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Ethnopharmacological relevance Many species within the family Combretaceae are popular medicinal plants that are used traditionally to treat various conditions, of which many are related to bacterial infections. Global concerns regarding the increasing resistance of pathogens towards currently available antibiotics have encouraged researchers to find new drugs with antibacterial activity, particularly from plant sources. Aim of the study This study was aimed at exploring the broad-spectrum antibacterial potential of methanol extracts of species representing four genera of Combretaceae (Combretum, Pteleopsis, Quisqualis, Terminalia), indigenous to South Africa, using a biochemometric approach. Materials and methods The microdilution assay was used to determine the antibacterial activities, measured as minimum inhibitory concentrations (MICs), of the 51 methanol extracts representing 35 Combretaceae species, against nine species of pathogenic bacteria. Integrative biochemometric analysis was performed, thereby correlating the MIC values with the metabolomic data obtained from ultra-performance liquid chromatography-mass spectrometry (UPLC-MS) analysis. Orthogonal projections to latent structures-discriminant analysis (OPLS-DA) models were constructed for six pathogens displaying variation in their susceptibility towards the extracts. Results Evaluation of the overall MIC values obtained indicated that extracts of species from the four genera displayed the highest activity towards Bacillus cereus ATCC 11778 (average MIC 0.52 mg/mL) and Salmonella typhimurium ATCC 14028 (average MIC 0.63 mg/mL). These bacteria were the most sensitive Gram-positive and Gram-negative bacteria, respectively. Extracts from Combretum acutifolium, Combretum imberbe and Combretum elaeagnoides were the most active, with average MIC values of 0.70 mg/mL, 0.52 mg/mL and 0.45 mg/mL, respectively. Five triterpenoid compounds were tentatively identified as biomarkers from the biochemometric analysis. Conclusion Correlation of the phytochemistry of species from four genera in the Combretaceae family with antibacterial activity revealed that triterpenoids are responsible for the broad-spectrum antibacterial activity observed.

Ethnopharmacological relevance Khat, the leaves of Catha edulis, is used as a “natural amphetamine-like” stimulant in eastern and southern Africa, as well as in the Arabian Peninsula. Leaves are masticated to elicit a state of euphoria. Although the psychostimulatory effects of the leaves are attributed to the presence of phenylpropylamino alkaloids ( i.e. cathinone, cathine and norephedrine), the extent of permeation of these alkaloids across the oral and intestinal mucosa has not been established. Materials and methods Cathinone was isolated in the form of the oxalate salt from young buds, following acid-base extraction. High performance countercurrent chromatography (HPCCC) was used to isolate cathine and norephedrine, following borohydride reduction of a mixture of the three alkaloids. The in vitro permeability of these three alkaloids in their pure form, as well as in a crude extract, was evaluated across Caco-2 cell monolayers and across excised porcine intestinal, sublingual and buccal tissues. Results The purities of the isolated cathine and norephedrine were in excess of 90%, thereby proving that HPCCC can be applied for efficient separation of these alkaloids from extracts of Khat. The apparent permeability (P app ) coefficients for the Khat alkaloids in their pure form were all above 1.0×10 −6 cm/s, indicating that the transport of the three alkaloids across the selected biological membranes is comparable to that of the highly permeable reference compound, caffeine. Although readily transported across the various membranes, the alkaloids were transported to a lesser extent when present in a leaf extract, suggesting that other phytochemicals present in the extract influence their permeation. Conclusions These results provide evidence that chewing of Khat contributes to the buccal and sublingual absorption of the psychoactive alkaloids in the bloodstream directly across the oral mucosal membranes. In addition, it confirms that these metabolites will be readily absorbed from the gastrointestinal tract when swallowed.

Ethnopharmacological relevance The use of Lawsonia inermis L. (henna) for medicinal and cosmetic purposes is inextricably linked to ancient and modern cultures of North Africa and Asia. Literature and artwork indicates that Lawsonia inermis played an important holistic role in the daily lives of some ancient cultures, providing psychological and medicinal benefits, as well as being used for personal adornment. Although henna was historically applied to the hands and feet to protect against fungal pathogens and to hair to combat lice and dandruff, other traditional uses include the treatment of liver and digestive disorders, reduction of tissue loss in leprosy, diabetic foot disorders and ulcers. Phytochemistry: Almost 70 phenolic compounds have been isolated from various parts of the plant. Naphthaquinones, which include the dyeing principle lawsone, have been linked to many of the pharmacological activities. The terpene, β-ionone is largely responsible for the pungent odour of the essential oil isolated from the flowers. In addition to other volatile terpenes, some non-volatile terpenoids, a single sterol, two alkaloids and two dioxin derivatives have also been isolated from the plant. Bioactivity: Henna is a pharmacologically important plant with significant in vitro and in vivo biological activities. Although a myriad of pharmacological activities have been documented, the antioxidant and antimicrobial activities are the most thoroughly investigated. Some incidents of adverse reactions following application to the skin have been reported, but these are mainly confined to cases involving individuals with glucose-6-phosphate dehydrogenase deficiency and reactions to adulterants added to henna products. Conclusions: Adulteration of henna is very common and may have resulted in unwarranted scientific findings. Phytochemical profiling studies of the plant, which are crucial for the establishment of proper quality control protocols, are lacking and hamper the development of medicinal products. Although many in vitro studies have been conducted to evaluate the pharmacological activities and many in vivo studies have focussed on the toxicity of extracts, more in vivo studies to validate pharmacological activities are needed. The roles of specific compounds and their synergies have not been comprehensively investigated.