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Hypoxis hemerocallidea (Hypoxidaece) is thoroughly researched and well documented for its plethora of anecdotal and scientifically backed pharmacological potentials. Its anecdotal uses and pharmacological activities are attributed to its extract’s inherent bioactive compounds like hypoxoside, rooperol, and β-sitosterol. This study aimed at conducting a targeted and holistic phytochemical profiling of variations in Hypoxis hemerocallidea (H. hemerocallidea) and related species. The chemotaxonomic classifications of H. hemerocallidea and seven other related species were also carried out to avert the possibility of over harvesting H. hemerocallidea and the encouragement of species inter-change. The plant extracts were analysed with reverse phase ultra-pure liquid chromatography quadrupole time-of-flight mass spectrometry and gas chromatography, as well as high-performance thin-layer chromatography. The generated chromatographic data were made compatible for chemometric computation using Principal Component Analysis (PCA) and Orthogonal Partial Least Squares Discriminant Analysis (OPLS-DA) models. The results obtained unveil orcinol glycoside, curculigoside C, hypoxoside, dehydroxyhypoxoside, bisdehydroxy hypoxoside, hemerocalloside, galpinoside, cholchicoside, geraniol glycoside, β-sitosterol, oleic acid, and 2-hydroxyethyl linoleate as target phytochemicals that define the profiles of the Hypoxis species. In addition, three distinct chemotypes defined by hemerocalloside, galpinoside, and colchicoside, respectively, were observed, as well as holistic variations in all secondary metabolites. Due to similarities in the phytochemical constituents of selected species, species inter-change seems imminent if further research confirms the findings of this study. Full article

Pharmacokinetic and metabolism studies were carried out on curculigoside C (CC), a natural product with good antioxidant and neuroprotective effects, with the purpose of investigating the effects of the hydroxyl group at C-3′ in curculigoside. A rapid and sensitive method with UPLC-MS was developed and fully validated for the first time in the pharmacokinetic analysis for quantification of CC in rat plasma. The assay was linear (R² > 0.9984) over the concentration range of 1–2500 ng/mL, with the lower limit of quantification (LLOQ) being 1 ng/mL. The intra-day and inter-day precision (expressed as relative standard deviation, RSD) ranged from 4.10% to 5.51% and 5.24% to 6.81%, respectively. The accuracy (relative error, RE) ranged from −3.28% to 0.56% and −5.83% to −1.44%, respectively. The recoveries ranged from 92.14% to 95.22%. This method was then applied to a pharmacokinetic study of rats after intragastric administration of 15, 30 and 60 mg/kg CC. The results revealed that CC exhibited rapid oral absorption (T_max = 0.106 h, 0.111 h, and 0.111 h, respectively), high elimination (t_1/2 = 2.022 h, 2.061 h, and 2.048 h, respectively) and low absolute bioavailability (2.01, 2.13, and 2.39%, respectively). Furthermore, an investigation on the metabolism of CC was performed by UPLC-QTOF-MS^E. Twelve metabolites of CC from plasma, bile, urine and faeces of rats were confirmed. The main metabolic pathways of CC, which involve dehydration, glucosylation, desaturation, formylation, cysteine conjugation, demethylation and sulfonation, were profiled. In conclusion, this research has developed a sensitive quantitative method and demonstrated the metabolism of CC in vivo. Full article