Potential Cytotoxicity, Pharmacokinetics, and Excretion Properties of Sapindoside B from the Seeds of Nigella sativa var. hispidula

Abstract

The seeds of Nigella sativa var. hispidula are widely used in food preparation by the Uighur people in western China. Recently, series of oleanane triterpenoid saponins were extracted from the seeds of Nigella sativa var. hispidula, especially α-hederin as representative that exhibited strong antitumor activity. Compared to α-hederin, sapindoside B has just 1 more terminal xylopyranose in the 3-O position and displays similar effects against various human cancer cell lines with cisplatin. Considering this potential cytotoxic activity, a reliable LC-MS/MS method was developed to quantify sapindoside B in rat plasma, urine, and feces. Chromatographic separation was conducted on an Agilent Zorbax SB-Aq (3.0 × 150 mm, 3.5 µm) column via an isocratic elution procedure with acetonitrile and water containing 0.1% formic acid. Mass spectrometric detection was coupled with an electrospray ionization source in the MRM mode. The linear range of calibration curves was 15 ~ 3000 ng/mL in plasma/urine and 30 ~ 3000 ng/g in feces. The intra-day and inter-day precision was less than 11.1%, and accuracy ranged from 92.2% to 108.7%. The proposed method was validated and shown to be reliable, precise, and accurate and was successfully applied to its pharmacokinetics and excretion studies. Sapindoside B exhibited dosage-dependent pharmacokinetics in the range of 2.5 mg/kg to 12.5 mg/kg, and only about 2% of intravenous dose of sapindoside B was excreted by the feces and urine in its unchanged form over 48 h. These results provide further data support for evaluating the druggability of sapindoside B.

Nigella A ameliorates experimental colitis via interacting with gut microbiota on dextran sulphate sodium (DSS)-induced C57BL/6 mice

“…For example, N. glandulifera and TSN were con rmed to exhibit signi cant antioxidant and anti-in ammatory properties (Zhao et al 2013;Zheng et al 2020). Triterpene saponins are the dominant group of anti-in ammatory compounds existed in this ethnomedicinal plant (Hu et al 2014;Hu et al 2020) and Nigella A was a major ingredient of triterpene saponins extracted from N. glandulifera. Nigella A was 60.36 ± 1.25 g/100 g total saponins of N. glandulifera (Zhao et al 2013).…”

“…The content of Nigella A was 60.36 ± 1.25 g/100 g existed in TSN (Zhao et al 2013). Our previous results revealed that saponins were the principal active components of N. glandulifera with the highest content (64.5%) and Nigella A (also named Sieboldianoside A) is a major oleanane triterpenoid saponin isolated from N. glandulifera (Hu et al 2020;Zheng et al 2020). We speculated that it could be used to treat a variety of in ammation-related diseases by regulating ora and immune.…”

“…The seeds of Nigella glandulifera Freyn et Sint (N. glandulifera), which were known as black cumin (black seeds) and were widely used as a traditional medicine for the treatment of numerous in ammatory diseases (Zheng et al 2020; Hu et al 2020). N. glandulifera seed powder, extracts (ethanolic, volatile oil, total avonoids, and total saponins, etc.…”

“…Although the anti-in ammatory activity of N. glandulifera and its main constitutes have gained a great deal of attention in recent years, no research has been conducted on its anti-colitis activity. In our previous study, a large amount of Nigella A was extracted and puri ed from the seeds of N. glandulifera (Hu et al 2014;Hu et al 2020). Due to these healthcare functions, it is worthwhile to explore the therapeutical effect of Nigella A, a main active triterpene saponin extracted from N. glandulifera, on UC.…”

Purified Tea (Camellia sinensis (L.) Kuntze) Flower Saponins Induce the p53-Dependent Intrinsic Apoptosis of Cisplatin-Resistant Ovarian Cancer Cells

“…As many saponins exhibit pharmacological properties, a review of the absorption, disposition, and pharmacokinetics of saponins had been done [79]. Recently, the pharmacokinetics and excretion studies of sapindoside B in rat were conducted and reported the pharmacokinetic profiles of sapindoside B in the range of 2.5 to 12.5 mg/kg dosage-dependently, and only 2% intravenous dose of sapindoside B was excreted in its parent form over 48 h [80]. More research is needed to explain the contradiction between the low bioavailability of saponins and their potential anticancer activity in vivo.…”