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ANTIMICROBIAL AND ANTI – INFLAMMATORY ACTIVITIES OF EXTRACTS OF FICUS THONNINGII BLUME (MORACEAE)
Published 2014-05Subjects: “…Triterpenoid…”
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PHYTOCHEMICAL SCREENING AND ANTIMYCOBACTERIAL POTENTIALS OF Syzygium guineense WILD DC. AND Mimosa pigra LINN
Published 2014-09Subjects: “…Triterpenoids…”
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Page will reload when a filter is selected or excluded.- Anti-inflammatory agents 1 results 1
- Antimicrobials 1 results 1
- Antimycobacterial activity 1 results 1
- Ficus thonningii 1 results 1
- Infectious diseases and the associated inflammation pose a serious health problem worldwide, accounting for about 50% of all deaths in tropical countries. This is further complicated by the frequent development of bacterial resistance to many chemotherapeutic agents. These problems have necessitated the continuous search for new and effective drugs from plant materials. Thus, Ficus thonningii Blume (Moraceae), a plant used ethnomedicinally in West Africa for the treatment of some microbial infections, was studied for its antimicrobial and anti-inflammatory activities. Dried leaves and stem bark of Ficus thonningii were screened for secondary metabolites. Successive gradient extraction was carried out on the pulverised plant parts using hexane, chloroform and methanol with Soxhlet apparatus. Antimicrobial activity of the extracts on Gram-positive (10) and Gram-negative (11) bacteria, and fungal (12) isolates was evaluated using agar-diffusion method. Antibiogram of the microorganisms was determined using established antibiotics. Bioassay-guided fractionation of crude extracts using column chromatography was done. Minimum Inhibitory Concentrations (MIC) and minimum bactericidal concentrations of the crude extracts, fractions and isolated compound were determined by agar-dilution. Bactericidal kinetics of the methanol leaf extract against Staphylococcus aureus and Escherichia coli at 2.5-10.0 mg/mL were determined. Structure elucidation of the bioactive compound was carried out using 1H-NMR, 13C-NMR, DEPT 135, COSY, UV and GC-MS spectroscopy. In vivo anti-inflammatory activity of leaf extract was evaluated using carrageenan-induced rat paw oedema with acetylsalicylic acid as the reference drug. Acute oral toxicity, haematological and histopathological evaluations were carried out to determine the safety profile of methanol leaf extract in rats. Statistical analysis was carried out using Student’s t-test at p = 0.05. Alkaloids, flavonoids, terpenoids and cardiac glycosides were detected in the plant extracts. Antimicrobial assay of crude extracts and fractions showed a broad spectrum activity on sensitive and multidrug-resistant strains with the leaf and stem bark extracts having similar antimicrobial activity. Hexane leaf extract and bioactive fractions gave MIC range of 78-625 µg/mL and 20-625 µg/mL respectively while methanol leaf extract and bioactive fractions gave 156-625 µg/mL and 39-625 µg/mL. Structure elucidation of the bioactive compound isolated from hexane leaf fraction revealed a triterpenoid with MIC range of 20-156 µg/mL (Gram-positive bacteria), 39-156 µg/mL (Gram-negative bacteria) and 10-78 µg/mL (fungi), while that of gentamicin and tioconazole were 5-30 µg/mL and 10-20 µg/mL respectively. Methanol leaf extract showed bactericidal activity in a concentration-dependent manner on the microorganisms, with a 100% bactericidal action at 10 mg/mL on Staphylococcus aureus and 84% on Escherichia coli within 4 hours. The anti-inflammatory activity of methanol leaf extract was 57.5% while that of acetylsalicylic acid was 93.2%. Acute oral toxicity of methanol leaf extract showed an LD50> 5g/Kg. Significant increases were observed in the red blood cell count and mean corpuscular haemoglobin value, while histopathological evaluation revealed no significant tissue pathological changes in the major organs. Extracts of Ficus thonningii leaves contain antimicrobial and anti-inflammatory agents. These could be useful in the development of safe chemotherapeutic agents for the treatment of relevant microbial infections and inflammation-prone diseases. 1 results 1
- Mimosa pigra 1 results 1
- Syzygium guineense 1 results 1
- The prevalence of multi-drug resistant tuberculosis is an increasing health challenge. Attention has therefore been shifted to the use of ethno-medicines in combating this disease. Traditionally, Syzygium guineense (stem-bark) and Mimosa pigra (aerial parts) are used in the treatment of respiratory tract infections with no scientific justification. This study was designed to identify the constituents of Syzygium guineense and Mimosa pigra that may be active against Mycobacterium tuberculosis. The S. guineense (stem-bark) and M. pigra (aerial parts) were obtained from farmlands in Abuja and authenticated at the herbarium of National Institute for Pharmaceutical Research and Development, Abuja. The S. guineense (1.0 kg) was extracted successively with chloroform and methanol. The extracts were separately fractionated with n-hexane followed by acetone. Mimosa pigra (0.5 kg) was extracted with methanol and partitioned with diethylether and n-butanol. The fractions were purified using chromatographic techniques. The extracts, fractions and isolated compounds were subjected to antimycobacterial assay with Mycobacterium tuberculosis (ZMC 050 and 303) strains using the Lowenstein-Jensen and mycobacterium growth indicator tube methods. Streptomycin, isoniazid, rifampicin, and ethambutol were used as standard drugs and dimethylsulphoxide as negative control. The structures of the isolated compounds were elucidated using infrared, ultra-violet/visible, nuclear magnetic resonance and mass spectroscopic techniques. The chloroform extract of S. guineense yielded 4.1 g n-hexane fraction and 5.2 g acetone fraction A while the methanol extract gave 5.2 g acetone fraction B and 98.0 g residue. Crude methanol extract of M. pigra gave 40.1, 4.6 and 12.3 g of diethylether, n-butanol and residue fractions respectively. Two new triterpenoids were isolated from S. guineense namely: 12-hydroxy-27-demethylfriedelan-3-one and betulinic acid methylenediol ester, in addition to the two known triterpenoids: betulinic acid, and friedelan-3-one. One new flavonoid, 8-hydroxy-3-phenyl-4-benzopyrone rhamnoside was isolated from M. pigra. The two plants‘ methanol extracts, n-butanol fraction, acetone fraction A, and isolated compounds: betulinic acid, betulinic acid methylenediol ester and 8-hydroxy-3-phenyl-4- benzopyrone rhamnoside were active against ZMC 050 strain with Minimum Inhibitory Concentrations (MIC) of 5.0, 5.0, 2.0, 0.6, 0.6, 0.15 and 0.5 mg/mL respectively. The ZMC 303 strain also gave similar MIC values as ZMC 050 strain. Spectroscopic analysis of 12-hydroxy-27-demethylfriedelan-3-one provided evidence for δH signals: 0.8-1.2 UNIVERSITY OF IBADAN LIBRARY iv (7CH3), 1.2-1.8 (10CH2), and 2.2-2.4 (5CH), δC signals: 29.9-41.7 (5C), 72.8 (1CHOH) and 213.4 (1C=O) with a molecular ion of 428 corresponding to C29H48O2. The betulinic acid methylenediol ester showed δH and δC signals similar to betulinic acid except for the downfield methylenedioxy carbinol (OCH2O) δC signal at 79.0 and molecular ion of 486 correspond to C31H50O4. Betulinic acid and friedelan-3-one signals are similar to published spectra. The 8-hydroxy-3-phenyl-4-benzopyrone rhamnoside showed δH signals: 0.9 (3Hd, J=5.8 Hz), 3.1-3.8 (overlapping glycone multiplet) and 5.2 (anomeric) typical of a rhamnose moiety, with δH 6.2 (1H), 6.4 (1H), 6.9 (5H) and δC 178.0 (1C=O) of the flavonoid ring. The bioactive compounds obtained from Syzygium guineense and Mimosa pigra exhibited anti-mycobacterial activities. They have potentials for the development of drugs for the management of tuberculosis. The new triterpenoids and flavonoids are addition to the library of compounds. Keywords: Syzygium guineense, Mimosa pigra, Antimycobacterial activity, Triterpenoids Word count: 484 1 results 1
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