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11-Aza-artemisinin derivatives Exhibit Anticancer Activities by Targeting the Fatty Acid Binding Protein 6(FABP6)

Chinese Journal of Chemistry 2018年第12期36卷 1197-1201页

作者： Xin-Ya Chen Yue Yin Jie Xi Yi Yuan Yan Li Qing Li Ren-Xiao Wang Zhu-Jun Yao Gong-Li Tang State Key Laboratory of Bio-organic and Natural Products Chemistry Shanghai Institute of Organic ChemistryChinese Academy of Sciences345 Lingling RoadShanghai 200032China State Key Laboratory of Coordination Chemistry Jiangsu Key Laboratory of Advanced Organic MaterialsSchool of Chemistry and Chemical EngineeringNanjing University163 Xianlin AvenueNanjingJiangsu 210023China

artemisinin (Qinghaosu), a sesquiterpene lactone isolated from the Chinese medicinal herb Artemisia annua, is famous as the first‐line antimalarial drug, and reported to also possess anticancer properties. Though many studies have proceeded focusing on artemisinin and bioactive derivatives in clinic or laboratory, their cellular targets and mechanism of actions have still remained obscure. Here, two new 11‐aza‐artemisinin derivatives AAD1 and AAD2, which displayed cytotoxity against multiple cancer cell lines, were synthesized and applied as the probes for target identification and anticancer mechanism research. Using T7 phage display screen method, fatty acid binding protein 6 (FABP6) was identified and verified as one of the potential targets. Further studies showed FABP6 is a direct binding protein of AAD1 and AAD2, and mediated the corresponding anticancer activities of these artemisinin derivatives.

关键词： artemisinin derivatives biological activity apoptosis phage display target FABP6 molecule‐protein interaction

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Thermodynamic Study on the Solubility Properties of Guangxi artemisinin derivatives

Thermodynamic Study on the Solubility Properties of Guangxi ...

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第十届全国中药和天然药物学术研讨会

作者： Shen Xue-song~a Qiu Zhuang-ping~a Zhang Zhi-peng~a Xie Yan-xia~a Qin Xue-lian~a Dong Jia-xin~b a Pharmacy Faculty of Guilin Medical College,Guilin 541004,China b Chemistry and Molecule Scientific Institute,Wuhan University,Wuhan 430072,China

Chemical thermodynamics was employed to study the solubility properties of artemisinin,dihydroartemisinin, aetemether and *** standard molar enthalpies of the four compounds were determined by an RBC-Ⅱrotating-bomb *** analysis was performed to decide concentrations of artesunate in water,the octanol/water partition coefficient of artesunate was *** combustion enthalpies of artemisinin,dihydroarterninin,artemether and artesunate△H were:(-7553.97±6.48)、(-6620.18±6.46)、(-7592.20±6.18)、(-8158.19±8.48)kJ·mol-1 respectively;Standard enthalpies of formation△H were:(-1492.81±7.62)、(-2712.43±7.62)、(-2419.75±7.52)、(-3320.12±9.90)kJ·mol-1, *** octanol/water partition coefficient(KOW)of artesunate was 29.07,RSD was 0.2%.Eutectic point of the simple eutectic mixture of artemisinin and urea was 84.5～85.9℃.

关键词： Thermochemistry artemisinin derivatives Standard enthalpy of formation Partition coefficient Eutectics

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Antitumor Research on artemisinin and Its Bioactive derivatives

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Natural Products and Bioprospecting 2018年第4期8卷 303-319页

作者： Yunqin Zhang Guowei Xu Shuqun Zhang Dong Wang PSaravana Prabha Zhili Zuo State Key Laboratory of Phytochemistry and Plant Resources in West China Kunming Institute of BotanyChinese Academy of SciencesKunming 650201China University of the Chinese Academy of Sciences Beijing 100049China Yunnan Key Laboratory of Natural Medicinal Chemistry Kunming 650201YunnanChina

Cancer is the leading cause of human death which seriously threatens human *** antimalarial drug artemisinin and its derivatives have been discovered with considerable anticancer ***,a variety of target-selective artemisinin-related compounds with high efficiency have been *** researches indicated that artemisinin-related compounds have cytotoxic effects against a variety of cancer cells through pleiotropic effects,including inhibiting the proliferation of tumor cells,promoting apoptosis,inducing cell cycle arrest,disrupting cancer invasion and metastasis,preventing angiogenesis,mediating the tumor-related signaling pathways,and regulating tumor *** importantly,artemisinins demonstrated minor side effects to normal cells and manifested the ability to overcome multidrug-resistance which is widely observed in cancer ***,we concentrated on the new advances and development of artemisinin and its derivatives as potential antitumor agents in recent 5 *** is our hope that this review could be helpful for further exploration of novel artemisinin-related antitumor agents.

关键词： artemisinin artemisinin derivatives Antitumor Activity Mechanism

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Antimalarial activity of a novel series of artemisinin-derived 1, 2, 3-triazole dimers

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Asian Pacific Journal of Tropical Medicine 2019年第5期12卷 195-203页

作者： Kabita Gogoi Gokul Baishya Biswajit Saikia Nabin Chandra Barua Chandrajit Dohutia Akalesh Kumar Verma Anil Prakash ICMR-Regional Medical Research Centre,N.E. CSIR-North-East Institute of Science and Technology Digboi College,Chemistry Department Pratiksha Institute of Pharmaceutical Scinces Cotton University,Zoology Department ICMR-National Institute for Research in Environmental Health ICMR-Regional Medical Research Centre N.E. CSIR-North-East Institute of Science and Technology Digboi College Chemistry Department Pratiksha Institute of Pharmaceutical Scinces Cotton University Zoology Department ICMR-National Institute for Research in Environmental Health

Objective: To obtain suitable artimisinin-based drug candidates with high antimalarial ***: Three different reaction schemes were used to synthesize a total of 15 artemisininbased *** first synthetic scheme involved the synthesis of diazido aliphatic and aromatic compounds from commercially available dihalides and azido derivatives of *** second scheme consisted of the reaction of dibromoaliphatic compounds with sodium azide in dimethylformamide which yielded the desired ***-based compounds on treatment with sodium azide and bromotrimethylsilane in dichloromethane produced the most potent compound *** potent compound GB-1 was synthesized from artemisinin by treatment with alcohols in the presence of Aberlyst-15 in anhydrous *** third scheme involved the Huisgen 1,3-dipolar cycloaddition between the synthesized aliphatic and aromatic diazides and two alkyne derivatives of artemisinin to obtain the desired artemisinin dimers with average ***: The best in vitro antiplasmodial activity was shown by the compound GB-2 registering IC_(50) value 0.066 μg/mL against chloroquine-sensitive and 0.865 μg/mL against chloroquineresistant strains of Plasmodium *** suppressed 59.0% parasitaemia in vivo of rodent malaria parasite Plasmodium berghei in Swiss albino model at 50 μg/kg body weight *** docking interactions of Plasmodium falciparum ATP6(PfATP6) protein revealed strong bonding of GB-2 with Thr255 residue which is likely to be the reason for excellent antimalarial activity of this ***: Two compounds GB-1 and GB-2 exhibited excellent in vitro antiplasmodial activity and fair in vivo antimalarial *** the two, GB-2 showed better activity which could be attributed to its strong bonding interactions with Thr255 as evidenced from the molecular docking *** helped in identifying artemisinin analogues possessing good antimalarial properties a

关键词： Antimalarial activity artemisinin derivatives Huisgen reaction Triazole dimers Plasmodium berghei Plasmodium falciparum Molecular docking

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Expanding the Therapeutic Spectrum of artemisinin:Activity Against Infectious Diseases Beyond Malaria and Novel Pharmaceutical Developments

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World Journal of Traditional Chinese Medicine 2016年第2期2卷 1-23页

作者： Thomas Efferth Marta R.Romero Anna Rita Bilia Ahmed Galal Osman Mahmoud ElSohly Michael Wink Rudolf Bauer Ikhlas Khan Maria Camilla Bergonzi Jose J.G.Marin Department of Pharmaceutical Biology Institute of Pharmacy and Biochemistry Johannes Gutenberg University Experimental Hepatology and Drug Targeting (HEVEFARM) CIBERehd IBSAL University of SalamancaCampus Miguel de Unamuno Department of Chemistry "Ugo Schiff" University of Florence National Center for Natural Products Research School of Pharmacy University of Mississippi ElSohly Laboratories Inc. Department of Pharmaceutics University of Mississippi Institute of Pharmacy and Molecular Biotechnology Ruprecht-Karls University Institute of Pharmaceutical Sciences Department of Pharmacognosy University of Graz Devision of Pharmacognosy Department of Biomolecular Sciences University of Mississippi

The interest of Western medicine in Traditional Chinese Medicine(TCM) as a source of drug leads/new drugs to treat diseases without available efficient therapies has been dramatically augmented in the last decades by the extensive work and the outstanding findings achieved within this kind of medicine. The practice of TCM over thousands of years has equipped scientists with substantial experience with hundreds of plants that led to the discovery of artemisinin(qinghaosu), which is extracted from the medicinal plant Artemisia annua L.(qinghao). The unexpected success of artemisinin in combating malaria has drawn strong attention from the scientific community towards TCM. artemisinin was discovered by Youyou Tu in 1972. Since then, several novel pharmacological activities based on the well-known properties of the sesquiterpene lactone structure with the oxepane ring and an endoperoxide bridge have been unravelled. Beyond malaria, artemisinin and its derivatives(artemisinins) exert profound activities towards other protozoans(Leishmania, Trypanosoma, amoebas, Neospora caninum, and Eimeria tenella), trematodes(Schistosoma, liver flukes), and viruses(human cytomegalovirus, hepatitis B and C viruses). Less clear is the effect against bacteria and fungi. Based on the promising results of artemisinin and the first generation derivatives(artesunate, artemether, arteether), novel drug development strategies have been *** included the synthesis of acetal-and non-acetal-type artemisinin dimeric molecules as well as developing nanotechnological approaches, ***-based liposomes, niosomes, micelles, solid lipid nanocarriers, nanostructured lipid carriers, nanoparticles, fullerenes and nanotubes. The current review presents an overview on different aspects of artemisinins, including sources, chemistry, biological/pharmacological properties, types of infectious pathogens that are susceptible to artemisinins in vitro and in vivo, in addition to the advancement in

关键词： artemisinin derivatives Artemisia annua Asteraceae Antimalarial drugs Anti-pathogen activity Antiviral properties artemisinin-loaded nanocarriers Traditional Chinese Medicine

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N1-{4-[（10S）-dihydroartemisinin-10-oxyl]}phenylmethylene-N2-（quinoline-4-yl）hydrazine derivatives as Antiplasmodial Falcipain-2 Inhibitors

N1-{4-[（10S）-dihydroartemisinin-10-oxyl]}phenylmethylene-N...

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2011年全国药物化学学术会议——药物的源头创新

作者： Wei Luo~1,Xin Zhang~1,Fei Yu~1,Jin Huang~2,Chun Guo~(1,*) 1 Key Laboratory of Structure-Based Drug Design & Discovery(Shenyang Pharmaceutical University), Ministry of Education Shenyang 110016. 2 School of Pharmacy,East China University of Science and Technology,Shanghai 200237.

＜正＞Malaria,the most common parasitic diseases in tropical and subtropical regions,is one of the major public health problems in the *** to the spread of multi-resistant Plasmodium falciparum strains,combined with the lack of effective vaccines,there is an urgent need for the rapid development of new mechanism and effective antimalarial *** has been used successfully against

关键词： antimalarial falcipain-2 inhibitors artemisinin derivatives

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