n-hexane, dichloromethane and ethyl acetate. The in vitro antioxidant activity of the extract and fractions was evaluated using 2,2-diphenyl-1-picryl hydrazyl (DPPH) radical scavenging, reducing power, nitric oxide scavenging, total antioxidant and hydrogen peroxide scavenging assays. The n-hexane fraction, which had the highest DPPH scavenging and total antioxidant activities, was subjected to column and thin layer chromatography to isolate the components. The isolated compounds were identified by ultraviolet-visible (UV), nuclear magnetic resonance (NMR), Fourier transform infrared (FTIR) spectroscopy and mass spectrometry.Results: Among the fractions tested, n-hexane had the best total antioxidant activity of 99.44 % at 20 mg/ml (p < 0.05) compared to ascorbic acid at 99.71 % of 20 mg/ml. This fraction also had the highest DPPH radical scavenging activity of all the fractions (p < 0.05) at all test concentrations. For nitric oxide scavenging activity, the whole extract, and the chloroform and aqueous fractions exhibited activity ranging from 92.29 to 97.66 % compared to 98.93 % for ascorbic acid. The hydrogen peroxide scavenging activity of the extract and fractions ranged from 92.60 to 96.23 % compared with of the standard, ascorbic acid (101.68 %). The major components of the n-hexane fractions were α- amyrin and β-amyrin.Conclusion: The fruit pericarp of Telfairia occidentalis possesses good DPPH radical scavenging activity. This is the first time the antioxidant activity of the fruit (pericarp) and the presence of α- and β- amyrins in Telfairia occidentalis have been reported.Keywords: Telfairia occidentalis, Fluted pumpkin, Amyrin, Antioxidant

Antimicrobial activity of compounds isolated from the leaves of Aspilia africana (Pers.) C. D. Adams (Asteraceae)

Background: Incidences of serious failures in the treatment of infectious disease by antibiotics caused by the emergence and spread of drug resistant strains of the microorganisms/multiple drug resistant bacteria have led to new global search for more effective anti-infective microbial agents from natural sources. This study intends to examine the anti-microbial potentials of the leaves of Aspilia africana, which is employed in the treatment of wounds and sores by traditional medical practitioners in Nigeria. Objective: To evaluate the anti-microbial potentials of the isolates from leaves of Aspilia africana (Pers.) C. D. Adams (Aristeraceae), using isolated clinical strains of pathogens such as Staphylococcus aureus, Methicillin Resistant Staphylococcus aureus (MRSA), Streptococcus pyogenes, Bacillus substilis, Proteus vulgaris, Salmonella typhi, Shigella dysenteriae, Escherichia coli, Klebsiella pneumonia, Candida albicans and Candida stellafoidea. Methodology: Three compounds isolated from butanol fraction of the methanol extract of the dried powdered leaves of Aspilia africana through repeated silica gel column-chromatography and sephadex gel filtration, were evaluated for anti-microbial potentials using Agar-well diffusion method. Results: The isolated compounds identified as oleanolic acid, ursolic acid, and corosolic acid by 1D, 2D-NMR and FITR spectroscopic analyses inhibited the growth of all the pathogens with inhibition diameters ranging between 25 – 33 mm compared with the standard drugs used. The MIC, MBC/MFC of the plant extracts ranged from between 5.00 and 10.00 mg/mL while that of the isolated compounds ranged between 0.0125 and 0.0500mg/mL Discussion: From the results, we conclude that isolated compounds namely oleanolic acid, ursolic acid and corosolic acid are the bioactive constituents responsible for the anti-microbial activity of Aspilia africana. Key words: Aspilia africana, Anti-microbial, Oleanolic acid, Ursolic acid, Corosolic aci

Biochemical changes in serum of Rat treated with aqueous extract of the fruit of Telfairia occidentalis

The effects of the ethanolic fruit extract of T. Occidentalis on some enzymes and biochemical parameters were evaluated in rats. 100,500, and 1000mg/kg of the extract were administered orally and once daily to three different groups of rats, respectively, for 28days .The fourth group which served as Control received distilled water only. On the 29th day, the rats which had been fasted overnight were dissected under Chloroform anaesthesia and blood was collected directly from their hearts. The blood was allowed to clot and centrifuged to obtain the serum which was kept in a refrigerator at –4°C until used for analysis of the following parameters :alanine and aspartate transaminases, alkaline phosphatase, cholesterol, Triglycerides, creatinine, high density lipoproteins, total and conjugated bilirubin ,and total proteins. The fruit extract of the plant significantly elevated the serum concentrations of cholesterol, triglycerides, total proteins, at the three dose levels . The 500 and 1000mg/kg doses increased the concentrations of HDL and conjugated bilirubin. While only 100 and 500mg/kg doses of the extract reduced the level of total bilirubin. The hypercholesterolemic, hyperproteinemic, hypertriglyceridemic and hyperconjugated bilirubinemic effect of this extract coupled with the increased activity of alkaline phosphatase suggest that the fruit of Telfaira Occidentalis may not be safe for consumption. This is quite contrary to the nutritional usage of the leaf and seed of this plant

Biochemical Changes in Serum of Rat Treated With Aqueous Extract of the Fruit of Telfairia Occidentalis

The effects of the ethanolic fruit extract of T. Occidentalis on some enzymes and biochemical parameters were evaluated in rats. 100,500, and 1000mg/kg of the extract were administered orally and once daily to three different groups of rats, respectively, for 28days .The fourth group which served as Control received distilled water only. On the 29th day, the rats which had been fasted overnight were dissected under Chloroform anaesthesia and blood was collected directly from their hearts. The blood was allowed to clot and centrifuged to obtain the serum which was kept in a refrigerator at –4°C until used for analysis of the following parameters :alanine and aspartate transaminases, alkaline phosphatase, cholesterol, Triglycerides, creatinine, high density lipoproteins, total and conjugated bilirubin ,and total proteins. The fruit extract of the plant significantly elevated the serum concentrations of cholesterol, triglycerides, total proteins, at the three dose levels . The 500 and 1000mg/kg doses increased the concentrations of HDL and conjugated bilirubin. While only 100 and 500mg/kg doses of the extract reduced the level of total bilirubin. The hypercholesterolemic, hyperproteinemic, hypertriglyceridemic and hyperconjugated bilirubinemic effect of this extract coupled with the increased activity of alkaline phosphatase suggest that the fruit of Telfaira Occidentalis may not be safe for consumption. This is quite contrary to the nutritional usage of the leaf and seed of this plant

Studies On The Effects Of An Alcohol Extract Of The Leaves Of Telfairia occidentialis On Alloxan Induced Diabetic Rats

The effect of 96% ethanol extract of the leaf of Telfaria ocidentalis on alloxan induced diabetic rats were investigated. A dose of 500mg/kg of the extract was orally administered daily to the test animals for 9 days while the control animals received saline. The following biochemical parameters were evaluated: haemoglobin, glucose, cholesterol, total protein, proteins fractions, Alanine Amino transferase (ALAT) and Aspartate Transaminase (ASAT) levels. The weight of animal were also monitored. Glucose concentration and ASAT/ALAT quotient increased while ALAT activity decreased significally in the test animal compared with control (

Effect of some Artemisinin and Combination Therapy Regimens with and without Concomitant Administration of Phospholipids on the Levels of Plasma Aminotransferases and Bilirubin in Nigerian Male Subjects

Background: Previous studies in animal have shown that high doses of artemisinin caused injury to liver cells. Presently artemisinin and its derivatives such as artesunate (ART), and it’s combination therapy (ACT) has been adopted as the frontline drug for treatment of uncomplicated malaria in Nigeria without considering the effect it has on some major organs of the body. Objective: The objective of this study was to evaluate the effect of ART when administered as a monotherapeutic agent and in combination as ACT on the plasma levels of aspartate aminotransferase (AST), alanine aminotransferase (ALT) and bilirubin (BIL) and the effect of concomitant administration of a hepatotonic phospholipid (PL) on such effects. Methodology: The prepared plasma samples were analyzed using the end point calorimetric method for each parameter as explained in the Randox kits manual. Results: Co-administration of ART with amodiaquine (AMQ), mefloquine (MFQ) and sulphadoxine/pyremethamine (SP) respectively, on the 4th day of the studies increased the mean plasma concentration of AST to 80.70%, 108.0% and 75.0% against 59% for ART alone; ALT increased to 104%, 33.0% and 43.30% against 25.05% for ART alone; total bilirubin (TBIL) increased to 80.0%, 78.88% and 98.91% against 17.6% for ART alone. The co-administration and post-administration of ART and the ACTs with 900mg and 1800mg daily dose of PL respectively reduced the levels of the AST, ALT and BIL by 65.0% and 97.0% of the increased values respectively on 4th day. Discussion: The results suggest that ART as a monotherapeutic agent has injurious effect on the liver, and this effect is aggravated when ART is used in ACTs, however, the co-administration with phospholipids cushions the adverse effects. Key words: Artesunate; Artemisinin Combination Therapy (ACT); Aminotransferases; Bilirubin; Phospholipid