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Rapid Microwave Assisted Synthesis and Antiproliferative Evaluation of Novel steroidal Thiazole Derivatives

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Chemical Research in Chinese Universities 2017年第2期33卷 206-212页

作者： HUANG Yanmin ZHAO Dandan LIU Chang GAN Chunfang ZHAN Junyan LIN Qifu SHI Haixin CUI Jianguo College of Chemistry and Material Science Guangxi Teachers Education University Nanning 530001 P. R. China Guangxi Colleges and University Key Laboratory of Beibu Gulf Oil and Natural Gas Resource Effectfve Utffizat~'on Qizhou University Qizhou 535011 P. R. China

Three series of novel steroidal thiazole derivatives were synthesized by microwave assisted one-potreaction from pregnenolone, testosterone and estrone, respectively. Their structures were characterized by IR, NMRand HRMS, and the antiproliferative activities of all the synthesized compounds against human cervical carcinoma（HeLa）, human liver carcinoma（HepG2）, human lung carcinoma（A549）, nasopharyngeal carcinoma（CNE2） andnormal kidney epithelial cells（HEK293T） were screened. Among the compounds, 1-estron-17＇-ylidene-2-[4＇-（p-bromophenyl）-2＇-thiazol]hydrazone（12） displayed distinct antiproliferative activity against all the tested cancercell lines and was almost inactive to normal kidney epithelial cells.

关键词： Microwave assisted synthesis Pregnenolone Testosterone Estrone steroidal thiazole derivative

Antiproliferative and apoptosis-inducing potential of 3β-hydroxy-△5-steroidal congeners purified from the soft coral Dendronephthya putteri

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Journal of Oceanology and Limnology 2019年第4期37卷 1382-1392页

作者： Thilina U. JAYAWARDENA Won Woo LEE I. P. Shanura FERNANDO K. K. Asanka SANJEEWA Lei WANG Tee Gee LEE Young Jin PARK Chang-ik KO You-Jin JEON Department of Marine Life Sciences Jeju National University Jeju 690-756 Republic of Korea Department of Hotel Cooking Nutrition Jeonnam Provincial College Jeollanam-do Republic of Korea Department of Family Medicine College of Medicine Dong-A University Busan 602-715 Republic of Korea Choung Ryong Fisheries Co. Ltd. 7825 Iljudong-ro Namwon-eup Seogwipo-si Jeju-do Republic of Korea

The exploration and identification of antiproliferative phytochemicals have received increased attention in medicinal chemistry. In particular, research focused on the toxicology of marine natural products has increased in recent years. Terpenoids, among many secondary metabolites, have been demonstrated to act as effective anticancer agents. Soft corals, a group of marine invertebrates, produce a variety of terpenoids with biofunctional properties. The current study presents the extraction, purification, and identification of sterol congeners from the soft coral Dendronephthya putteri. The method involves 50% chloroform-methanol extraction, polar column fractionation, and analysis through GC-MSn. Dose-dependent antiproliferative activity was observed within the sterol-rich fraction (DPCMH 2-4), which consisted of 3β-hydroxy-Δ5-steroidal congeners. This fraction inhibited the growth of HL-60 and MCF-7 cells with IC50 values of 25.27±1.43 and 22.81±0.15 μg/mL, respectively. Apoptotic body formation, DNA damage, cell cycle arrest, and apoptotic cell signaling pathway activation were also observed, reinforcing the dose-dependent antiproliferative and apoptosis-inducing activity of 3β-hydroxy-Δ5-steroidal congeners. To our knowledge, this is the first report of anticancer agent identification from the soft coral D. putteri. Based on the observations, these steroidal congeners are promising candidates for the development of anticancer drugs.

关键词： Dendronephthya putteri soft coral antiproliferative agent HL-60 MCF-7 apoptosis steroidal congeners

New steroidal alkaloid and furostanol glycosides isolated from Solanum lyratum with cytotoxicity

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Chinese Journal of Natural Medicines 2018年第7期16卷 499-504页

作者： XU Yun-Ling LV Jia WANG Wei-Fang LIU Yue XU Ya-Juan XU Tun-Hai School of Chinese Pharmacy Beijing University of Traditional Chinese Medicine Key Laboratory of Effective Substances of Traditional Chinese Medicine Jilin Academy of Chinese Medicine Sciences School of Traditional Chinese Medicine Changchun University of Traditional Chinese Medicine

Two previously undescribed steroidal compounds, 16, 23-epoxy-22, 26-epimino-cholest-22(N), 23, 25(26)-trien-3β-ol-3-O-β-D-glucopyranosyl-(1→2)-β-D-glucopyranosyl-(1→4)-β-D-galactopyranoside(1) and 26-O-β-D-glucopyranosyl-(25 R)-5α-furost-20(22)-en-3β, 26-diol(2), together with 7 known ones including 26-O-β-D-glucopyranosyl-(25 R)-5, 20(22)-dien-furost-3β, 26-diol(3),(25 R)-5-en-spirost-3β-ol-O-β-D-glucopyranosyl-(1→4)-[α-L-rhmanopyranosyl-(1→2)]-β-D-galactopyranoside(4), funkioside D(5), aspidistrin(6), tigogenin-3-O-β-D-lucotrioside(7), desglucolanatigonin II(8), and degalactotigonin(9), were isolated from Solanum lyratum Thunb. Their cytotoxic activities were tested in two cancer cell lines by MTT method. One of the steroidal glycosides(6) showed significant cytotoxic activity against gastric cancer SGC7901 and liver cancer BEL-7402 cells.

关键词： steroidal alkaloid Furostanol glycoside Solanum lyratum Cytotoxic activity

Inheritance of steroidal glycoalkaloids in potato tuber flesh

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Journal of Integrative Agriculture 2019年第10期18卷 2255-2263页

作者： PENG Zhen WANG Pei TANG Die SHANG Yi LI Can-hui HUANG San-wen ZHANG Chun-zhi The CAAS-YNNU Joint Academy of Potato Sciences Yunnan Normal UniversityKunming 650500P.R.China Genome Analysis Laboratory of the Ministry of Agriculture and Rural Affairs Agricultural Genomics Institute at ShenzhenChinese Academy of Agricultural SciencesShenzhen 518124P.R.China Key Laboratory of Biology and Genetic Improvement of Horticultural Crops of the Ministry of Agriculture and Rural Affairs Sino-Dutch Joint Laboratory of Horticultural GenomicsInstitute of Vegetables and FlowersChinese Academy of Agricultural SciencesBeijing 100081P.R.China

Potato (Solanum tuberosum L.) is the third most important food crop worldwide after wheat and rice in terms of human consumption. A critical domestication trait for potato was the decrease of toxic steroidal glycoalkaloids (SGAs) in tuber flesh. Here, we used a diploid F2 segregating population derived from a cross between S. tuberosum and the wild potato species Solanum chacoense to map the quantitative trait loci (QTLs) associated with the regulation of SGAs content in tuber flesh. In a three-year study, we identified two QTLs on chromosomes 2 and 8 affecting SGAs content in tuber flesh. The QTL on chromosome 8 harbors 38 genes that are co-expressed with the GLYCOALKALOID METABOLISM genes. These findings lay the foundation for exploiting the genes controlling SGAs content in tuber flesh and they provide a theoretical basis for the use of wild germplasm in potato breeding.

关键词： steroidal glycoalkaloids domestication tuber flesh QTL mapping

The enzymatic biosynthesis of acylated steroidal glycosides and their cytotoxic activity

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Acta Pharmaceutica Sinica B 2018年第6期8卷 981-994页

作者： Ming Liu Jian-Qiang Kong State Key Laboratory of Bioactive Substance and Function of Natural Medicines & Ministry of Health Key Laboratory of Biosynthesis of Natural Products Institute of Materia Medica Chinese Academy of Medical Sciences & Peking Union Medical College

Herein we describe the discovery and functional characterization of a steroidal glycosyltransferase(SGT) from Ornithogalum saundersiae and a steroidal glycoside acyltransferase(SGA) from Escherichia coli and their application in the biosynthesis of acylated steroidal glycosides(ASGs). Initially,an SGT gene, designated as OsSGT1, was isolated from O. saundersiae. OsSGT1-containing cell free extract was then used as the biocatalyst to react with 49 structurally diverse drug-like compounds. The recombinant OsSGT1 was shown to be active against both 3β-and 17β-hydroxyl steroids. Unexpectedly,in an effort to identify OsSGT1, we found the bacteria lacA gene in lac operon actually encoded an SGA,specifically catalyzing the acetylations of sugar moieties of steroid 17β-glucosides. Finally, a novel enzymatic two-step synthesis of two ASGs, acetylated testosterone-17-O-β-glucosides(AT-17β-Gs) and acetylated estradiol-17-O-β-glucosides(AE-17β-Gs), from the abundantly available free steroids using OsSGT1 and EcSGA1 as the biocatalysts was developed. The two-step process is characterized by EcSGA1-catalyzed regioselective acylations of all hydroxyl groups on the sugar unit of unprotected steroidal glycosides(SGs) in the late stage, thereby significantly streamlining the synthetic route towards ASGs and thus forming four monoacylates. The improved cytotoxic activities of 30-acetylated testosterone17-O-β-glucoside towards seven human tumor cell lines were thus observable.

关键词： steroidal glycosyltransferase steroidal glycoside acyltransferase Ornithogalum saundersiae Acylated steroidal glycosides LacA

Antibacterial steroidal alkaloids from Holarrhena antidysenteriaca

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Chinese Journal of Natural Medicines 2017年第7期15卷 540-545页

作者： ZHOU Li-Na GE Xiao-Lei DONG Ting-Ting GAO Hui-Yuan SUN Bo-Hang School of Life Science and Biopharmaceutieal Sciences Shenyang Pharmaceutical University Shenyang 110016 China School of Traditional Chinese Materia Medica Shenyang Pharmaceutical University Shenyang 110016 China Key Laboratory of Structure-Based Drug Design & Discovery of Ministry of Education Shenyang Pharmaceutical University Shenyang 110016 China

Two new steroidal alkaloids, isoconkuressine and N-formylconessimine, together with 6 known steroidal alkaloids including conkuressine, conessine, isoconessimine, conimine, conarrhimine, and funtudienine, were isolated from the seeds of Holarrhena antidysenteriaca *** ***. Their intrinsic antibacterial activities and synergistic effects with penicillin and vancomycin were analyzed in methicillin sensitive staphylococcus aureus(MSSA) and methicillin resistant staphylococcus aureus(MRSA). Two of the steroidal alkaloids including one new compound(N-formylconessimine) showed potential antibacterial activity and possessed synergistic effects with penicillin and vancomycin, respectively.

关键词： Holarrhena antidysenteriaca steroidal alkaloid Antibacterial MRSA MSSA Synergistic effect

Two new C_(21) steroidal glycosides isolated from Cynanchum komarovii

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Chinese Journal of Natural Medicines 2018年第8期16卷 610-614页

作者： ZHAO Dan SU Shan-Shan CHEN Shao-Fei LU Xiao-Jie CHEN Gang WANG Yu-Bo SU Guang-Yue PEI Yue-Hu Key Laboratory of Structure-Based Drug Design & Discovery Ministry of EducationShenyang Pharmaceutical University School of Traditional Chinese Materia Medica Shenyang Pharmaceutical University Testing Laboratory Qinghai Entry Exit Inspection and Quarantine Bureau School of Pharmacy Jinzhou Medical University

The present study was designed to further investigate the C_(21) steroidal glycosides in Cynanchum *** new steroidal glycosides based on a 13,14:14,15-disecopregnane-type aglycone,komaroside P(1) and komaroside Q(2),together with three known compounds(3-5) were isolated from the whole herbs of Cynanchum *** aglycones of compounds 1 and 2 were two new *** structures were elucidated on the basis of 1 D,2 D NMR spectroscopic data and acid *** the compounds(1-5) showed potent inhibitory activities against human leukemia cell lines(HL-60) with IC50 values ranging from 16.6 to 26.3 μmol·L^(-1),compared to the positive control 5-fluorouracil(6.4 μmol·L^(-1)).

关键词： Cynanchum komarovii C21 steroidal glycosides Cytotoxic activity

Plants’steroidal Saponins‑A Review on Its Pharmacology Properties and Analytical Techniques

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World Journal of Traditional Chinese Medicine 2022年第3期8卷 350-385页

作者： Sudha Porte Veenu Joshi Kamal Shah Nagendra Singh Chauhan Center for Basic Sciences Pt.Ravishankar Shukla UniversityRaipurChhattisgarhIndia Institute of Pharmaceutical Research GLA UniversityMathuraUttar PradeshIndia Drugs Testing Laboratory Avam Anusandhan KendraRaipurChhattisgarhIndia

The plant is a rich repository of useful secondary metabolites with profound medicinal ***,one type of bioactive compound,are amphitheatric glycosides with one and more hydrophilic sugar and hydrophobic steroidal and terpenoid *** former is known as steroidal saponin,and the latter is called terpenoid *** saponin is mostly distributed among monocotyledon families such as Asparagaceae,Amaryllidaceae,Dioscoreaceae,Smilacaceae,and *** though it is unusual,it could also be detected to some extent by dicotyledonous angiosperms,such as Plantaginaceae,Zygophyllaceae,Fabaceae,Asteraceae,and *** exhibits diverse pharmacological ability including antimicrobic,anti‑inflammatory,cAMP phosphodiesterase inhibitory,antiadipogenic,bactericide,cardioprotective,antitumor,antidiabetic,cytotoxic activity,antifungal,antiviral,antioxidant,and *** saponin timosaponin AIII from Anemarrhena asphodeloides has been found to possess antitumor ***,another steroidal sapogenin,has the potential of preventing neurological diseases by affecting different signaling pathways,increasing bone formation,and increasing antithrombotic *** A from Liriope platyphylla possesses anti‑inflammatory,antiasthma,and antiosteoclastogenic ***2 from Trillium tschonoskii exhibits anticancer *** cell cycle arrest and ROS‑dependent autophagy are induced by polyphyllin *** diverse biological activities of steroidal saponins are attributed to the variability of their structural *** of steroidal saponins in plant materials mainly utilizes classically and advances thin layer chromatography(TLC)on normal and reverses‑phase(high‑performance thin‑layer chromatography,densitometric TLC),gas chromatography,LC,UPLC,ultra‑high‑performance liquid chromatography(HPLC),supercritical fluid chromatography,and HPLC coupled to ultraviolet detector and diode array *** coupled with

关键词： steroidal Saponins Glycosides Antitumour Antioxidant Analytical techniques

Effects of structural modification of anti-inflammatory steroidal antedrug on pro-inflammatory mediators and inhibitory cytokines in human alveolar epithelial cells

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Health 2009年第3期1卷 127-133页

作者： Gui-Fang Wang Soonjo Kwon Rakesh Sharma Hemang Patel Henry J. Lee Florida State University Utah State University

The anti-inflammatory effects of the new ster-oidal antedrug, 21-acetyloxy-9α-fluoro-11β-hy-droxyl-3, 20-dioxo-1, 4-pregnadieno-[16α, 17α-d] isoxazoline (FP-ISO-21AC), on nitric oxide (NO) and interleukin 8 (IL-8) production, were inves-tigated together with its parent steroid predni-solone (PRED). PRED is one of the anti-in-flammatory steroids but has systemic side ef-fects which limit the use of it. PRED was modi-fied with ‘antedrug concept’ to create safer drugs that attack problems such as inflamma-tion, then quickly become inactive before they can cause systemic side effect. We had a test about the effect of the modified anti-inflamma-tory steroidal antedrug on anti-inflammatory activity. The present study evaluated their ability to inhibit cytokine-induced NO and IL-8 produc-tion in human alveolar epithelial cells. We also investigated their ability to enhance the expres-sion of inhibitory cytokine receptor, interleukin 22 receptor (IL-22R) in human alveolar epithelial cells. Our results showed that FP-ISO-21AC sh- owed higher ability to inhibit the cytokine - in-duced production of NO than PRED. Exogenous IL-22 was added to the media of both human alveolar epithelial cells (A549) and human lung fibroblast (HLF-1). In the presence of the ex-ogenous inhibitory cytokine IL-22, further re-duction of NO production was observed in A549 cells, which express IL-22R, but not in HLF1, which does not express IL-22R. These data suggested that the steroidal antedrugs en-hanced the expression of IL-22R. FP-ISO- 21AC showed higher potency than PRED to restore the expression of IL-22R. FP-ISO-21AC further reduced NO production to 27% and PRED further reduced NO production to 39%. In con-clusion, a synthesized steroidal antedrug FP- ISO-21AC showed higher anti-inflammatory ef-fects than PRED by inhibiting the expression of pro-inflammatory mediator NO and stimulating the expression of IL-22R.

关键词： steroidal Antedrug NO Production IL-8 Production Anti-Inflammatory Cytokine Receptor IL-22 Receptor