Evaluation of the Antibacterial Activities of Isolated Bioactive Components from the plant Adenodolichos paniculatus

The three bioactive components isolated included: component A (major phytochemicals were Bis (2-ethylhexyl) phthalate (16.36 %), 9,12-Octadecadienoic acid, ethyl ether (14.77 %) and 9.cis., 11.trans.-octadecadie noate (14.77 %), component B (major phytochemicals were 9,12-Octadecadienal (Linoleic acid) (40.98 %), Octadecanoic acid (Stearic acid) (9.26 %), Undecanoic acid, 10-bromo- (10-bromoudecanoic acid) (9.26 %) and n-Hexadecanoic acid (Palmitic acid) and component C (cis-9-octadecenoic acid (Oleic Acid) (30.45 %), Octadecanoic acid (Stearic acid) (17.33 %)). These components isolated from the chloroform fraction of Adenodolichos paniculatus are used by traditional medicinal practitioners for the management of mouth and throat infections. The antibacterial activities against Streptococcus pyogenes, Staphylococcus aureus and Pseudomonas aeruginosa were evaluated using bioautography and agar-well diffusion methods. The bioautogram result showed that component A had inhibited spots against S. pyogenes (17.50 mm) and P. aeruginosa (16.00 mm), corresponding to the TLC spots with Rf values of 0.594, 0.55 and 0.26, respectively. Component B showed inhibition spots against Streptococcus pyogenes (36.50 mm), Staphylococcus aureus (16.00 mm) and Pseudomonas aeruginosa (11.00 mm), corresponding to the TLC spots with Rf values 0.891, 0.87, 0.85 and 0.25, respectively. Component C showed inhibition spots against Streptococcus pyogenes (16.50 mm), Staphylococcus aureus (15.00 mm) and Pseudomonas aeruginosa (10.50 mm), corresponding to the TLC spots Rf values of 0.938, 0.44, 0.21 and 0.90, respectively. For the agar-well diffusion method, component A at 1 mg/ml inhibited Streptococcus pyogenes, Staphylococcus aureus and Pseudomonas aeruginosa growths with zones of inhibition 23.0, 19.5 and 17.50 mm, respectively. MIC and MBC of component A were 125, 250 and 250 and 250, 500 and 500 μg/ml, respectively. Component B at 1 mg/ml inhibited Streptococcus pyogenes, Staphylococcus aureus and Pseudomonas aeruginosa growth with zones of inhibition 30.0, 28.0 and 18.5 mm, respectively. MIC and MBC of the compound B were 31, 62 and 125 and 62, 125 and 250 μg/ml, respectively. Component C at 1 mg/ml inhibited Streptococcus pyogenes, Staphylococcus aureus and Pseudomonas aeruginosa growth with zones of inhibition 24.5, 20.5 and 17.0 mm, respectively. MIC and MBC of the component C were 62, 125 and 250 and 125, 250 and 500 μg/ml, respectively. This study confirmed that bioactive compounds of A. paniculatus root have antibacterial properties and support the use of this part of the plant as a traditional remedy for mouth and throat infections possibly caused by the test bacteria.

Pharmacognostic and physicochemical evaluation, HPLC analysis and antiproliferative properties of Kigelia africana (Lam.) Benth

Introduction/Objective of study: Kigelia africana (Bignoniaceae) is enriched with bioactive constituents and has thus found various uses in African folklore. This study aims to evaluate the pharmacognostic, physicochemical, chromatographic and antiproliferative properties of K. africana.Methodology: Standard methods were used to determine the qualitative microscopy, moisture content, ash and extractive value. Furthermore, HPLC analysis was conducted on the samples in order to detect and quantify some phenolic compounds (gallic acid, chlorogenic acid, rutin, ferulic acid, caffeic acid and quercetin). The Sorghum bicolor model was used for the antiproliferative assay. All experiment was carried out in triplicates.Results: Microscopy revealed amphistomata with the presence of non-glandular unicellular, uniseriate trichomes on K. africana leaf. Cellulose, tannins, calcium oxalate crystals on the leaf and stem bark, while the roots lacked calcium oxalate crystals. Ash contents were leaf (21.8 ± 0.1) %w/w, stem bark (4.8 ± 0.03)%w/w and root (3.9 ± 0.2)%w/w. Moisture content was (10.5 ± 0.5) %w/w and (9.5 ± 0.2) %w/w for the root and leaf parts, respectively. All values were within WHO limits for crude drugs. The stem bark and root parts contained more water-soluble constituents than alcohol soluble constituents. From the results of HPLC analysis the leaf, stem bark and root extracts gave 24 peaks, 16 peaks and 30 peaks, respectively, a few peaks matched with reference compounds- quercetin, caffeic acid, ferulic acid and rutin. Results of antiproliferative assay showed that methotrexate was significantly (p ˂ 0.05) more effective than the stem bark (from 2-64 mg/mL) with inhibitions ranging from 72.0 ± 1.4% - 90.0 ± 2.4% and root extracts (from 4 – 64 mg/mL) that had inhibitions ranging from 50.3 ± 1.5% - 97.7 ± 0.4% but comparable with leaf extract (from 16 mg/mL - 64 mg/mL) with inhibitions ranging from 68.4 ± 0.8% - 99.0 ± 0.1%.Conclusion: Further information which can be included in an official monograph of the plant for its proper identification and quality control has been provided by this study. Kigelia africana exhibited effective antiproliferative activities and the presence of phenolic compounds.

Extraction, isolation and evaluation of anti-toxic principles from Moringa oleifera (MOF6) and Myristica fragrans (Trimyristin) upregulated Acetylcholinesterase concentrations in Sodium arsenite-induced neurotoxicity in rats.

This study evaluated the neuroprotective effects of MOF6 (isolated from Moringa oleifera leaves) and Trimyristin (isolated from Myristica fragrans seeds) on Acetylcholinesterase concentrations in cerebral cortices of rats with Sodium arsenite-induced neurotoxicity. Sixty-five adult male rats (150 g-250 g) were randomly divided into thirteen groups comprising of five rats per group. Groups 1 and 3 received physiological saline and 1 ml/200 g bodyweight of Olive oil respectively for 9 weeks. Group 2 received 20 mg/kg bodyweight of Sodium arsenite (SA) for 6 weeks and left untreated for another 3 weeks. Groups 4-5 received 20 mg/kg bodyweight of SA for 3 weeks followed by treatments with 5.0 and 7.5 mg/kg bodyweight of MOF6 respectively for 6 weeks. Groups 6-7 received 20 mg/kg bodyweight of SA for 3 weeks followed by treatments with 15 and 30 mg/kg bodyweight of Trimyristin respectively for 6 weeks. Groups 8-11 received 5.0 and 7.5 mg/kg bodyweight of MOF6; 15 and 30 mg/kg bodyweight of Trimyristin respectively for 9 weeks. Groups 12-13 received 7.5 mg/kg bodyweight of MOF6 and 30 mg/kg bodyweight of Trimyristin respectively for 6 weeks followed by co-administration of each extract dose with 20 mg/kg bodyweight of SA for another 3 weeks. Histological examination of cerebral cortices and biochemical analyses of Acetylcholinesterase concentrations were carried out in all rats. Computed data were analyzed using Microsoft Excel 2016 with statistical significance at p≤0.05. Histo-pathological evaluations revealed normal histo-architecture of cerebral cortices of all rats. Results showed statistically significant (p≤0.05) increases in Acetylcholinesterase concentrations in rats of Groups 1-10 and 12 compared with Group 2 (2.78±1.76 𝜇mole/min/g). 7.5 mg/kg bodyweight of MOF6 showed the best therapeutic and neuro-regenerative potential against SA-induced neurotoxicity.Conclusions: Our findings implied that MOF6 and Trimyristin reversed downregulation of Acetylcholinesterase concentrations in SA-induced neurotoxicity in rats; and possess neuro-protective and neuro-regenerative potentials.

Preparation and evaluation of the physicochemical and stability properties of three herbal tea blends derived from four native herbs

Herbal teas consist of mono and sometimes poly-herbal recipes of herbs with acclaimed health benefits which are often brewed as infusion or decoction. Three variants of poly-herbal teas containing Herbiscus sabdariffa, Moringa oleifera, Citrus limon, and Zingiber officinale were prepared and evaluated for their physicochemical and stability properties. Intrinsic physicochemical properties that include organoleptic, ash value, pH of brew solutions, extractive matter as well as non-intrinsic properties such as moisture content, flow and particle size of granules and dust leak from teabags were determined. Also, the effects of stressful storage conditions on some physicochemical properties were evaluated. The different tea blends showed remarkable differences in their physicochemical properties. The products also showed discrepancies in stability parameters such as appearance, pH of the brew and antioxidant properties when stored under different conditions. In all, the herbal tea showed good physicochemical and stability properties that are characteristic of a good finished herbal product.

Preliminary Evaluation of the Acute and Sub-Acute Anti-Inflammatory Activities of Aqueous and Butanol Leaf Fractions of Olax subscorpioidea Oliv. (Olacaceae).

Olax subscorpioidea (Oliv.) leaf is widely used as a traditional remedy for pain, reduction of small tumors, edema, painful swellings, and other inflammatory conditions. Its anti-inflammatory potential in experimental animals has been documented. Furthermore, an anti-inflammatory assay guided fractionation showed that the aqueous and butanol leaf fractions were the most active. This study is aimed at investigating further, the acute and sub-acute anti-inflammatory potentials of the aqueous and butanol leaf fractions in mice and rats.Carrageenan induced paw edema in rats, xylene induced ear edema in mice, and cotton pellet induced granuloma in rats were the models employed for the studies. For each of the methods, four randomly-selected groups of animals (n=5/6) were orally administered with distilled water (1 ml/kg), aqueous or butanol fraction (1,000 mg/kg) and standard drugs (acetylsalicylic acid [ASA] 300 mg/kg or dexamethasone, 1 mg/kg).The aqueous and butanol fractions each showed significant (p < 0.01) inhibition of ear swelling, the fractions also significantly (p < 0.05, p < 0.01) decreased the paw edema, and significantly (p < 0.01) inhibited the granuloma formation.The result of the study suggests that aqueous and butanol leaf fractions of Olax subscorpioidea are effective against acute and sub-acute inflammation.

Physicochemical and phytochemical screening of six plants commonly used in the treatment of malaria in Nigeria.

Medicinal plants contain active compounds usually present as complex mixtures though at low concentrations, which accounts for the medicinal properties. Therefore it is important to identify and characterize these compounds. This study aims to quantify and characterize the physicochemical and phytochemical compositions of six plants commonly used in the treatment of malaria using High-Performance Liquid Chromatography (HPLC). These plants which are used individually or in combinations: Enantia chlorantha, Cymbopogon citratus, Curcuma longa, Carica papaya, Alstonia boonei and Mangifera indica, were extracted with hot water and the extracts characterized with HPLC using standard procedures. The results showed that M. indica stem bark had the highest yield with 81.48% and C. papaya had the lowest yield with 53.80%. Physicochemical properties of the extracts of E. chlorantha, C. citratus, C. longa, C. papaya, A. boonei and M. indica respectively are as follows: Melting point 90, 80, 95, 92, 96 and 96; pH 7.43, 8.02, 6.24, 6.81, 6.41, 6.85; moisture content 18.27, 22.77, 9.96, 9.62, 3.85 and 10.00; Total ash 1.45, 3.51, 0.34, 0.57, 9.10,10.21; refractive index 1.34, 1.34, 1.34, 1.34, 1.34, 1.34 and 1.34. Alkaloids, phenols, flavonoids, terpenoids, tannins, coumarin were some of the antimalarial active phytochemicals identified. Alkaloid (Atropine) was highest in C. longa (4382.2mg/g). M. indica (32982.8mg/g) had the highest Rutin Hydrate content. While Quercetin was not detected in C. papaya, it was considerably present in A. boonei (491.1mg/g). All the analyzed six plants contain low phenol (gallic acid). The characterized physicochemical and phytochemical compositions of the examined plants suggests why the plants are effective in the treatment of malaria. The information reported herein describes the physicochemical and phytochemical contents of six commonly used antimalarial plants in Nigeria. It is expected that the information will be useful in understanding the pharmaceutical effects of how the plants work in the body and in the development of efficacious and safe antimalarial drugs.

Formulation of non-effervescent floating matrix tablets of metronidazole using Abelmoschus esculentus gum as binder and 2-camphanone as sublimating agent.

The aim of this study was to formulate non-effervescent floating drug delivery system of metronidazole tablets using Abelmoschus esculentus (Okra) (AE) gum as a binder and 2-camphanone (camphor®) as the sublimating agent. Granules were prepared by wet granulation technique using varying concentrations of AE gum (2, 4, 6 and 8% w/w) admixed with 1%w/w acrylate methacrylate copolymer. A 30 %w/w of 2-camphanone was used as the sublimating agent. The granules were characterized for micromeritic properties. And thereafter, compressed at a compression pressure of 25 N/m2 using a Manesty single punch tableting machine. The metronidazole tablet was then sintered at 70oC for 12 h. Drug-excipient compatibility study was done using Fourier Transform Infra-red Spectroscopy (FTIR). Tablets were evaluated for floating lag time, in-vitro buoyancy and release kinetics. FTIR studies showed that the excipients and the active pharmaceutical ingredient (API) i.e. metronidazole, were compatible. All the granules were free flowing, with Carr’s index ≤ 15 %, Hausner ratio ≤ 1.18 and angle of repose of ≤ 33.5o. The tablets had hardness and friability values of 5.0-9.5 N and 0.4-0.8% respectively. The floating lag time was 0 s showing that the tablets floated immediately after immersion in the simulated gastric fluid. The maximum % release (m∞) and time to achieve it (t∞) were ≥ 88 % and ≥ 10 h, respectively. Release exponent (n) for all the formulations had values >0.45, hence their release was by non-Fickian diffusion. Non-effervescent floating matrix tablets of metronidazole were formulated using AE gum as the binder and 2-camphanone as the sublimating agent. The formulated floating tablets had increased in-vitro retention time, which indicated potential for sustained release of the drug. If well developed, this may help reduce the oral dosing frequency and encourage patient adherence to the drug therapy. Keywords: Non-effervescent, Abelmoschus esculentus, 2-camphanone, floating

GC-MS analysis and Mitochondrial Functionality Potential of the Fruits ofTetrapleura tetraptera By Cupric Reducing Antioxidant Capacity Assay

The use of antioxidants has emerged as a promising therapeutic strategy for the management of mitochondrial dysfunction and other oxidative stress-related degenerative pathologies. Tetrapleura tetraptera is a well-known tree and its fruit is applied traditionally as spice and in the preparation of remedies for different ailments. In this study, the gas chromatography-mass spectrometry (GC-MS) analysis and mitochondrial functionality potential of T. tetraptera fruits were investigated. GC-MS was used to detect compounds in then-hexane and ethanol extracts of T. tetraptera fruits. Cupric reducing antioxidant capacity (CUPRAC) assay was used to evaluate the mitochondrial functionality potential of the ethanol extract. GC-MS analysis revealed the presence of six compounds in then-hexane extract of T. tetraptera fruits. These compounds were detected in trace quantities, the most abundant being 2,3-dimethyl-3-buten-2-ol (0.04%). The compounds: cis-vaccenic acid (35.37%), n-hexadecanoic acid (28.09%), 6-octadecenoic acid (25.21%), and octadecanoic acid (11.33%) were identified in the ethanol extract of the fruits. Consequently, the ethanol extract was subjected to CUPRAC assay. The ethanol extract exhibited a concentration-dependent high cupric reducing capacity, returning CUPRAC values in the range of 0.090 to 0.403 at the concentration of 10 – 80 μg/ml. This activity was comparable to that of the positive control, naringenin, which showed CUPRAC values of 0.059 – 0.378 at the same concentrations. These results indicate that T. tetraptera fruits possess good antioxidant property as evaluated by other related antioxidant assays. This could be attributed to a synergistic effect of the phytochemical constituents. Hence consumption of T. tetraptera fruits could be beneficial for the prevention of mitochondrial dysfunction and other oxidative stress-related degenerative disorders. Keywords: Tetrapleura tetraptera, mitochondrial dysfunction, degenerative disorders, CUPRAC, GC-MS, Nigeria

Phytochemical, Antioxidant and Antimicrobial studies of Lannea egregia Engl. & K. Krause (Anacardiaceae) extracts and chromatographic fractions

Screening ‘new’ medicinal plants of traditional importance for bioactive components is a sure way of discovering novel therapeutic agents to treat diseases. This study, therefore investigated the presence of phytochemical, antioxidant and antibacterial components of the extracts of Lannea egregia. Phytochemical screening was done by standard methods. Antibacterial activity of the extracts of Lannea egregia was determined by agar well diffusion method while the minimum inhibitory concentration (MIC) was determined by agar dilution method. The antioxidant capacity of the crude extracts was determined through the evaluation of total flavonoid content, total phenolic content, ferric reducing power, total antioxidant capacity and 2,2-diphenyl-1-picryhydrazyl. The phytochemical screening of the different parts of this plant revealed the presence of tannins, saponins, alkaloids, flavonoids, steroids, terpenoids, emodins, phlobatannins, anthocyanins, coumarins and phenolics. Phlobatannins was observed to be absent in the stem bark. The crude extracts obtained from the leaves, stem bark and roots of this plant exhibited good antibacterial activity against typed strains of Staphylococcus aureus, Bacillus subtilis, Pseudomonas aeruginosa and Escherichia coli. The diameter of the zone of inhibition ranged from 9.0 to 26.0 mm at 100 mg/mL for all the plant parts. The ethyl acetate leaf extract of this plant possessed the highest antibacterial activity with MIC and MBC values of the range of (3.125 to ˃50 mg/mL) and (12.5 to ˃50 mg/mL) respectively. The zone inhibition of the chromatographic fractions of both plants ranged 15-23 mm. Antioxidant study of the extracts of the leaf of L. egregia revealed that the ethyl acetate and methanol extracts have good antioxidant potentials comparable to that of ascorbic acid control. This study has revealed that the extracts from different parts of L. egregia possess good antibacterial and antioxidant activities which could be a function of the various phytochemicals detected in the plant. Keywords: Lannea egregia, Phytochemical, Antibacterial, Antioxidant, Column chromatography.

A Comparative Evaluation of Fast Dissolving Tablets of Acetaminophen Using Super-disintegrant Blends and Sublimation Method

Fast disintegrating tablets (FDTs) are gaining prominence as drug delivery systems and emerging as one of the popular and widely accepted dosage forms, especially for the peadiatric and geriatric patients. This study aims to evaluate and compare the tablet properties of fast disintegrating tablets of acetaminophen prepared by super-disintegrant blends and sublimation methods. Two groups of tablets comprising various batches were prepared by wet granulation. Granules batches of one group of tablets (A-G) were prepared with different concentrations of sodium starch glycolate and croscarmellose sodium while the other group of tablets (H-N) were incorporated with varying concentrations of menthol into the batches. The granules were subjected to analysis and compressed into tablets. The post-compression parameters of the tablets such as weight uniformity, crushing strength, friability, wetting and disintegration times, as well as dissolution studies were evaluated. Drug-excipient compatibility studies using Fourier transform infrared (FTIR) analysis was also carried out. Granules were fair to good in flow with Carr’s indices ≤ 20.14 and angles of repose ranging from 21.34 to 35.00°. Tablets crushing strength values were between 3.44 to 8.26 kp while their friability values were < 1.52%. They showed wetting and disintegration times that were ≥ 0.18 and ≥ 0.25 min. Dissolution studies showed that four batches of tablets (two from each method used in formulation) achieved 100% drug release within 30 min. FTIR analysis shows no interactions between acetaminophen and excipients used in formulation. Tablets from both methods were comparable in their tablet properties but the disintegrant blend tablets exhibited superior crushing strengths, hence formed harder tablets, while the sublimation method tablets were superior in their wetting and disintegration times. Keywords: acetaminophen, super-disintegrants, sublimation, tablet parameters