This is the first review on the new subclass of N , C -coupled NIQs, their isolation and structural elucidation, their N , C -axial chirality, their biosynthetic origin, their promising antiparasitic and antileukemia activities, and their total synthesis.
Ethnobotanical surveys indicate that the Masai and Kikuyu in Kenya, the Venda in South Africa, and the Gumuz people of Ethiopia use Pappea capensis for the treatment of malaria. The present study aimed to investigate the phytochemical and antiplasmodial properties of the plant leaves. The bioactive compounds were isolated using chromatographic techniques. The structures were established using NMR, HRMS, and UV spectroscopy. Antiplasmodial activity of P. capensis leaf extract and isolated compounds against chloroquine-sensitive 3D7 P. falciparum was evaluated using the parasite lactate dehydrogenase assay. Cytotoxicity against HeLa (human cervix adenocarcinoma) cells was determined using the resazurin assay. The extract inhibited the viability of Plasmodium falciparum by more than 80% at 50 µg/mL, but it was also cytotoxic against HeLa cells at the same concentration. Chromatographic purification of the extract led to the isolation of four flavonoid glycosides and epicatechin. The compounds displayed a similar activity pattern with the extract against P. falciparum and HeLa cells. The results from this study suggest that the widespread use of P. capensis in traditional medicine for the treatment of malaria might have some merits. However, more selectivity studies are needed to determine whether the leaf extract is cytotoxic against noncancerous cells.
The first reported investigation into the phytochemical constituents of Commiphora pedunculata led to the isolation of two flavonoids: kaempferol and dihydrokaempferol from the ethyl acetate-soluble fraction of the methanol extract of the stem bark of the plant. The structures of these compounds were characterised by comparing their spectral data including 1D and 2D NMR with those reported in the literature. The two compounds were active against 6 out of 10 tested microorganisms including two resistant strains [methiciline-resistant Staphylococcus aureus and vancomycin-resistant entrococci (VRE)], Candida albicans and Escherichia coli. The zones of inhibition ranged between 24 and 30 mm for both compounds against the microorganisms. The MIC value was as low as 6.25 μg/mL against VRE and Staphylococcus aureus. This is the first report of the isolation of these compounds from the plant.
Vachellia xanthophloea is used in Zulu traditional medicine as an antimalarial remedy. A moderate antiplasmodial activity was previously reported for extracts of the plant against D10 Plasmodium falciparum. This study aimed to identify the phytochemicals responsible for the antiplasmodial activity of the leaf extract. The compounds were isolated by chromatography and their structures were determined using spectroscopic and spectrometric methods. The antiplasmodial activity was evaluated using a parasite lactate dehydrogenase assay and cytotoxicity was determined using a resazurin assay. The ethyl acetate fraction inhibited P. falciparum with IC50 = 10.6 µg/mL and showed minimal cytotoxicity (98% cell viability at 33 µg/mL). The chromatographic purification of this fraction afforded sixteen compounds, including two new flavonoids. A 1:1 mixture of phytol and lupeol was also isolated from the hexane fraction. All the compounds were reported from V. xanthophloea for the first time. Among the isolated metabolites, methyl gallate displayed the best activity against P. falciparum (IC50 = 1.2 µg/mL), with a 68% viability of HeLa cells at 10 µg/mL. Therefore, methyl gallate was responsible for the antiplasmodial activity of the V. xanthophloea leaf extract and its presence in the leaf extract might account for the folkloric use of the plant as an antimalarial remedy.
Diabetes mellitus (DM) is a chronic metabolic disease with a high global prevalence. Lignans, a class of plant natural compounds found in commonly consumed foods, are well-tolerated by humans and have demonstrated promising potential in the management of DM. Consumption of lignan-rich foods has been associated with improved overall health and quality of life. The clinical and preclinical evidence on the role of lignans in managing DM are critically examined. A thorough literature search was conducted across major scientific databases, focusing on studies that reported the effects of individual lignans on key diabetes indicators, such as glucose utilisation and insulin sensitivity, in both human and animal models, as well as in cell-based studies. A total of 180 lignans were included in the review. Out of these, only three were investigated in randomised clinical trials in humans and 31 in animal models. The reviewed evidence suggests some beneficial effects of lignans in preventing the development of obesity-related diabetes. Their therapeutic benefits in preventing diabetes-related complications, particularly diabetic nephropathy, in both type 1 and type 2 diabetes, are also supported. Metabolites of various lignans, produced by microbial metabolism in the gut and serum enzymes, appear to be key bioactive forms, highlighting the need for detailed pharmacodynamic studies, optimised dosage designs, and the use of the appropriate lignan molecules for cell-based screening. Lignans and their microbial metabolites show promise in preventing obesity-related diabetes and mitigating diabetes-related complications such as diabetic nephropathy, though further clinical studies are needed to optimize their therapeutic potential.