Weisheng Feng

Lignanamides with potent antihyperlipidemic activities from the root bark of Lycium chinense

Seven new lignanamides, lyciumamides D-J (1-4 and 9-11), together with nine known analogues (5-8 and 12-16), were isolated from the root bark of Lycium chinense. The structures of the isolated compounds were elucidated on the basis of NMR spectroscopic and HRESIMS data. All isolated compounds were evaluated for antihyperlipidemic activities in HepG2 cells. The primary structure-activity relationships were discussed.

A Metabolomics-Based Strategy for the Mechanism Exploration of Traditional Chinese Medicine: Descurainia sophia Seeds Extract and Fractions as a Case Study

A UPLC-QTOF-MS based metabolomics research was conducted to explore potential biomarkers which would increase our understanding of the model and to assess the integral efficacy of Descurainia sophia seeds extract (DS-A). Additionally, DS-A was split into five fractions in descending order of polarity, which were utilized to illustrate the mechanism together. The 26 identified biomarkers were mainly related to disturbances in phenylalanine, tyrosine, tryptophan, purine, arginine, and proline metabolism. Furthermore, heat map, hierarchical cluster analysis (HCA), and correlation network diagram of biomarkers perturbed by modeling were all conducted. The results of heat map and HCA suggested that fat oil fraction could reverse the abnormal metabolism in the model to some extent; meanwhile the metabolic inhibitory effect produced by the other four fractions helped to relieve cardiac load and compensate the insufficient energy supplement induced by the existing heart and lung injury in model rats. Briefly, the split fractions interfered with the model from different aspects and ultimately constituted the overall effects of extract. In conclusion, the metabolomics method, combined with split fractions of extract, is a powerful approach for illustrating pathologic changes of Chinese medicine syndrome and action mechanisms of traditional Chinese medicine.

Two new phenolic constituents from the root bark of Morus alba L. and their cardioprotective activity

Abstract A new biphenyl-furocoumarin, named morescoumarin A (1), and a new prenylated flavanone, named morflavanone A (2) were isolated from the root bark of Morus alba L., together with four known compounds (3–6). Their structures were determined by extensive spectroscopic analyses and comparison with literature data. The cardioprotective effects of these compounds against doxorubicin-induced cell death were evaluated by MTT method.

Uridine derivatives from the seeds of Lepidium apetalum Willd. and their estrogenic effects

Ten uridine derivatives (lepidiumuridine B-K) were isolated from the seeds of Lepidium apetalum Willd. Lepidiumuridine B-J were previously undescribed compounds, and were structurally characterized using analysis of their NMR and MS data. Lepidiumuridine C, D, I, and J increased cell proliferation and expression of ERα in the MCF-7 cell line. In addition, blockage of ERα completely abolished cell proliferation and expression of ERα in MCF-7 cells, suggesting that the proliferation effects of lepidiumuridine C, D, I, and J were ERα-mediated. The uridine derivatives might belong to undescribed phytoestrogens.

Antihyperlipidemic glycosides from the root bark of Lycium chinense

Abstract Three new glycosides (1–3), together with six known ones (4–9), were isolated from the root bark of Lycium chinense. Their structures were elucidated on the basis of MS and NMR spectroscopic data. Five compounds (3, 5, 6, 8, and 9) exhibited potent antihyperlipidemic activities in HepG2 cells as assessed by Oil Red O staining and significant inhibition of intracellular triglyceride (TG) levels, whereas two compounds (5 and 9) significantly reduced total cholesterol (TC) levels.

Homoisoflavanones with estrogenic activity from the rhizomes of Polygonatum sibiricum

Abstract A new homoisoflavanone, (3R)-5-hydroxy-7-methoxyl-3-(2′-hydroxy-4′- methoxybenzyl)-chroman-4-one (1), together with six known analogs, were isolated from the rhizomes of Polygonatum sibiricum. Their structures were elucidated on the basis of extensive spectroscopic analysis. All compounds were tested for their estrogenic activity using the MCF-7 estrogenresponsive human breast cancer cell lines. At a dose of 0.1 μmol/L, compounds 1–7 exhibited significant proliferative effects on MCF-7 cells compared with E2. The molecular docking study results indicated that the activity of compounds 3, 5, 6, and 7 may be the binding with ERR.

Lepidiumuridine A: A New Natural Uridine Derivative as a Phytoestrogen Isolated from the Seeds of Lepidium apetalum Willd.

There has been great interest in phytoestrogens, which are polyhydric compounds that are derived from plants and have a structure similar to that of the mammalian steroid hormone 17β-estradiol. The present study examined the estrogenic effects of a new natural uridine derivative, lepidiumuridine A (LA), that was isolated from the seeds of Lepidium apetalum. The structure was clarified and determined via analysis of extensive spectroscopic data interpretation. The activity of LA was investigated by measuring the levels of estradiol (E2), luteinizing hormone (LH), follicle stimulating hormone (FSH), and the uterus growth in mice. The proliferation experiment of MCF-7 breast cancer cells was also conducted. Western blot, in-cell western, and antagonist assays with methyl piperidino-pyrazole (MPP) were used for exploring the mechanism of the effects of LA. The results showed that LA elevated the uterine coefficient, the levels of E2, and FSH significantly. In addition, LA significantly elevated ERα expression in the uterus and MCF-7 cells. MPP inhibited the proliferation of LA-stimulated MCF-7 cell and ERα expression in MCF-7 cells. Taken together, LA had an estrogen-like effect, which was mainly mediated by the estrogen receptor ERα.

Two New Biflavonoids from the Roots and Rhizomes of Sinopodophyllum emodi

Two new biflavonoids, sinodiflavonoids A (1) and B (2), were isolated from the roots and rhizomes of Sinopodophyllum emodi. Their structures were established on the basis of extensive spectroscopic evidences (HR-ESI-MS, 1H NMR, 13C NMR, HSQC, HMBC, CD). Their cytotoxic activities were evaluated in comparison with etoposide against four cell lines (MCF-7, HepG2, HeLa, KB). The preliminary structure–activity relationships showed that the simple, nonprenylated, nonmethylated biflavonoid (2) showed higher cytotoxic activities than the corresponding prenylated 3-hydroxymethylated one (1).