Abdul K. Jaleel, Sapna Jacob, Suresh Mohan Ghosh, Amritesh Suresh

The Banana (Musa paradisiaca Linn., Family: Musaceae) is one of the oldest and most widely cultivated fruit plants, dating back to prehistoric times. Bananas are rich in minerals and phytochemicals, contributing to their significant culinary, nutritional, and medicinal properties. This review analyzes 191 peer-reviewed articles published between 1981 and July 2023 to comprehensively assess the health benefits of bananas. Studies highlight their effectiveness in reducing inflammation, cancer, diabetes, depression, diarrhea, urolithiasis, and ulcers. Additionally, bananas exhibit antibacterial, antiviral, antihyperlipidemic, antiatherosclerotic, hepatoprotective, hair-growing, wound-healing, and antihypertensive properties. The articles were sourced from databases such as PubMed, Scopus, and Google Scholar using keywords like Musa paradisiaca, health benefits, inflammation, cancer, diabetes, and phytochemicals. Inclusion criteria included original research, clinical trials, in vitro and in vivo studies, and reviews focused on banana’s medicinal properties, while non-peer-reviewed papers and studies not directly related to Musa paradisiaca were excluded. This review reinforces the comprehensive health-promoting benefits of bananas and sets the stage for future research, which should focus on large-scale clinical trials, phytochemical standardization, and sustainable utilization of banana plant components. Bananas hold immense potential as both a functional food and a medicinal plant, making them a promising subject for future studies in nutraceuticals and sustainable agriculture.

Sciences of Phytochemistry

Dauda Garba, Bila Hassan Ali, Bashar Bawa, Abdulrazaq Sanusi, Yahaya Mohammed Sani, Muhammad Garba Magaji, Musa Isma’il Abdullahi, Aliyu Muhammad Musa, Hassan Halimatu Sadiya

The development of parasite resistance to first-line antimalarial medicines, especially the Artemisinin-based combination therapies (ACTs), has made the research and development of novel antimalarial medications vital. Globimetula oreophila, a plant used in traditional medicine to treat malaria, is a natural product that may provide new antimalarial drugs with fewer side effects, greater efficacy and lower risk of resistance than synthetic drugs. This study aims to evaluate the antiplasmodial properties of G. oreophila's fractions. The plant leaves were air-dried and reduced in size using a pestle and mortar. The pulverized plant was macerated in 70% ethanol and fractionated with solvent in increasing polarity of n-hexane, chloroform, ethyl acetate, and n-butanol to produce the various fractions. The antiplasmodial activity of the n-hexane, chloroform, ethyl acetate, and n-butanol fractions of G. oreophila leaf extract was assessed using an in vivo method in Plasmodium berghei-infected mice via prophylactic, suppressive, and curative test. The fractions' median lethal dose (LD50) was estimated to be greater than 5000 mg/kg in mice. The median effective dose (ED50) of the fractions at doses of 125, 250, and 500 mg/kg produced a significant (p<0.001) decrease in the level of parasitemia. The ethyl acetate fraction had the best antiplasmodium activity compared to other plant fractions. The fractions of G. oreophila showed significant in vivo antiplasmodial activity, which upholds the earlier in vivo findings for the crude extract and its folkloric use. Further study should be carried out to isolate active secondary metabolites responsible for this observed antimalarial activity in all four investigated fractions.

Sciences of Phytochemistry

Samukelisiwe Nhlapho, Musawenkosi Hope Lotriet Nyathi, Brendeline Linah Ngwenya, Thabile Dube, Arnesh Telukdarie, Inderasan Munien, Andre Vermeulen, Uche A. K Chude-Okonkwo

In the field of pharmaceutical research, identifying promising pharmaceutical compounds is a critical challenge. The observance of Lipinski's Rule of Five (RO5) is a fundamental criterion, but evaluating many compounds manually requires significant resources and time. However, the integration of computational techniques in drug discovery in its early stages has significantly transformed the pharmaceutical industry, enabling further efficient screening and selection of possible drug candidates. Therefore, this study explores RO5 using algorithms of Machine Learning (ML), offering a comprehensive method to predict the druggability of pharmaceutical compounds. The study developed, evaluated, and validated the performance metrics of multiple supervised machine learning models. The best model was used to build an application that can predict and classify potential drug candidates. The findings revealed promising capabilities across all models for drug classification. Among all the explored models, Random Forest (RF), Extreme Gradient Boost (XGBoost), and Decision Tree (DT) classifiers demonstrated exceptional performance, achieving near-perfect accuracy of 99.94%, 99.81% and 99.87% respectively. This highlights the robustness of ensemble learning methods in classifying compounds based on RO5 adherence. The comparative analysis of these models underscores the importance of considering balanced accuracy, precision, F1-score, recall, and Receiver Operating Characteristics-Area Under the Curve (ROC-AUC) score, interpretability, and computational efficiency when choosing between ML algorithms in drug discovery. The DrugCheckMaster application was subsequently developed using the most predictive model and is now available on Render (https://capstone-project-dc7w.onrender.com/).

Sciences of Pharmacy

Mubarak Muhammad Dahiru, James Danga, Abdulhasib Oluwatobi Oni, Hesper Alex Zoaka, Rejoice Daniel Peter, Usanye Zira, Patience Christopher, Hauwa Yahaya Alkasim, Muhammad Zainab

The present study explored the phytoconstituents and radical scavenging activity of the respective n-hexane and aqueous fractions of Cucurbita maxima (CMHF and CMAF) and Leptadenia hastata (LHHF and LHAF) for potential application in oxidative stress-related ailments. The phytoconstituents were qualitatively determined and characterized using Fourier-transform Infrared (FTIR), while the antioxidant activity was determined in vitro. Alkaloids were present in only the aqueous fractions of C. maxima and L. hastata, while saponins, steroids, and flavonoids were detected in all the fractions. The FTIR revealed the presence of functional groups, including alcohols, sulfonates, alkenes, alkanes, amines, and aromatics in both plant fractions. The LHHF (35.53 ±2.11 ascorbic acid (AA) equivalent µg/mL) exhibited a significantly (p<0.05) higher total reducing power (TRP) than all the other fractions. The CMHF (69.11 ±2.56 AAE µg/mL) demonstrated a significantly (p<0.05) higher total antioxidant capacity (TAC) than all the other fractions. For the ferric thiocyanate (FTC) assay, the highest inhibition was exhibited by LHHF (79.78 ± 3.24%), significantly (p<0.05) higher than AA (26.46 ± 2.12%), CMHF (69.77 ± 3.16%), and CMAF (43.80 ± 2.12%). In the thiobarbituric acid assay, the lowest MDA concentration was exhibited by the CMHF (0.07 ±0.01 nmol/mL), significantly (p<0.05) lower than all the other fractions and ascorbic acid. Conclusively, the n-hexane fraction of both plants presents potential sources of novel antioxidant compounds with significant free radical scavenging and anti-lipid peroxidation activities, applicable in ailments linked to oxidative stress.

Sciences of Pharmacy

Mohamed Said Rajab

Spodoptera frugiperda is an invasive pest causing significant crop losses worldwide. Resistance development and health and environmental concerns associated with synthetic insecticides have prompted a search for eco-friendly biopesticides. Limonoids such as salannin, volkensin, and volkensinone, isolated from the East African plant Melia volkensii, show antifeedant activity against S. frugiperda larvae. Volkensin had an ED50 of 3.5 µg/cm², volkensinone (a lactone of volkensin) an ED50 of 6 µg/cm², and salannin an ED50 of 13 µg/cm². Additional limonoids from M. volkensii, including salanninolide and toosendanin, also displayed strong antifeedant effects. With toosendanin already used commercially, a re-evaluation of M. volkensii antifeedant compounds was conducted using in silico techniques. Docking simulations with 3D models of these limonoids and the S. frugiperda ryanodine receptor protein revealed binding affinities from -6.4 to -7.5 kcal/mol, comparable to those of chlorantraniliprole, a commercial insecticide targeting ryanodine receptors. These binding affinities at two distinct receptor sites align well with in-vitro antifeedant activity, underscoring M. volkensii’s potential for environmentally friendly, receptor-targeted biopesticide development against S. frugiperda.

Sciences of Phytochemistry

Aisosa Prince Erhabor, Osayawe Pride Erhabor

Azadirachta indica (neem) and Vernonia amygdalina (bitter leaf) are among the most promising medicinal plants, valued for their broad spectrum of biological activities, including antibacterial, antifungal, anti-inflammatory, antiviral, antidiabetic, and antitumor properties. These plants play a central role in traditional Nigerian medicine for treating tropical diseases such as malaria, typhoid fever, yellow fever, and scabies. This study employed gravimetric analysis to identify and quantify the phytochemical compounds in both plants. Fresh leaves were collected, cleaned, air-dried, and their aqueous extracts were screened for key phytochemical constituents. The analysis revealed the presence of alkaloids, flavonoids, terpenoids, saponins, tannins, glycosides, and phenolic compounds in both extracts. Quantitative results showed that Azadirachta indica had the highest flavonoid content (13.80%), slightly surpassing Vernonia amygdalina (13.62%). Similarly, terpenoids (13.13%) and alkaloids (10.67%) were more abundant in the neem extract compared to the bitter leaf (8.21% and 9.68%, respectively). Lower percentages of glycosides and saponins were observed, with neem containing higher concentrations of both compounds than the bitter leaf. These findings suggest that both plants are rich sources of bioactive compounds with potential applications in developing antibacterial and antifungal treatments. Further research into the phytochemical properties of these plants may facilitate the discovery of novel drugs to combat tropical diseases while reducing the reliance on synthetic chemicals, thus mitigating environmental degradation.

Sciences of Phytochemistry

Nusrat Jahan Juthy, Gazi Jahirul Islam, Abdullah Zehad, Shaheda Zannah

This research was designed to examine the phytochemicals of Mentha viridis (M. viridis) ethanolic extract and the antidiabetic and antihyperlipidemic activities in alloxan-induced animal models. Diabetes was induced chemically by administering a unit dose of alloxan at 120 mg/kg BW. After alloxan induction, hyperglycemic rats were dealt with ethanolic extract of leaf and whole plant, metformin, and a mixture of leaf extract with metformin and whole plant extract with metformin for two weeks. Ethanolic extract of leaf and whole plant, metformin, and a combination of both leaf and whole plant extract with metformin therapies reduced glucose levels in the blood compared with the diabetic negative control group after two weeks of treatment. However, among the therapies, the ethanolic leaf extract and the combination of whole plant extracts with metformin were found to be the most effective (p<0.05), with reductions of 62.82% and 72.89%, respectively. After diabetes induction, the serum level of TG (triglycerides), TC (total cholesterol), LDL-C (low-density lipoprotein-cholesterol) escalated notably (p<0.05), and HDL-C (high-density lipoprotein-cholesterol) level decreased remarkably (p<0.05) in hyperglycemic rats as opposed to healthy normal rats. Ethanolic leaf extract and a combination of whole plant extract with metformin significantly minimized the elevated extent of TG and LDL-C. They surged HDL-C, but the TC level was reduced by whole plant extract only after two weeks of treatment. The standard procedures were used to identify the phytochemical compounds of the medicinal plant M. viridis. The phytochemical compounds such as alkaloids, resins, tannins, phenols, flavonoids, steroids, and terpenoids appeared in the ethanolic leaf extract of M. viridis. The findings suggest that M. viridis might provide better glycemic control and hypolipidemic effect in diabetic rats when administered alone or combined with oral antidiabetic agents. Incorporating M. viridis extract with metformin in improving hyperglycemic and hyperlipidemic conditions in diabetic rats proves that M. viridis has a synergistic effect, which could enhance the antidiabetic activity of oral hypoglycemic agents.

Sciences of Pharmacy

Ivan Ivanov, Daria Kirillova, Kenes Erimbetov, Denis Shatalov

Polyhexamethylene guanidine (PHMG) is a commonly used disinfectant, but safety concerns have arisen due to poisoning cases. This systematic review assesses the toxicity and safety of PHMG by inhalation, oral administration, skin contact, and ocular contact to determine its potential medical applications and acceptable concentration limits. Searches in PubMed, ScienceDirect, CENTRAL, and CyberLeninka up to January 2024 identified 11 in vitro studies with human cell lines, 28 animal studies, and 10 articles involving patients and healthy volunteers. The review found that inhalation of PHMG leads to pulmonary fibrosis and malignant neoplasms, making aerosol forms unacceptable. PHMG can also affect liver function and have adverse effects on the heart, kidneys, and hematopoietic system. For dermal use, PHMG appears to be safe at concentrations up to 3%, although practical use may limit this to 1% due to potential discomfort. Still, it is important to consider possible sensitization, especially in patients with pre-existing skin conditions. In oral hygiene, 1% PHMG-P has been used safely in periodontal treatment, suggesting its potential in dentistry. For ophthalmic use, concentrations should be carefully monitored. PHMG-P solutions below 0.13% appear to be safe for human corneal epithelium, however lower concentrations still pose a risk of corneal fibrosis, as shown in animal studies. Physicians should prefer lower concentrations and consider alternatives or formulations with reduced toxicity for sensitive applications such as eye drops. Overall, although PHMG and its derivatives show promise in a variety of medical applications, their use should be reasonable, with careful consideration of the associated risks.

Sciences of Pharmacy

Mohamed Said Rajab

Structural features of the triterpenoid skeleton that are necessary for antimycobacterial activity are not well understood. Following the isolation of the triterpenoids ergosterol-5,8-endoperoxide, 6β-hydroxykulactone, 12β-hydroxykulactone, (24R)-24,25-epoxycycloartan-3-one and (3β,24R)-24,25-epoxycycloartan-3-ol, and (3β,24R)-24,25-epoxycycloartan-3-acetate with varying antimycobacterial activity ranging between MIC of 1 µg/ml to128 µg/ml prompted us to study this class of compounds further to shade light on the structural features necessary for their antimycobacterial activity. This in silico study involved docking the triterpenoids on the mycobacterial multi-pharmacophore receptor protein MmpL3. The docking results were compared with the MmpL3 receptor protein co-crystallized TB drug candidate, AU1235, (1-(2-adamantyl)-3-[2,3,4-tris(fluoranyl)phenyl] urea). The virtual screening revealed key structural features in the triterpenoid skeleton, including the C-3 keto and β-hydroxy group on C-3 or C-6, as important for antimycobacterial activity. Also, the decreased binding affinity for compounds 2 and 7 with an acetate group on C-3 were in tandem with those observed in vitro. Toxicity predictions revealed that this class of compounds had no mutagenic effects and displayed favorable pharmacokinetic parameters. The study reveals the potential of the triterpenoid skeleton exemplified by the readily available ergosterol-5,8-endoperoxide as a useful scaffold in searching and developing effective therapeutic lead entities to facilitate anti-tuberculosis drug discovery.

Sciences of Phytochemistry

Desi Nadya Aulena, Shirly Kumala, Syamsudin Abdillah, Deni Rahmat, Fenty Sugiastuti, Indarwati Indarwati, Dwi Fitriyani

Secondary metabolites content in Sida rhombifolia L. (SR) are believed to inhibit the xanthine oxidase (XO) enzyme, which is responsible for converting hypoxanthine and xanthine into uric acid. This study aimed to compare flavonoid levels, XO inhibitory activity, and the reduction of uric acid levels of sidaguri herb, stem, leaves, and root extract both in vitro and in vivo. The research results showed that the highest total flavonoid content in SR was found in the leaves, at 21.29±0.08 mg/QE/g extract. The IC50 values were as follows: roots (EESRR 1096.07±1.07 ppm), stems (EESRS 561.62±7.01 ppm), leaves (EESRL 101.84±0.63 ppm), and herbs (EESRH 104.70±3.50 ppm). EESR can inhibit the XO enzyme and has potential as an anti-hyperuricemia agent. The best total flavonoid content and IC50 values were observed in EESRL, which are 21.29±0.08 mg/QE/g and 101.84±0.63 ppm, respectively. EESRL at a dose of 400 mg/kg BW has the equivalent ability to reduce blood uric acid levels in mice when compared to the positive control group. Based on these findings, it can be concluded that EESRL has significant potential as a natural XO inhibitor and can be considered a promising candidate for the development of anti-hyperuricemia treatments.

Sciences of Pharmacy