Developing an activity and absorption-based quality control platform for Chinese traditional medicine: Application to Zeng-Sheng-Ping(Antitumor B)

Abstract

Ethnopharmacological relevance Zeng-Sheng-Ping (ZSP) is a marketed Chinese traditional medicine used for cancer prevention. Aim of the study Currently, for the quality control of Chinese traditional medicines, marker compounds are not selected based on bioactivities and pharmaceutical behaviors in most of the cases. Therefore, even if the “quality” of the medicine is controlled, the pharmacological effect could still be inconsistent. The aim of this study is to establish an activity and absorption-based platform to select marker compound(s) for the quality control of Chinese traditional medicines. Materials and methods We used ZSP as a reference Chinese traditional medicine to establish the platform. Activity guided fractionation approach was used to purify the major components from ZSP. NMR and MS spectra were used to elucidate the structure of the isolated compounds. MTT assay against oral carcinoma cell line (SCC2095) was performed to evaluate the activities. UPLC-MS/MS was used to quantify the pure compounds in ZSP and the active fraction. The permeabilities of the identified compounds were evaluated in the Caco-2 cell culture model. The intracellular accumulation of the isolated compounds was evaluated in the SCC2095 cells. Results The major compounds were identified from ZSP. The contents, anti-proliferation activities, permeabilities, and intracellular accumulations of these compounds were also evaluated. The structure of these purified compounds were identified by comparing the NMR and MS data with those of references as rutaevine (1), limonin (2) , evodol (3), obacunone (4), fraxinellone (5), dictamnine (6), maackiain (7), trifolirhizin (8), and matrine (9). The IC50 of compounds 5, 6, and 7 against SCC2095 cells were significantly lower than that of ZSP. The uptake permeability of compounds 5, 6, and 7 were 2.58 ± 0. 3 × 10−5, 4.33 ± 0.5 × 10−5, and 4.27 ± 0.8 × 10−5 respectively in the Caco-2 cell culture model. The intracellular concentrations of these compounds showed that compounds 5, 6, and 7 were significantly accumulated inside the cells. Conclusion Based on the activity against oral carcinoma cell line as well as the absorption permeability, compound 5, 6, and 7 are selected as quality control markers for ZSP. A activity and absorption-based platform was established and successfully used for the quality control of ZSP.

Understanding the Effectiveness of Natural Compound Mixtures in Cancer through Their Molecular Mode of Action

“…Zhou et al also showed that it was able to inhibit the growth of human ovarian A2780 and lung H23 cancer cells in vitro. The compound also has anti-proliferative activity in oral carcinoma SCC2095 cells [62]. A combination of trifolirhizin together with maackiain (a constituent of Trifolium pratense ) has been shown to induce apoptosis in human leukemia HL-60cells.…”

Isoflavones: Anti-Inflammatory Benefit and Possible Caveats

“…Numerous epidemiological studies have indicated that vegetarian diets based on fruit and vegetable consumption are beneficial for human health [ 9 , 10 , 11 ], but the involved food components and the underlying mechanisms still remain unclear. Chinese traditional medicine has had a long history of applying crude plant extracts to treat diseases and disorders exemplified by acute and chronic inflammation [ 12 , 13 , 14 ]. Recent investigations have demonstrated that the polyphenols from plant sources, in particular flavonoids, exhibit anti-inflammatory activity both in vitro and in vivo [ 14 , 15 , 16 , 17 ].…”

High‐performance liquid chromatography coupled with tandem mass spectrometry technology in the analysis of Chinese Medicine Formulas: A bibliometric analysis (1997–2015)

“…Besides, the effective ingredients in most TCM are still unknown . It was reported that among the 1203 herbs included in the Chinese Pharmacopoeia (2010 version), only 529 could be regulated by reference compounds . Currently, there are about 500 herbal reference materials are available, but some unstable reference compounds are difficult to be obtained .…”