In vitro assessment of deworming potential of Guiera senegalensis in Nigerian ethnoveterinary industry using Caenorhabditis elegans

Background Although Guiera senegalensis is used as a dewormer in ethnoveterinary health care in Nigeria, its anthelmintic potential has not been validated. Hence, this work investigated the in vitro anthelmintic potential of G. senegalensis extracts on two Caenorhabditis elegans strains: Bristol N2 (wild type/ivermectin susceptible) and DA1316 (ivermectin resistant). Results Aqueous and methanol extracts of G. senegalensis were tested against the motility of the L4 larvae at two exposure periods of 24 and 48 h and found to be active against the C. elegans strains. Motility of C. elegans DA1316 was reduced to 18.6% and 8.3% by aqueous and methanol extracts, respectively, at 2.0 mg/ml after 48 h, whereas that of C. elegans DA1316 treated with ivermectin (0.02 µg/ml) remained above 95%. The motility of C. elegans Bristol N2 was reduced to 16.6% and 7.2% by aqueous and methanol extracts, respectively, at 2.0 mg/ml after 48 h and ≤ 2.7% by ivermectin (0.02 µg/ml). Activity of the plant extracts was concentration and time dependent. Conclusions This work confirms the anthelmintic activity of G. senegalensis and its effectiveness against ivermectin-resistant nematodes, thus validating its ethnoveterinary use as an animal dewormer in Nigeria and pharmacological potential as a source of anthelmintic compounds against ivermectin-resistant nematodes. There is, however, the need for in vivo studies to confirm the in vitro efficacy of the extracts.

Antimicrobial activities of certain seaweeds from muddy shore places of kerala

A study was carried out to reveal the growth inhibitory effect of methanol crude extract (MCE) and methanol supernatant extract (MSE) of sea weeds: 1) Gracillaria corticata, 2) Hypnea musciforms, 3) Gelidium micropterum and 4) Hypnea valentiae against six bacterial pathogens, 1) Pseudomonas aeruginosa, 2) Bacillus licheniformis, 3) Serratia marcescens, 4) Aeromonas hydrophila, 5) Acinetobacter baumanii, 6) Escherichia coli and two fungal strains, 1) Aspergillus niger and 2) Candida albicans respectively. Well diffusion method using zone of inhibition as indicator for growth inhibition was adopted. The results showed that methanol extracts of seaweeds viz., Gracillaria corticata, Hypnea musciforms, and Hypnea valentiae prevented the growth of pathogenic bacteria and fungi. The effect on growth was observed as zone of inhibition, the diameter of which was indicated in the units of a millimeter. The growth of the bacterium, Serratia marcescens was affected by methanol supernatant extract of the three types of seaweeds, Gracillaria corticata, Hypnea musciforms, and Hypnea valentiae, and by the methanolic crude extract of Hypnea musciforms and Hypnea valentiae. However, the growths of other species of bacteria were not controlled by either of the extracts of the seaweeds except, Bacillus licheniformis which was controlled by only Gracillaria corticata. The growth of fungi: Aspergillus niger and Candida albicans were inhibited by the methanol extracts of Gracillaria corticata. Between the two forms of methanolic extracts i.e., supernatant and crude, the efficiency of the supernatant extract was greater than that of crude one. Further, among the three types of seaweeds which showed an effect on the growth of microbes, the level of the zone of inhibition caused by Gracillaria corticata was statistically higher than that of the other two, Hypnea musciforms, and Hypnea valentiae.

In vivo and in silico Evaluation of Analgesic and Hypoglycemic Activities of Roots of Acacia nilotica, Azadirachta indica and Justica adhatoda

The present study focuses on the investigation of methanol extracts of roots of three indigenous plants of Bangladesh namely Acacia nilotica, Azadirachta indica and Justicia adhatoda to evaluate their analgesic and hypoglycemic activities in experimental animal model along with in silico modelling of several compounds present in the root extracts of these plants. Analgesic and hypoglycemic activities were evaluated in Swiss albino mice using acetic acid-induced writhing inhibition method and glucose tolerance test, respectively. In silico molecular docking and ADME study was conducted to assess the binding affinity with the target receptors and oral bioavailability of the compounds. The methanol extracts of A. nilotica, J. adhatoda and A. indica roots at a dose of 400 mg/kg body weight reduced the number of writhes by 61.53%, 54.61% and 47.69%, respectively compared to standard diclofenac sodium (70.77% at a dose of 50 mg/kg bw) (p<0.05). A. nilotica and A. indica root extracts showed significant hypoglycemic activity at a dose of 400 mg/kg bw (% reduction of blood glucose 43.66 and 37.55% respectively, p<0.001) and J. adhatoda root extract reduced the blood glucose level by 33.71% (p<0.001) compared to that of standard drug, glibenclamide (57.46% reduction of blood glucose) after 120 minutes of administration. Among the computationally tested compounds, flavan-3-ol showed the lowest binding energy (-8.7 kcal/mol) with both COX-1 and COX-2 compared to standard diclofenac sodium (-7.8 kcal/mol). On the other hand, quercetin demonstrated the lowest binding energy (-8.8 kcal/mol) with ATP-sensitive potassium channel with Sulfonylurea Receptor 1 subunit among the tested compounds compared to standard glibenclamide (-9.3 kcal/mol). All the compounds showed high oral bioavailability in ADME analysis. Among all the root extracts, A. nilotica exhibited the most promising analgesic and hypoglycemic activities and should be employed to future investigation for isolating specific chemical constituents. Dhaka Univ. J. Pharm. Sci. 20(2): 185-197, 2021 (December)

Antibaterial activity of the extracts of pineapple and pomelo against five different pathogenic bacterial isolates

To combat the infections caused by antibiotic resistant bacteria, natural candidates are being studied to find out antibacterial activity against the drug-resistant microorganisms. Among the variety of natural candidates of plant origin, many fruits have been proved to have potent antibacterial activity. In the current study, we chose pineapple (Ananas comosus), and pomelo (Citrus maxima) to determine their efficacy against some clinical isolates. Fruit samples were subjected to prepare crude, ethanol, methanol and aqueous extract to determine their antibacterial potency. Clinical isolates were used to determine the antibacterial activity of the extracts against them. The isolates were found to be multi-drug resistant. Out of twenty-eight antibiotics, Pseudomonas aeruginosa was resistant to ten antibiotics and Salmonella spp. was resistant to nine antibiotics. Rather than the crude extracts of the fruits, ethanol and methanol extracts showed antibacterial activity towards multi-drug resistant pathogenic bacteria. Aqueous extract did not show any significant antibacterial activity at all. Extracts of pomelo fruit exhibited the highest results whereas pomelo skin and pineapple peel crude extracts were the least effective compared to the other extracts. Ethanol extract of pineapple fruit (against all isolates but Staphylococcus aureus) and methanol extract of pomelo fruit (against all isolates) showed the lowest MIC (minimum inhibitory concentration) of 187.5 μg/ml. MBC (minimum bactericidal concentration) was found (within the range of 500 μg/ml to 1000 μg/ml) only with ethanol and methanol extracts of pomelo and pineapple. As the clinical isolates were found to be inhibited by the extracts, they can be used as an alternative for treating infections caused by these bacteria. Stamford Journal of Microbiology, Vol.11 (1) 2021: 1-6

Antioxidant Potential, Phenolics Content and Antimicrobial Attributes of Selected Medicinal Plant

The bioactive extracts recovered from Curcuma longa (stem), Mentha aquatica (stem and leaves), Emblica officinalis (fruits), Nigella sativa (seeds), and Glycyrrhiza glabra (stem) using methanol and ethanol, were appraised for antioxidant (total flavonoid contents, total phenolic contents, DPPH free radical scavenging ability, inhibition of linoleic acid peroxidation and reducing power) and antimicrobial attributes. Total phenolics (16.89 ± 0.18 - 25.06 ± 0.31g GAE/100g) and total flavonoids (1.96 ± 0.07 - 13.54 ± 0.18 CE g/100g) contents of aqueous methanol extracts of tested plant materials were significantly (p < 0.05) lower than that of aqueous ethanol extracts (13.87 ± 0.12 - 28.63 ± 0.34 g GAE/100g) and (2.20 ± 0.10 - 8.71 ± 0.24 CE /100g), respectively. The percent inhibition of linoleic acid per oxidation by crude ethanol extracts of plants was in the range of 48.72 ± 1.24 - 70.79 ± 1.57 and crude methanol extract 35.90 ± 1.28 - 61.54 ± 2.14, while the range of DPPH free radical scavenging activity of ethanol extracts was (58.36 ± 1.98 - 80.55 ± 3.07) and methanol extracts (39.55 ± 1.52 - 79.64± 2.33). The reducing power of the tested extracts obtained by ethanol (at the concentration of 10 mg/mL) ranged 1.11 ± 0.12 – 1.53 ± 0.18 while for methanol extracts 0.98 ± 0.11 – 1.39 ± 0.12. Among the attributes analyzed, total phenolics, total flavonoids, and DPPH free scavenging activity were found to be varied significantly in all the tested medicinal plants. The extracts from all plants showed good antimicrobial potential against a penal of bacteria, including E. coli, P. multocida and S. aureus, and fungi including A. niger, A. flavus, A. alternate, and G. lucidium. Overall, the tested samples were found to be a good source of natural antioxidant and antimicrobial agents and thus can be explored for potential functional food and nutra-pharmaceutical applications.

Evaluation of Nigerian Medicinal Plants Extract on Human P-glycoprotein and Cytochrome P450 Enzyme Induction: Implications for Herb-Drug Interaction

Background: Herbal medicine represents a significant component of disease prevention and therapy in most African countries. Herb-drug interactions (HDI) can arise from the co-administration of herbal and orthodox medicines. Objective: This study assessed the potential for HDI of V. amygdalina, O. gratissimum, M. oleifera, A. indica, and P. nitida extracts using in vitro assays. Little is known about these medicinal plants' potential for drug interaction despite their extensive use in Nigeria for several disease conditions. Method: The medicinal plant crude extracts were evaluated for Cytochrome P450 (CYP) enzyme induction using cryopreserved human hepatocytes. Enzyme activity was determined by quantifying probe substrate metabolism and metabolite formation using liquid chromatography-mass spectrometry/mass spectrometry. The extracts were evaluated for the potential to inhibit P-glycoprotein (P-gp) activity using human embryonic kidney membrane vesicles over-expressing human P-gp. The herbal extracts in vivo drug interaction potential was predicted based on the USFDA drug interaction guidance. Result: O. gratissimum and P. nitida methanol extracts induced CYP1A2 enzyme activity by greater than 3-fold. P. nitida methanol extracts showed over 2-fold induction of CYP1A2 mRNA expression. O. gratissimum methanol extract induced CYP2B6 mRNA expression over 2-fold. P. nitida and A. indica methanol extracts showed potent inhibition of P-gp activity (IC50: 3.8 and 5.4 µg/mL), respectively, while V. amygdalina and M. oleifera methanol extracts showed moderate P-gp inhibition (IC50: 12.1 and 37.2 µg/mL, respectively). Conclusion: Our studies suggested that the medicinal plants’ extracts can modulate CYP enzymes and P-gp activity with the potential to cause herb-drug interaction in vivo.

Exploring the Biotechnological Value of Marine Invertebrates: A Closer Look at the Biochemical and Antioxidant Properties of Sabella spallanzanii and Microcosmus squamiger

Sabella spallanzanii and Microcosmus squamiger were profiled for proximate composition, minerals, amino acids, fatty acids (FA), carotenoids, radical scavenging activity on the 2,2-diphenyl-1- picrylhydrazyl (DPPH) radical, oxygen radical absorbance capacity (ORAC) and iron and copper chelating properties. Microcosmus squamiger had the highest level of moisture and crude protein, S. spallanzanii was enriched in crude fat and ash. Both species had similar levels of carbohydrates and energy. There was a prevalence of arginine and glycine in S. spallanzanii, and of taurine in M. squamiger. The most abundant minerals in both species were Na, Ca, and K. The methanol extract of S. spallanzanii had metal chelating properties towards copper and iron, while the methanol extract of M. squamiger was able to chelate copper. M. squamiger extracts had similar ORAC values. Fucoxanthinol and fucoxanthin were the major carotenoids in the M. squamiger dichloromethane extract. Saturated FA were more abundant than unsaturated ones in methanol extracts, and unsaturated FA prevailed in the dichloromethane extracts. Palmitic acid was the predominant FA in methanol extracts, whereas eicosapentaenoic (EPA) and dihomo-γ-linolenic acids were the major compounds in dichloromethane extracts. Low n-6/n-3 ratios were obtained. Our results suggests that both species could be explored as sources of bioactive ingredients with multiple applications.

Preliminary Phytochemical Screening, In Vitro Antidiabetic, Antioxidant Activities, and Toxicity of Leaf Extracts of Psychotria malayana Jack

Psychotria malayana Jack belongs to the Rubiacea and is widespread in Southeast Asian countries. It is traditionally used to treat diabetes. Despite its potential medicinal use, scientific proof of this pharmacological action and the toxic effect of this plant are still lacking. Hence, this study aimed to investigate the in vitro antidiabetic and antioxidant activities, toxicity, and preliminary phytochemical screening of P. malayana leaf extracts by gas chromatography-mass spectrometry (GC-MS) after derivatization. The antidiabetic activities of different extracts of this plant were investigated through alpha-glucosidase inhibitory (AGI) and 2-NBDG glucose uptake using 3T3-L1 cell line assays, while the antioxidant activity was evaluated using DPPH and FRAP assays. Its toxicological effect was investigated using the zebrafish embryo/larvae (Danio rerio) model. The mortality, hatchability, tail-detachment, yolk size, eye size, beat per minute (BPM), and body length were taken into account to observe the teratogenicity in all zebrafish embryos exposed to methanol extract. The LC50 was determined using probit analysis. The methanol extract showed the AGI activity (IC50 = 2.71 ± 0.11 μg/mL), insulin-sensitizing activity (at a concentration of 5 µg/mL), and potent antioxidant activities (IC50 = 10.85 μg/mL and 72.53 mg AAE/g for DPPH and FRAP activity, respectively). Similarly, the water extract exhibited AGI activity (IC50 = 6.75 μg/mL), insulin-sensitizing activity at the concentration of 10 μg/mL, and antioxidant activities (IC50 = 27.12 and 33.71 μg/mL for DPPH and FRAP activity, respectively). The methanol and water extracts exhibited the LC50 value higher than their therapeutic concentration, i.e., 37.50 and 252.45 µg/mL, respectively. These results indicate that both water and methanol extracts are safe and potentially an antidiabetic agent, but the former is preferable since its therapeutic index (LC50/therapeutic concentration) is much higher than for methanol extracts. Analysis using GC-MS on derivatized methanol and water extracts of P. malayana leaves detected partial information on some constituents including palmitic acid, 1,3,5-benzenetriol, 1-monopalmitin, beta-tocopherol, 24-epicampesterol, alpha-tocopherol, and stigmast-5-ene, that could be a potential target to further investigate the antidiabetic properties of the plant. Nevertheless, isolation and identification of the bioactive compounds are required to confirm their antidiabetic activity and toxicity.