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Cloning and analysis of 1-hydroxy-2-methyl-2-(E)-butenyl-4-diphosphate reductase genes HsHDR1 and HsHDR2 in Huperzia serrate

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Acta Pharmaceutica Sinica B 2015年第6期5卷 583-589页

作者： Haizhou Lv Xin Zhang Baosheng Liao Wanjing Liu Liu He Jingyuan Song Chao Sun Hongmei Luo Shilin Chen institute of medicinal Plant Development Chinese Academy of Medical Sciences & Peking Union Medical College institute of Chinese materia Medica China Academy of Chinese Medicinal Sciences

We cloned and analyzed the two genes of the 1-hydroxy-2-methyl-2-(E)-butenyl-4-diphosphate reductase(HDR) gene family from Huperzia *** two transcripts coding HDR,named Hs HDR1 and Hs HDR2,were discovered in the transcriptome dataset of *** and were cloned by reverse transcription-polymerase chain reaction(RT-PCR).The physicochemical properties,protein domains,protein secondary structure,and 3D structure of the putative Hs HDR1 and Hs HDR2 proteins were *** full-length c DNA of the Hs HDR1 gene contained 1431 bp encoding a putative protein with 476 amino acids,whereas the Hs HDR2 gene contained 1428 bp encoding a putative protein of 475 amino *** two proteins contained the conserved domain of 1-hydroxy-2-methyl-2-(E)-butenyl-4-diphosphate reductase(PF02401),but without the transmembrane region and signal *** most abundant expression of Hs HDR1 and Hs HDR2 was detected in *** roots,followed by the stems and *** results provide a foundation for exploring the function of Hs HDR1 and Hs HDR2 in terpenoid and sterol biosynthesis in Huperziaceae plants.

关键词： 1-Hydroxy-2-methyl-2(E)-butenyl-4-diphosphate reductase Huperzia serrate Terpenoid Gene clone Bioinformatics analysis

Synthesis of 1,7-dimethoxy-2-hydroxyxanthone,a natural product with potential activity on erectile dysfunction

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Chinese Chemical Letters 2013年第6期24卷 515-517页

作者： Wen-Jing Liu De-Sheng Mei Wen-Hu Duan School of Pharmacy East China University of Science and Technology Department of medicinal Chemistry Shanghai Institute of Materia Medica.Chinese Academy of Sciences Department of medicinal Chemistry Shanghai Institute of Materia MedicaChinese Academy of Sciences

The natural product,1,7-dimethoxy-2-hydroxyxanthone（1）,isolated from Securidaca inappendiculate Hassk,has a potential in the treatment of erectile dysfunction due to its significant relaxation activity on rabbit Corpus ***,the isolation of compound 1 is problematic because of its high similarity in structure to its *** this paper,the first synthesis of 1 was reported featuring two key reactions：a copper-catalyzed coupling reaction and an intramolecular cyclization.

关键词： 1 7-Dimethoxy-2-hydroxyxanthone Erectile dysfunction Synthesis Copper-catalyzed coupling reaction

Identification of a dual functional betulinic acid analog for the treatment of osteoarthritis by phenotypic screening

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Science China Life Sciences 2025年第1期 300-302页

作者： Ze-Min Lin Mai Xiang Wen-Hui Wei Shu-Hui Fan Li Chen Jie Wang Xiao-Qian Yang Chun-Hao Yang Shi-Jun He Jian-Ping Zuo Laboratory of Immunopharmacology State Key Laboratory of Drug ResearchShanghai Institute of Materia MedicaChinese Academy of Sciences School of Pharmacy University of Chinese Academy of Sciences School of Pharmacy Nanjing University of Chinese Medicine State Key Laboratory of Drug Research Department of Medicinal ChemistryShanghai Institute of Materia MedicaChinese Academy of Sciences Innovation Research institute of Traditional Chinese Medicine Shanghai University of Traditional Chinese Medicine Experiment Center for Science and Technology Shanghai University of Traditional Chinese Medicine

Dear Editor, Phenotypic drug discovery, which observes compound effects on physiology,has given way to targeting specific molecules, but has revived by using modern methods to find drugs based on therapeutic outcomes in disease models(Vincent et al., 2022). Osteoarthritis(OA) is a prevalent chronic joint disorder, primarily affecting knee joints, with osteoclast activation due to low-grade inflammation resulting in increased bone resorption and structural changes in the joint(Katz et al.,2021).

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A New Flavone from the Roots of Uvaria macrophylla

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Chinese Chemical Letters 2001年第9期12卷 791-792页

作者： Hai Ling ZHANG Ruo Yun CHEN institute of materia Medica Chinese Academy of Medicinal Sciences&Peking Union Medical CollegeBeijing 100050

A New flavone named Macrophyllol was isolated from the roots of Uvaria macrophylla. The structure of 1 was elucidated on the basis of spectroscopic evidence.

关键词： Uvaria macrophylla flavone Macrophyllol

Two New Diterpenes from Helianthus annuus L.

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Chinese Chemical Letters 2006年第1期17卷 45-48页

作者： Mao Rong SUO Jun Shan YANG Yang LU Li WU Qi Tai ZHENG institute of medicinal Plant Development Chinese Academy of Medical Sciences ＆ Peking Union Medical College Beijing 100094 institute of medicinal materia Chinese Academy of Medical Sciences ＆ Peking Union Medical College Beijing 100050

Two new diterpenes, 2β, 16β-ent-kaurane diol, 15α, 16α-epoxy-17β-al-ent-kaurane- 19-oic acid were isolated from Helianthus annuus L. Their structures were determined by spectroscopic evidences.

关键词： Helianthus annuus diterpene.

Synthesis of Mono- and Di-fluorinated Benzimidazoles

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Chinese Journal of Chemistry 2011年第5期29卷 983-990页

作者：梁武刘刚 Department of Synthetic medicinal Chemistry Institute of Materia Medica Chinese Academy of Medical Sciences & Peking Union Medical College Beijing 100050 China

Three efficient methods to synthesize mono- and di-fluorinated benzimidazoles are reported. These methods provide 5-amino-6-fluoro-benzimidazoles （5）, 5,7-difluoro-benzimidazoles （10）, and 6-fluoro-benzimidazoles （13） starting from commercially available 1,5-difluoro-2,4-dinitrobenzene （DFDNB）, 2,3,4,5-tetrafluoro-6-nitrobenzoic acid （TFNBA）, and 2,4-difluoro-l-nitrobenzene （DFNB）, respectively.

关键词： fluorine benzimidazoles fluorinated benzimidazoles synthesis design

Simultaneous inhibition of PI3Kα and CDK4/6 synergistically suppresses KRAS-mutated non-small cell lung cancer

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Cancer Biology & Medicine 2019年第1期16卷 66-78页

作者： Yuxiang Wang Xian Li Xueling Liu Yi Chen Chunhao Yang Cun Tan Bobo Wang Yiming Sun Xi Zhang Yinglei Gao Jian Ding Linghua Meng Division of Anti-Tumor Pharmacology Shanghai Institute of Materia Medica Chinese Academy of Sciences University of Chinese Academy of Sciences Division of Anti-Tumor Pharmacology State Key Laboratory of Drug Research Shanghai Institute of Materia Medica Chinese Academy of Sciences Department of medicinal Chemistry Shanghai Institute of Materia Medica Chinese Academy of Sciences

Objective: Activating KRAS mutations are the most common drivers in the development of non-small cell lung cancer(NSCLC).However, unsuccess of treatment by direct inhibition of KRAS has been proven. Deregulation of PI3K signaling plays an important role in tumorigenesis and drug resistance in NSCLC. The activity of PI3Kα-selective inhibition against KRAS-mutated NSCLC remains largely ***: Cell proliferation was detected by sulforhodamine B assay. Cell cycle distribution and apoptosis were measured by flow cytometry. Cell signaling was assessed by Western blot and immunohistochemistry. RNA interference was used to down-regulate the expression of cyclin D1. Human NSCLC xenografts were employed to detect therapeutic efficacy in ***: CYH33 possessed variable activity against a panel of KRAS-mutated NSCLC cell lines. Although CYH33 blocked AKT phosphorylation in all tested cells, Rb phosphorylation decreased in CYH33-sensitive, but not in CYH33-resistant cells, which was consistent with G1 phase arrest in sensitive cells. Combined treatment with the CDK4/6 inhibitor, PD0332991, and CYH33 displayed synergistic activity against the proliferation of both CYH33-sensitive and CYH33-resistant cells, which was accompanied by enhanced G1-phase arrest. Moreover, down-regulation of cyclin D1 sensitized NSCLC cells to CYH33. Reciprocally, CYH33 abrogated the PD0332991-induced up-regulation of cyclin D1 and phosphorylation of AKT in A549 cells. Co-treatment with these two drugs demonstrated synergistic activity against A549 and H23 xenografts, with enhanced inhibition of Rb ***: Simultaneous inhibition of PI3Kα and CDK4/6 displayed synergistic activity against KRAS-mutated NSCLC. These data provide a mechanistic rationale for the combination of a PI3Kα inhibitor and a CDK4/6 inhibitor for the treatment of KRASmutated NSCLC.

关键词： PI3Kα CDK4/6 KRAS NSCLC CYH33

Safety issues and new rapid detection methods in traditional Chinese medicinal materials

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Acta Pharmaceutica Sinica B 2015年第1期5卷 38-46页

作者： Lili Wang Weijun Kong Meihua Yang Jianping Han Shilin Chen institute of medicinal Plant Development Chinese Academy of Medical Sciences & Peking Union Medical College institute of Chinese materia Medica China Academy of Chinese Medical Sciences

The safety of traditional Chinese medicine(TCM) is a major strategic issue that involves human health. With the continuous improvement in disease prevention and treatment, the export of TCM and its related products has increased dramatically in China. However, the frequent safety issues of Chinese medicine have become the ‘bottleneck' impeding the modernization of TCM. It was proved that mycotoxins seriously affect TCM safety; the pesticide residues of TCM are a key problem in TCM international trade; adulterants have also been detected, which is related to market circulation. These three factors have greatly affected TCM safety. In this study, fast, highly effective, economically-feasible and accurate detection methods concerning TCM safety issues were reviewed, especially on the authenticity, mycotoxins and pesticide residues of medicinal materials.

关键词： Traditional Chinese medicine Safety issue Rapid detection Mycotoxins Pesticide residues Authentication 2D DNA barcodes Traceability

Tetrahydroisoquinolines as novel histone deacetylase inhibitors for treatment of cancer

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Acta Pharmaceutica Sinica B 2016年第1期6卷 93-99页

作者： Danqi Chen Aijun Shen Guanghua Fang Hongchun Liu Minmin Zhang Shuai Tang Bing Xiong Lanping Ma Meiyu Geng Jingkang Shen Department of medicinal Chemistry State Key Laboratory of Drug ResearchShanghai Institute of Materia MedicaChinese Academy of Science Division of Anti-tumor Pharmacology State Key Laboratory of Drug ResearchShanghai Institute of Materia MedicaChinese Academy of Sciences

Histone acetylation is a critical process in the regulation of chromatin structure and gene *** deacetylases(HDACs)remove the acetyl group,leading to chromatin condensation and transcriptional *** inhibitors are considered a new class of anticancer agents and have been shown to alter gene transcription and exert antitumor *** paper describes our work on the structural determination and structure-activity relationship(SAR)optimization of tetrahydroisoquinoline compounds as HDAC *** compounds were tested for their ability to inhibit HDAC 1,3,6 and for their ability to inhibit the proliferation of a panel of cancer cell *** these,compound 82 showed the greatest inhibitory activity toward HDAC 1,3,6 and strongly inhibited growth of the cancer cell lines,with results clearly superior to those of the reference compound,vorinostat(SAHA).Compound 82 increased the acetylation of histones H3,H4 and tubulin in a concentration-dependent manner,suggesting that it is a broad inhibitor of HDACs.

关键词： Histone deacetylases inhibitor Anticancer Tetrahydroisoquinoline Structure–activity relationship