Constituents from the Roots of Actinidia chinensis and Their Cytochrome P450 Enzyme Inhibitory Activities

Abstract

A newly discovered triterpenoid, (2α,3β)-2,3,23-trihydroxyurs-13(18)-en-28-oic acid (1), along with twelve known compounds (2 - 13), were isolated from the roots of Actinidia chinensis Planch (Actinidiaceae). Their chemical structures were determined by 1D- and 2D-NMR spectra and mass spectrometry (MS). The crude extracts and six main constituents (8 - 13) were tested for cytochrome P450 (CYPs) enzyme inhibitory activity. The results showed that, except for compound 8, compounds 9 - 13 had different inhibitory effects on the cytochrome P450 (CYPs) enzyme, and compound 9 significantly inhibited the catalytic activities of CYP3A4 to < 10% of its control activities.

Actinidia chinensis Planch.: A Review of Chemistry and Pharmacology

“…Table 2 lists the nutritional composition of sun-gold kiwifruit reported from the USDA Food Composition Database (United States Department of Agriculture, USDA Food Composition Databases, 2018). Table 3 shows the chemical content of A. chinensis fruit (Chang and Case, 2005; Cui et al, 2007; Zhou et al, 2009; Xu et al, 2010; He et al, 2014; He et al, 2015a; He et al, 2015b; Xu et al, 2016; Twidle et al, 2018; Sivakumaran et al, 2018; Wei et al, 2018; Zhang et al, 2018). Of particular note, nutritional composition in kiwifruit is vitamin C (1.61 mg/g) and minerals K (3.15 mg/g).…”

“…The 90% EtOH extract of A. chinensis root at 50 μg/ml exhibited inhibition activities on CYP2C9, CYP2D6, and CYP3A4 in human liver tissue with the 69.0, 76.3, and 53.3% of remaining activity, respectively. The inhibitory effect of the crude extract could be largely attributed to the presence of triterpenoids (Xu et al, 2016). It is worth noting that the combination of crude extracts or these triterpenoids with other medical herbs or drugs may lead to drug interaction with cytochrome CYPs at pharmacokinetic and pharmacodynamic levels, which indicates that people should cautiously consume A. chinensis fruit when taken medicine.…”

Salvisertin A, a New Hexacyclic Triterpenoid, and Other Bioactive Terpenes from Salvia deserta Root

“…In addition, if the H-C(24) is α -oriented, the chemical shift of the Me(23) group is generally lower than 18 ppm and C(24) is present at about δ (C) 68 ppm; while if H-C(24) is β -oriented, the chemical shift of the Me(23) group is usually higher than 20 ppm and C(24) is present at around δ (C) 64 ppm. These differences occur because the equatorial hydroxymethylene is less shielded than its axial counterpart [6][7] . The chemical shifts of the C(23) and C(24) in 1 were 24.2 ppm and 65.7 ppm, respectively, indicating that H-C(23) was α -oriented, whereby H-C(24) was β -oriented.…”

Cytotoxic Triterpenoids from Roots of Actinidia chinensis

“…The roots of this plant, called Tengligen usually, were used as the traditional Chinese medicine for the treatment of various cancers, such as esophagus cancer, liver cancer, and gastric cancer . Phytochemical investigation of roots of the plant showed triterpenoids,– flavanoids, phenolic acids, and steroids were isolated before . Pentacyclic triterpenoids, especially 12‐en‐28‐oic acids of ursane‐ or oleanane‐type as common constituents of roots of the plant have exibited antitumor activity in vitro – .…”