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AbstractThree undescribed pregnane steroids, 12β‐O‐4‐hydroxybenzoyl tenacigenin D (1), 12β‐O‐4‐hydroxybenzoyl tenacigenin A (2), and 11α‐nicotinoyl‐17β‐marsdenin (3), along with two known analogues (4 and 5), were isolated from the roots of Marsdenia tenacissima. Their structures were elucidated using one‐ and two‐dimensional NMR, high‐resolution electron ionization‐mass spectrometry, single‐crystal X‐ray diffraction data, and experimental and density‐functional‐theory‐calculated electronic circular dichroism measurements. All isolated compounds were evaluated for their cytotoxic activities against human lung cancer cells (A549), ovarian carcinoma cells (SKOV‐3), gastric cancer cells (MGC 803) and breast cancer cells (MCF‐7). Notably, 3 exhibited significant cytotoxic activity against both A549 (median inhibitory concentration (IC50)=16.79 μM) and SKOV‐3 (IC50=12.30 μM) cells while exhibiting moderate cytotoxicity on MGC803 and MCF‐7 cells.

01 Oct 2024·Journal of Ethnopharmacology

Efficacy and mechanism of action of Yanxiao Di'naer formula for non-alcoholic steatohepatitis treatment based on metabolomics and RNA sequencing

Article

Author: Yin, Qiang ; Zheng, Dong-Xuan ; Xue, Tao-Tao ; Hou, Qiang ; Wang, Zhi ; Wen, Li-Mei ; Geng, Ruo-Yu ; Gao, Xiang ; Yin, Hai-Long ; Hu, Jun-Ping ; Yang, Jian-Hua

ETHNOPHARMACOLOGICAL RELEVANCENonalcoholic fatty liver disease (NAFLD) is the most prevalent chronic liver disease worldwide. Nonalcoholic steatohepatitis (NASH) is a crucial component of this disease spectrum. The Yanxiao Di'naer formula (YXDNE) is an Uyghur medical extract that has been used in folk medicine to treat hepatitis for a long time. However, the role and mechanism of action of YXDNE in NASH treatment remains unclear.OBJECTIVEThe objective of this study was to assess the effectiveness of YXDNE in treating NASH induced by injections of carbon tetrachloride combined with a high-fat high-cholesterol diet (HFHCD), and to clarify the underlying mechanisms.METHODSThe compounds in the YXDNE extract were analysed for classification and proportions using ultra-performance liquid chromatography-mass spectrometry. The efficacy of YXDNE in treating abnormal lipid metabolism was evaluated in L02 cells in vitro. In addition, a C57BL/6 mouse model of NASH was established to evaluate the therapeutic efficacy of YXDNE in vivo. Metabolomics and RNA sequencing were used to analyse the therapeutic effects of YXDNE on the liver. The corresponding signalling pathways were found to target AMPKα1, PPARα, and NF-κB. The efficacy of YXDNE was validated using inhibitors or silencing RNA (siRNA) against AMPKα1 and PPARα.RESULTSThis study confirmed that YXDNE treatment ameliorated NASH in a murine model of this disease. Metabolomics analysis suggested that YXDNE efficacy was associated with fatty acid catabolism and AMPK signalling pathways. RNA sequencing results showed that YXDNE efficacy in treating NASH was highly correlated with the AMPK, PPARα and NF-κB pathways. Both in vitro and in vivo experimental data demonstrated that YXDNE affected the expression of p-AMPKα1, PPARα, p-NF-κB, IκB, and p-IκB. The efficacy of YXDNE in treating NASH in vitro was cancelled when AMPK was inhibited with Compound C or PPARα was modulated via siRNA.CONCLUSIONSYXDNE may have a therapeutic effect on abnormal lipid metabolism in L02 cells and in a murine model of NASH by affecting the AMPKα1/PPARα/NF-κB signalling pathway. Therefore, YXDNE has the potential for clinical application in the prevention and treatment of NASH.

01 Sep 2023·Phytochemistry

C21 steroids from the roots of Marsdenia tenacissima

Article

Author: Mu, Dan-Dan ; Xu, Hong-Tao ; Chou, Gui-Xin ; Du, Ting-Ting ; Wei, Xiao-Hui ; Liu, Jin-Ling ; Han, Xiao ; Wang, Yong-Li

A phytochemical investigation of the dichloromethane soluble fraction of the ethanolic extract obtained from the roots of Marsdenia tenacissima led to the discovery of the sixteen undescribed pregnane C₂₁ steroids (1-16) and isolation of eleven known C₂₁ steroidal analogues (17-27). Their chemical structures were elucidated by one- and two-dimensional nuclear magnetic resonance spectroscopy and, high resolution-electrospray ionization mass spectrometry and their absolute configurations were determined using electronic circular dichroism or single-crystal X-ray diffraction. The in vitro anti-proliferative effects of 1-16 were evaluated against HepG2 (human hepatocellular cancer), A549 (lung cancer), and MCF-7 (human breast cancer) cell lines. Even though some of them showed moderate cytotoxic activities, marsectohexol derivative 12 exhibited significant cytotoxicity against A549 cells with an IC₅₀ value of 5.2 μM.

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Pipeline Snapshot as of 10 May 2025

The statistics for drugs in the Pipeline is the current organization and its subsidiaries are counted as organizations,Early Phase 1 is incorporated into Phase 1, Phase 1/2 is incorporated into phase 2, and phase 2/3 is incorporated into phase 3

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Current Projects

Drug(Targets)	Indications	Global Highest Phase

Wenwei Ayaranji Tablets	Decrease in appetite More	Phase 3
Qubai Bairesi Tincture	Vitiligo More	Phase 2
Flos gossypii flavonoids tablet	Alzheimer Disease More	Phase 2
Xing Qi Tan Ni Ka Er Capsule	Constipation - functional More	Phase 2
Tongzhi Surunjiang Tablets	Arthritis, Gouty More	Pending