Journal of Phytomedicine doi: 10.3390/jphytomed1020008

Authors: Joshua Kamani Mike Shand Shimon Harrus

This review aims to highlight the rich biodiversity of plants with acaricidal properties in Africa and the potential for harnessing them for the development of eco-friendly acaricides. Terrestrial plant-derived bioactive substances hold huge potential as cost-effective and eco-friendly insecticides that can serve as a suitable alternative to chemical pesticides. Ticks and tick-borne diseases (TTBDs) constitute a serious challenge to animal and human health globally, necessitating the need for effective control measures. However, the use of chemical acaricides, the mainstay of tick control, is no longer sustainable due to the development of multiple acaricide resistance, economic constraints, and environmental and public health concerns, necessitating the exploration of phytochemical acaricides as a viable option. In Africa, the rich plant biodiversity remains largely underexplored and underutilized for TTBDs control. Our bibliographical review identified 144 plant species from 48 families across 27 African countries that have been assessed in various in vitro assays. These studies report that these plant species possess phytochemicals with acaricidal properties, causing over 50% mortality or repellency on various tick developmental stages. Plant species belonging to the Asteraceae (n = 23), Lamiaceae (n = 17) and Fabaceae (n = 11) from several African countries were reported to possess effective anti-tick properties. Bioactive substances and essential oils, such as the tannins, flavonoids, steroids, terpenoids, camphor, camphene, 1,8-cineole (eucalyptol), alpha-pinene and more were the most frequently isolated compounds, attesting to the rich biodiversity of plants possessing phytochemicals with strong prospects for use in tick control. Despite these encouraging findings, none so far has been translated or formulated into an anti-tick product for commercial use. Therefore, we advocate for robust continental and regional collaborations to coordinate the bioprospecting of anti-tick ethnobotanicals, ultimately leading to the development of cost-effective and eco-friendly natural products for tick control.

Journal of Phytomedicine doi: 10.3390/jphytomed1020007

Authors: Fatemeh Naderi Maryam Salami Seyed Hadi Razavi Mona Miran Michael J. Serpe Marleny D. A. Saldaña Raimar Loebenberg Marlon C. Mallillin Shengnan Zhao Neal M. Davies

Many bioactive constituents of medicinal plants depend on microbial biotransformation for their pharmacological activity, positioning postbiotics from plant substrates as microbially matured phytomedicines. An emerging framework integrates prebiotic phytochemicals with probiotic strains to modulate gut microbiota and host health. In this study, we explored the functional properties of heat-inactivated Lactobacillus strains following the fermentation of oligosaccharides obtained from sesame hulls (Sesamum indicum L.), underutilised agro-industrial residues. Cell-wall oligosaccharides were obtained by alkaline or enzymatic (Celluclast® 1.5 L (Novonesis, Copenhagen, Denmark)) extraction with Ultraflo® L (Novonesis, Copenhagen, Denmark) hydrolysis and fermented with Lactobacillus acidophilus, L. casei, or L. paracasei. Heat-inactivated pre-postbiotic preparations were profiled for antioxidant capacity, inhibition of metabolic enzymes implicated in obesity and type 2 diabetes, and anti-Helicobacter pylori urease activity. Moreover, these preparations were incorporated into a barley malt (Hordeum vulgare L.) beverage. Bioactivity was strain- and substrate-dependent: L. casei-derived postbiotics most strongly inhibited pancreatic lipase (47.82%) and α-glucosidase (52.14%); L. acidophilus most strongly inhibited α-amylase (43.67%); and L. paracasei exhibited the strongest urease inhibition (20.66%). All strains displayed enhanced antioxidant activity, with ABTS scavenging reaching 87.02%. The supplemented beverages improved antioxidant activity by ~20%. The fermentation of these oligosaccharides thus yields a microbially matured phytomedicine with multi-target activity, supporting postbiotics as active mediators of plant-based therapeutics.

Journal of Phytomedicine doi: 10.3390/jphytomed1010006

Authors: Michail Panagiotidis

Plant-based bio-actives exert a chemical complexity characterized by a plurality of health-promoting and/or disease-preventing properties [...]

Journal of Phytomedicine doi: 10.3390/jphytomed1010005

Authors: Papy M. Moke Salvius A. Bakari Julie Carette Vianney N. Ntabaza Cedrick S. Mutombo Pierre Duez Amandine Nachtergael Joh B. Kahumba

The Aristolochia genus contains aristolochic acids (AAs), nephrotoxic and carcinogenic compounds found in many species. Although the use of Aristolochia has been restricted worldwide due to safety concerns, no information is currently available on the species occurring in the flora of the Democratic Republic of the Congo (DRC). This lack of information regarding occurrence, use, and chemical composition of Aristolochia species limits the evaluation of potential exposure risks associated with traditional medicinal practices. This study identified Aristolochia species reported in the DRC through a bibliographic survey and assessed the presence of AAs in A. heppii, a species native to Katanga. Microscopic examination of root powders and HPLC-DAD/MS analysis of hydroalcoholic and aqueous extracts were performed according to the European Pharmacopoeia on one authenticated sample and twelve commercial samples purchased in Lubumbashi. Microscopy confirmed diagnostic features consistent with Aristolochia. Mass spectrometry analysis identified AAs, with AA-I quantified in hydroalcoholic extracts at 566 ± 5 ppm to 3533 ± 32 ppm (0.057–0.353% w/w) and in the aqueous extract at 204.2 ± 0.4 ppm (0.020% w/w). These results demonstrate that traditional preparations of A. heppii may lead to exposure to AA-I and underline the need for risk assessment and regulatory oversight.

Journal of Phytomedicine doi: 10.3390/jphytomed1010004

Authors: Dongmin Yu Jonghyun Park Taeho Kim Chanju Choi Simseok A. Yuk Hyungjun Kim

Phytochemicals have attracted considerable attention as therapeutically relevant bioactive compounds due to their diverse pharmacological activities, including anti-inflammatory, antioxidant, anticancer, and metabolic regulatory effects. However, their clinical translation is frequently hindered by unfavorable pharmaceutical properties such as poor aqueous solubility, chemical instability, rapid metabolism, and limited bioavailability. These challenges have constrained the reproducibility and therapeutic reliability of phytochemical-based interventions. In this context, nanotechnology-enabled delivery systems have emerged as effective strategies to overcome the intrinsic limitations of phytochemicals and enhance their biological performance. This review provides a comprehensive overview of recent advances in nanotechnology-based delivery platforms for phytochemicals, with emphasis on lipid-based nanocarriers, polymeric nanoparticles, nanoemulsions and self-nanoemulsifying drug delivery systems, inorganic and hybrid nanocarriers, as well as hydrogel-based and transdermal delivery systems. We discuss how rational nanocarrier design improves solubility, stability, pharmacokinetics, cellular uptake, and tissue targeting, thereby enhancing therapeutic efficacy across multiple disease areas. In addition, critical safety, toxicity, manufacturing, and regulatory considerations that influence translational potential are addressed. By adopting a delivery-centered perspective, this review highlights current challenges and future opportunities in nano-phytomedicine and underscores the importance of integrating nanotechnology, biological insight, and regulatory-conscious development to advance phytochemicals toward clinically viable therapeutic applications.

Journal of Phytomedicine doi: 10.3390/jphytomed1010003

Authors: Tahere Razzaghi Sara Hasanvand Seyed-Behnam Ghaffari Mona Miran Marlon C. Mallillin Shengnan Zhao Masoud Homapour Michael J. Serpe Raimar Loebenberg Maryam Salami Neal M. Davies

Pomegranate (Punica granatum L.) is a potent source of bioactive compounds with antioxidant and anti-inflammatory properties, offering therapeutic potential against cancer, Alzheimer’s disease, hypertension, diabetes, hepatic disorders, and obesity. This review highlights the capacity of pomegranate leaves, flowers, arils, juice, seeds, and peel to modulate or inhibit key enzymes involved in inflammatory, metabolic, neurodegenerative, cardiovascular, hepatic, and melanogenic pathways. Additionally, pomegranate enhances endogenous antioxidant defenses (CAT, SOD, GPx, GR, and GST) and regulates caspase activity, further contributing to its health-promoting effects. While preclinical evidence underscores its multifaceted enzymatic and therapeutic benefits, positioning pomegranate as a promising natural adjunct for the prevention and management of enzyme-related diseases, further research is needed to elucidate mechanisms and validate clinical efficacy.

Journal of Phytomedicine doi: 10.3390/jphytomed1010002

Authors: Md Harunur Rashid Matthew J. Williams Andres Garcia Guerra Arunporn Itharat Raimar Loebenberg Neal M. Davies

Kratom (Mitragyna speciosa (Korth.) Havil.) oxindole alkaloids remain underexplored compared to the well-studied indole constituents mitragynine and 7-hydroxymitragynine. Previous research has primarily focused on phytochemical identification and preliminary pharmacology, with limited pharmacokinetic insight. This study pioneers an in silico ADMET modeling analysis of 27 kratom-derived oxindole alkaloids using ADMET Predictor™ v3.0, delivering the first comprehensive predictions of their physicochemical properties, CYP450/UGT enzyme interactions, transporter affinities, permeability, and pharmacokinetic parameters. Representative compounds such as speciophylline, isomitraphylline, and isospeciophylline displayed notably favorable predicted jejunal permeability and moderate metabolic stability, suggesting promising oral drug-like characteristics. Across the dataset, high CYP3A4 substrate affinity (98% confidence), variable CYP3A4, CYP2D6, CYP2C19 inhibition, strong P-gp substrate potential, and differential BBB penetration probabilities (46–99%) were observed. These findings provide a foundational computational framework to guide future experimental validation and rational drug development of kratom oxindole alkaloids.

Journal of Phytomedicine doi: 10.3390/jphytomed1010001

Authors: Md Harunur Rashid Matthew J. Williams Andres Garcia Guerra Arunporn Itharat Raimar Loebenberg Neal M. Davies

Kratom alkaloids are classified as aromatic pentacyclic indole and substituted carbonyl oxindole alkaloids. This study investigates the metabolism and interactions of indole alkaloids using in silico tools, including ADMET Predictor 13.0™, to assess pharmacokinetic and metabolic profiles. The analysis examined absorption, distribution, metabolism, and excretion (ADME), focusing on cytochrome P450 (CYP) and UDP-glucuronosyltransferase (UGT) enzyme interactions, drug transporters, and clearance. Most indole alkaloids showed strong substrate interaction and inhibition of CYP3A4 (79–99% confidence) and induction of CYP1A2 (up to 94% confidence). Among UGT enzymes, UGT1A1 demonstrated the highest substrate affinity (97%), while none interacted with UGT2B15. All alkaloids showed strong P-glycoprotein (Pgp) interaction but minimal inhibition of BCRP. Mitralactonine exhibited the highest skin permeability, and Mitralactonal showed maximal jejunal permeability. Most indole alkaloids demonstrated significant blood–brain barrier penetration (up to 99% confidence) and compliance with Lipinski’s rule of five. Predictive modeling indicated notable effects on hepatic microsomal clearance parameters. This investigation offers the first comprehensive in silico ADMET profiling of kratom indole alkaloids, uncovering their CYP3A4 inhibition potential and metabolic liabilities to prioritize candidates for safer therapeutic development, though limited by model biases, applicability domain restrictions, and inability to fully capture biological complexity, stereochemistry, or interindividual variability necessitating experimental in vitro and in vivo validation.