☆ 4.5 Article

Cytotoxic quassinoids from Ailanthus altissima

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2013)

Journal

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Volume 23, Issue 3, Pages 654-657

Publisher

PERGAMON-ELSEVIER SCIENCE LTD

DOI: 10.1016/j.bmcl.2012.11.116

Keywords

Ailanthus altissima; Simaroubaceae; Quassinoids; Cytotoxicity

Categories

Chemistry, Medicinal Chemistry, Organic

Funding

Program for Changjiang Scholars and Innovative Research Team in University [IRT0965]
National Natural Science Foundation of China [30901848, 81172947, 81202428]
Natural Science Foundation of Guangdong Province [8351063201000003, S2012040007825]
Fundamental Research Funds for the Central Universities [21612203]

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Abstract

Two new quassinoids, altissinol A (1) and B (7), together with 12 known quassinoids, were isolated from the 95% ethanol extract of the barks of Ailanthus altissima. The structures of the new compounds (1 and 7) were determined on the basis of the spectroscopic methods including UV, IR, HR-ESI-MS, 1D and 2D NMR. The cytotoxic potential of all isolates were evaluated in vitro against three human hepatoma cell lines. Quassinoids 1-7 displayed potent cytotoxic activities against human hepatoma Hep3B and HepG2 cell lines. Interestingly, compounds 2, 3, and 5 exhibited cytotoxic activity against multidrug resistance HepG2/ADM cell line with IC50 value 4.3-fold more sensitive to Doxorubicin (DOX). (c) 2012 Elsevier Ltd. All rights reserved.

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Camonis, Nadine Camougrand, Michelangelo Campanella, Edward M. Campbell, Francois-Xavier Campbell-Valois, Silvia Campello, Ilaria Campesi, Juliane C. Campos, Olivier Camuzard, Jorge Cancino, Danilo Candido de Almeida, Laura Canesi, Isabella Caniggia, Barbara Canonico, Carles Canti, Bin Cao, Michele Caraglia, Beatriz Carames, Evie H. Carchman, Elena Cardenal-Munoz, Cesar Cardenas, Luis Cardenas, Sandra M. Cardoso, Jennifer S. Carew, Georges F. Carle, Gillian Carleton, Silvia Carloni, Didac Carmona-Gutierrez, Leticia A. Carneiro, Oliana Carnevali, Julian M. Carosi, Serena Carra, Alice Carrier, Lucie Carrier, Bernadette Carroll, A. Brent Carter, Andreia Neves Carvalho, Magali Casanova, Caty Casas, Josefina Casas, Chiara Cassioli, Eliseo F. Castillo, Karen Castillo, Sonia Castillo-Lluva, Francesca Castoldi, Marco Castori, Ariel F. Castro, Margarida Castro-Caldas, Javier Castro-Hernandez, Susana Castro-Obregon, Sergio D. Catz, Claudia Cavadas, Federica Cavaliere, Gabriella Cavallini, Maria Cavinato, Maria L. Cayuela, Paula Cebollada Rica, Valentina Cecarini, Francesco Cecconi, Marzanna Cechowska-Pasko, Simone Cenci, Victoria Ceperuelo-Mallafre, Joao J. Cerqueira, Janete M. Cerutti, Davide Cervia, Vildan Bozok Cetintas, Silvia Cetrullo, Han-Jung Chae, Andrei S. Chagin, Chee-Yin Chai, Gopal Chakrabarti, Oishee Chakrabarti, Tapas Chakraborty, Trinad Chakraborty, Mounia Chami, Georgios Chamilos, David W. Chan, Edmond Y. W. Chan, Edward D. Chan, H. Y. Edwin Chan, Helen H. Chan, Hung Chan, Matthew T. Chan, Yau Sang Chan, Partha K. Chandra, Chih-Peng Chang, Chunmei Chang, Hao-Chun Chang, Kai Chang, Jie Chao, Tracey Chapman, Nicolas Charlet-Berguerand, Samrat Chatterjee, Shail K. Chaube, Anu Chaudhary, Santosh Chauhan, Edward Chaum, Frederic Checler, Michael E. Cheetham, ChangShi Chen, Guang-Chao Chen, Jian-Fu Chen, Liam L. Chen, Leilei Chen, Lin Chen, Mingliang Chen, MuKuan Chen, Ning Chen, Quan Chen, Ruey-Hwa Chen, Shi Chen, Wei Chen, Weiqiang Chen, XinMing Chen, Xiong-Wen Chen, Xu Chen, Yan Chen, Ye-Guang Chen, Yingyu Chen, Yongqiang Chen, YuJen Chen, Yue-Qin Chen, Zhefan Stephen Chen, Zhi Chen, Zhi-Hua Chen, Zhijian J. Chen, Zhixiang Chen, Hanhua Cheng, Jun Cheng, Shi-Yuan Cheng, Wei Cheng, Xiaodong Cheng, Xiu-Tang Cheng, Yiyun Cheng, Zhiyong Cheng, Zhong Chen, Heesun Cheong, Jit Kong Cheong, Boris Chernyak, Sara Cherry, Chi Fai Randy Cheung, Chun Hei Antonio Cheung, King-Ho Cheung, Eric Chevet, Richard J. Chi, Alan Kwok Shing Chiang, Ferdinando Chiaradonna, Roberto Chiarelli, Mario Chiariello, Nathalia Chica, Susanna Chiocca, Mario Chiong, Shih-Hwa Chiou, Abhilash Chiramel, Valerio Chiurchiu, Dong-Hyung Cho, Seong-Kyu Choe, Augustine M. K. Choi, Mary E. Choi, Kamalika Roy Choudhury, Norman S. Chow, Charleen T. Chu, Jason P. Chua, John Jia En Chua, Hyewon Chung, Kin Pan Chung, Seockhoon Chung, So-Hyang Chung, Yuen-Li Chung, Valentina Cianfanelli, Iwona A. Ciechomska, Mariana Cifuentes, Laura Cinque, Sebahattin Cirak, Mara Cirone, Michael J. Clague, Robert Clarke, Emilio Clementi, Eliana M. Coccia, Patrice Codogno, Ehud Cohen, Mickael M. Cohen, Tania Colasanti, Fiorella Colasuonno, Robert A. Colbert, Anna Colell, Nuria S. Coll, Mark O. Collins, Maria Colombo, Daniel A. Colon-Ramos, Lydie Combaret, Sergio Comincini, Marcia R. Cominetti, Antonella Consiglio, Andrea Conte, Fabrizio Conti, Viorica Raluca Contu, Mark R. Cookson, Kevin M. Coombs, Isabelle Coppens, Maria Tiziana Corasaniti, Dale P. Corkery, Nils Cordes, Katia Cortese, Maria do Carmo Costa, Sarah Costantino, Paola Costelli, Ana Coto-Montes, Peter J. Crack, Jose L. Crespo, Alfredo Criollo, Valeria Crippa, Riccardo Cristofani, Tamas Csizmadia, Antonio Cuadrado, Bing Cui, Jun Cui, Yixian Cui, Yong Cui, Emmanuel Culetto, Andrea C. Cumino, Andrey Cybulsky, Mark J. Czaja, Stanislaw J. Czuczwar, Stefania D'Adamo, Marcello D'Amelio, Daniela D'Arcangelo, Andrew C. D'Lugos, Gabriella D'Orazi, James A. da Silva, Hormos Salimi Dafsari, Ruben K. Dagda, Yasin Dagdas, Maria Daglia, Xiaoxia Dai, Yun Dai, Yuyuan Dai, Jessica Dal Col, Paul Dalhaimer, Luisa Dalla Valle, Tobias Dallenga, Guillaume Dalmasso, Markus Damme, Ilaria Dando, Nico P. Dantuma, April L. Darling, Hiranmoy Das, Srinivasan Dasarathy, Santosh K. Dasari, Srikanta Dash, Oliver Daumke, Adrian N. Dauphinee, Jeffrey S. Davies, Valeria A. Davila, Roger J. Davis, Tanja Davis, Sharadha Dayalan Naidu, Francesca De Amicis, Karolien De Bosscher, Francesca De Felice, Lucia De Franceschi, Chiara De Leonibus, Mayara G. de Mattos Barbosa, Guido R. Y. De Meyer, Angelo De Milito, Cosimo De Nunzio, Clara De Palma, Mauro De Santi, Claudio De Virgilio, Daniela De Zio, Jayanta Debnath, Brian J. DeBosch, JeanPaul Decuypere, Mark A. Deehan, Gianluca Deflorian, James DeGregori, Benjamin Dehay, Gabriel Del Rio, Joe R. Delaney, Lea M. D. Delbridge, Elizabeth Delorme-Axford, M. Victoria Delpino, Francesca Demarchi, Vilma Dembitz, Nicholas D. Demers, Hongbin Deng, Zhiqiang Deng, Joern Dengjel, Paul Dent, Donna Denton, Melvin L. DePamphilis, Channing J. Der, Vojo Deretic, Albert Descoteaux, Laura Devis, Sushil Devkota, Olivier Devuyst, Grant Dewson, Mahendiran Dharmasivam, Rohan Dhiman, Diego di Bernardo, Manlio Di Cristina, Fabio Di Domenico, Pietro Di Fazio, Alessio Di Fonzo, Giovanni Di Guardo, Gianni M. Di Guglielmo, Luca Di Leo, Chiara Di Malta, Alessia Di Nardo, Martina Di Rienzo, Federica Di Sano, George Diallinas, Jiajie Diao, Guillermo Diaz-Araya, Ines Diaz-Laviada, Jared M. Dickinson, Marc Diederich, Melanie Dieude, Ivan Dikic, Shiping Ding, Wen-Xing Ding, Luciana Dini, Miroslav Dinic, Albena T. Dinkova-Kostova, Marc S. Dionne, Jorg H. W. Distler, Abhinav Diwan, Ian M. C. Dixon, Mojgan Djavaheri-Mergny, Ina Dobrinski, Oxana Dobrovinskaya, Radek Dobrowolski, Renwick C. J. Dobson, Serap Dokmeci Emre, Massimo Donadelli, Bo Dong, Xiaonan Dong, Zhiwu Dong, Gerald W. Dorn Ii, Volker Dotsch, Huan Dou, Juan Dou, Moataz Dowaidar, Sami Dridi, Liat Drucker, Ailian Du, Caigan Du, Guangwei Du, Hai-Ning Du, Li-Lin Du, Andre du Toit, Shao-Bin Duan, Xiaoqiong Duan, Sonia P. Duarte, Anna Dubrovska, Elaine A. Dunlop, Nicolas Dupont, Raul Duran, Bilikere S. Dwarakanath, Sergey A. Dyshlovoy, Darius Ebrahimi-Fakhari, Leopold Eckhart, Charles L. Edelstein, Thomas Efferth, Eftekhar Eftekharpour, Ludwig Eichinger, Nabil Eid, Tobias Eisenberg, N. Tony Eissa, Sanaa Eissa, Miriam Ejarque, Abdeljabar El Andaloussi, Nazira El-Hage, Shahenda El-Naggar, Anna Maria Eleuteri, Eman S. El-Shafey, Mohamed Elgendy, Aristides G. Eliopoulos, Maria M. Elizalde, Philip M. Elks, Hans-Peter Elsasser, Eslam S. Elsherbiny, Brooke M. Emerling, N. C. Tolga Emre, Christina H. Eng, Nikolai Engedal, Anna-Mart Engelbrecht, Agnete S. T. Engelsen, Jorrit M. Enserink, Ricardo Escalante, Audrey Esclatine, Mafalda Escobar-Henriques, Eeva-Liisa Eskelinen, Lucile Espert, Makandjou-Ola Eusebio, Gemma Fabrias, Cinzia Fabrizi, Antonio Facchiano, Francesco Facchiano, Bengt Fadeel, Claudio Fader, Alex C. Faesen, W. Douglas Fairlie, Alberto Falco, Bjorn H. Falkenburger, Daping Fan, Jie Fan, Yanbo Fan, Evandro F. Fang, Yanshan Fang, Yognqi Fang, Manolis Fanto, Tamar Farfel-Becker, Mathias Faure, Gholamreza Fazeli, Anthony O. Fedele, Arthur M. Feldman, Du Feng, Jiachun Feng, Lifeng Feng, Yibin Feng, Yuchen Feng, Wei Feng, Thais Fenz Araujo, Thomas A. Ferguson, Jose C. Fernandez-Checa, Sonia FernandezVeledo, Alisdair R. Fernie, Anthony W. Ferrante, Alessandra Ferraresi, Merari F. Ferrari, Julio C. B. Ferreira, Susan Ferro-Novick, Antonio Figueras, Riccardo Filadi, Nicoletta Filigheddu, Eduardo FilippiChiela, Giuseppe Filomeni, Gian Maria Fimia, Vittorio Fineschi, Francesca Finetti, Steven Finkbeiner, Edward A. Fisher, Paul B. Fisher, Flavio Flamigni, Steven J. Fliesler, Trude H. Flo, Ida Florance, Oliver Florey, Tullio Florio, Erika Fodor, Carlo Follo, Edward A. Fon, Antonella Forlino, Francesco Fornai, Paola Fortini, Anna Fracassi, Alessandro Fraldi, Brunella Franco, Rodrigo Franco, Flavia Franconi, Lisa B. Frankel, Scott L. Friedman, Leopold F. Frohlich, Gema Fruhbeck, Jose M. Fuentes, Yukio Fujiki, Naonobu Fujita, Yuuki Fujiwara, Mitsunori Fukuda, Simone Fulda, Luc Furic, Norihiko Furuya, Carmela Fusco, Michaela U. Gack, Lidia Gaffke, Sehamuddin Galadari, Alessia Galasso, Maria F. Galindo, Sachith Gallolu Kankanamalage, Lorenzo Galluzzi, Vincent Galy, Noor Gammoh, Boyi Gan, Ian G. Ganley, Feng Gao, Hui Gao, Minghui Gao, Ping Gao, Shou-Jiang Gao, Wentao Gao, Xiaobo Gao, Ana Garcera, Maria Noe Garcia, Veronica E. Garcia, Francisco Garcia-Del Portillo, Vega Garcia-Escudero, Aracely GarciaGarcia, Marina Garcia-Macia, Diana Garcia-Moreno, Carmen Garcia-Ruiz, Patricia Garcia-Sanz, Abhishek D. Garg, Ricardo Gargini, Tina Garofalo, Robert F. Garry, Nils C. Gassen, Damian Gatica, Liang Ge, Wanzhong Ge, Ruth Geiss-Friedlander, Cecilia Gelfi, Pascal Genschik, Ian E. Gentle, Valeria Gerbino, Christoph Gerhardt, Kyla Germain, Marc Germain, David A. Gewirtz, Elham Ghasemipour Afshar, Saeid Ghavami, Alessandra Ghigo, Manosij Ghosh, Georgios Giamas, Claudia Giampietri, Alexandra Giatromanolaki, Gary E. Gibson, Spencer B. Gibson, Vanessa Ginet, Edward Giniger, Carlotta Giorgi, Henrique Girao, Stephen E. Girardin, Mridhula Giridharan, Sandy Giuliano, Cecilia Giulivi, Sylvie Giuriato, Julien Giustiniani, Alexander Gluschko, Veit Goder, Alexander Goginashvili, Jakub Golab, David C. Goldstone, Anna Golebiewska, Luciana R. Gomes, Rodrigo Gomez, Ruben Gomez-Sanchez, Maria Catalina Gomez-Puerto, Raquel Gomez-Sintes, Qingqiu Gong, Felix M. Goni, Javier Gonzalez-Gallego, Tomas Gonzalez-Hernandez, Rosa A. Gonzalez-Polo, Jose A. Gonzalez-Reyes, Patricia Gonzalez-Rodriguez, Ing Swie Goping, Marina S. Gorbatyuk, Nikolai Gorbunov, Roxana M. Gorojod, Sharon M. Gorski, Sandro Goruppi, Cecilia Gotor, Roberta A. Gottlieb, Illana Gozes, Devrim Gozuacik, Martin Graef, Markus H. Graler, Veronica Granatiero, Daniel Grasso, Joshua P. Gray, Douglas R. Green, Alexander Greenhough, Stephen L. Gregory, Edward F. Griffin, Mark W. Grinstaff, Frederic Gros, Charles Grose, Angelina S. Gross, Florian Gruber, Paolo Grumati, Tilman Grune, Xueyan Gu, Jun-Lin Guan, Carlos M. Guardia, Kishore Guda, Flora Guerra, Consuelo Guerri, Prasun Guha, Carlos Guillen, Shashi Gujar, Anna Gukovskaya, Ilya Gukovsky, Jan Gunst, Andreas Gunther, Anyonya R. Guntur, Chuanyong Guo, Chun Guo, Hongqing Guo, Lian-Wang Guo, Ming Guo, Pawan Gupta, Alvaro F. Fernandez, Shashi Kumar Gupta, Swapnil Gupta, Veer Bala Gupta, Vivek Gupta, Asa B. Gustafsson, David D. Gutterman, H. B. Ranjitha, Annakaisa Haapasalo, James E. Haber, Shinji Hadano, Anders J. Hafren, Mansour Haidar, Belinda S. Hall, Gunnel Hallden, Anne Hamacher-Brady, Andrea Hamann, Maho Hamasaki, Weidong Han, Malene Hansen, Phyllis Hanson, Zijian Hao, Masaru Harada, Ljubica Harhaji-Trajkovic, Nirmala Hariharan, Nigil Haroon, James Harris, Takafumi Hasegawa, Noor Hasima Nagoor, Jeffrey A. Haspel, Volker Haucke, Wayne D. Hawkins, Bruce A. Hay, Cole M. Haynes, Soren B. Hayrabedyan, Thomas S. Hays, Congcong He, Qin He, RongRong He, You-Wen He, Yu-Ying He, Yasser Heakal, Alexander M. Heberle, J. Fielding Hejtmancik, Gudmundur Vignir Helgason, Vanessa Henkel, Marc Herb, Alexander Hergovich, Anna Herman-Antosiewicz, Agustin Hernandez, Carlos Hernandez, Sergio Hernandez-Diaz, Virginia Hernandez-Gea, Amaury Herpin, Judit Herreros, Javier H. Hervas, Daniel Hesselson, Claudio Hetz, Volker T. Heussler, Yujiro Higuchi, Sabine Hilfiker, Joseph A. Hill, William S. Hlavacek, Emmanuel A. Ho, Idy H. T. Ho, Philip Wing-Lok Ho, ShuLeong Ho, Wan Yun Ho, G. Aaron Hobbs, Mark Hochstrasser, Peter H. M. Hoet, Daniel Hofius, Paul Hofman, Annika Hohn, Carina Holmberg, Jose R. Hombrebueno, Chang-Won Hong, Yi-Ren Hong, Lora Hooper, Thorsten Hoppe, Rastislav Horos, Yujin Hoshida, I-Lun Hsin, Hsin-Yun Hsu, Bing Hu, Dong Hu, Li-Fang Hu, Ming Chang Hu, Ronggui Hu, Wei Hu, Yu-Chen Hu, Zhuo-Wei Hu, Fang Hua, Jinlian Hua, Yingqi Hua, Chongmin Huan, Canhua Huang, Chuanshu Huang, Chuanxin Huang, Chunling Huang, Haishan Huang, Kun Huang, Michael L. H. Huang, Rui Huang, Shan Huang, Tianzhi Huang, Xing Huang, Yuxiang Jack Huang, Tobias B. Huber, Virginie Hubert, Christian A. Hubner, Stephanie M. Hughes, William E. Hughes, Magali Humbert, Gerhard Hummer, James H. Hurley, Sabah Hussain, Salik Hussain, Patrick J. Hussey, Martina Hutabarat, Hui-Yun Hwang, Seungmin Hwang, Antonio Ieni, Fumiyo Ikeda, Yusuke Imagawa, Yuzuru Imai, Carol Imbriano, Masaya Imoto, Denise M. Inman, Ken Inoki, Juan Iovanna, Renato Iozzo, Giuseppe Ippolito, Javier E. Irazoqui, Pablo Iribarren, Mohd Ishaq, Makoto Ishikawa, Nestor Ishimwe, Ciro Isidoro, Nahed Ismail, Shohreh Issazadeh-Navikas, Eisuke Itakura, Daisuke Ito, Davor Ivankovic, Saska Ivanova, Anand Krishnan Iyer, Jose M. Izquierdo, Masanori Izumi, Marja Jaattela, Majid Sakhi Jabir, William T. Jackson, Nadia Jacobo-Herrera, Anne-Claire Jacomin, Elise Jacquin, Pooja Jadiya, Hartmut Jaeschke, Chinnaswamy Jagannath, Arjen J. Jakobi, Johan Jakobsson, Bassam Janji, Pidder JansenDurr, Patric J. Jansson, Jonathan Jantsch, Slawomir Januszewski, Alagie Jassey, Steve Jean, Helene JeltschDavid, Pavla Jendelova, Andreas Jenny, Thomas E. Jensen, Niels Jessen, Jenna L. Jewell, Jing Ji, Lijun Jia, Rui Jia, Liwen Jiang, Qing Jiang, Richeng Jiang, Teng Jiang, Xuejun Jiang, Yu Jiang, Maria Jimenez-Sanchez, Eun-Jung Jin, Fengyan Jin, Hongchuan Jin, Li Jin, Luqi Jin, Meiyan Jin, Si Jin, Eun-Kyeong Jo, Carine Joffre, Terje Johansen, Gail V. W. Johnson, Simon A. Johnston, Eija Jokitalo, Mohit Kumar Jolly, Leo A. B. Joosten, Joaquin Jordan, Bertrand Joseph, Dianwen Ju, Jeong-Sun Ju, Jingfang Ju, Esmeralda Juarez, Delphine Judith, Gabor Juhasz, Youngsoo Jun, Chang Hwa Jung, SungChul Jung, Yong Keun Jung, Heinz Jungbluth, Johannes Jungverdorben, Steffen Just, Kai Kaarniranta, Allen Kaasik, Tomohiro Kabuta, Daniel Kaganovich, Alon Kahana, Renate Kain, Shinjo Kajimura, Maria Kalamvoki, Manjula Kalia, Danuta S. Kalinowski, Nina Kaludercic, Ioanna Kalvari, Joanna Kaminska, Vitaliy O. Kaminskyy, Hiromitsu Kanamori, Keizo Kanasaki, Chanhee Kang, Rui Kang, Sang Sun Kang, Senthilvelrajan Kaniyappan, Tomotake Kanki, Thirumala-Devi Kanneganti, Anumantha G. Kanthasamy, Arthi Kanthasamy, Marc Kantorow, Orsolya Kapuy, Michalis Karamouzis, Md Razaul Karim, Parimal Karmakar, Rajesh G. Katare, Masaru Kato, Stefan H. E. Kaufmann, Anu Kauppinen, Gur P. Kaushal, Susmita Kaushik, Kiyoshi Kawasaki, Kemal Kazan, Po-Yuan Ke, Damien J. Keating, Ursula Keber, John H. Kehrl, Kate E. Keller, Christian W. Keller, Jongsook Kim Kemper, Candia M. Kenific, Oliver Kepp, Stephanie Kermorgant, Andreas Kern, Robin Ketteler, Tom G. Keulers, Boris Khalfin, Hany Khalil, Bilon Khambu, Shahid Y. Khan, Vinoth Kumar Megraj Khandelwal, Rekha Khandia, Widuri Kho, Noopur Khobrekar, Sataree Khuansuwan, Mukhran Khundadze, Samuel A. Killackey, Dasol Kim, Deok Ryong Kim, Do-Hyung Kim, Dong-Eun Kim, Eun Young Kim, Eun-Kyoung Kim, HakRim Kim, Hee-Sik Kim, Hyung-Ryong Kim, Jeong Hun Kim, Jin Kyung Kim, Jin-Hoi Kim, Joungmok Kim, Ju Hwan Kim, Keun Il Kim, Peter K. Kim, Seong-Jun Kim, Scot R. Kimball, Adi Kimchi, Alec C. Kimmelman, Tomonori Kimura, Matthew A. King, Kerri J. Kinghorn, Conan G. Kinsey, Vladimir Kirkin, Lorrie A. Kirshenbaum, Sergey L. Kiselev, Shuji Kishi, Katsuhiko Kitamoto, Yasushi Kitaoka, Kaio Kitazato, Richard N. Kitsis, Josef T. Kittler, Ole Kjaerulff, Peter S. Klein, Thomas Klopstock, Jochen Klucken, Helene Knovelsrud, Roland L. Knorr, Ben C. B. Ko, Fred Ko, JiunnLiang Ko, Hotaka Kobayashi, Satoru Kobayashi, Ina Koch, Jan C. Koch, Ulrich Koenig, Donat Kogel, Young Ho Koh, Masato Koike, Sepp D. Kohlwein, Nur M. Kocaturk, Masaaki Komatsu, Jeannette Konig, Toru Kono, Benjamin T. Kopp, Tamas Korcsmaros, Gozde Korkmaz, Viktor Korolchuk, Monica Suarez Korsnes, Ali Koskela, Janaiah Kota, Yaichiro Kotake, Monica L. Kotler, Yanjun Kou, Michael Koukourakis, Evangelos Koustas, Attila L. Kovacs, Tibor Kovacs, Daisuke Koya, Tomohiro Kozako, Claudine Kraft, Dimitri Krainc, Helmut Kramer, Anna D. Krasnodembskaya, Carole Kretz-Remy, Guido Kroemer, Nicholas T. Ktistakis, Kazuyuki Kuchitsu, Sabine Kuenen, Lars Kuerschner, Thomas Kukar, Ajay Kumar, Ashok Kumar, Deepak Kumar, Dhiraj Kumar, Sharad Kumar, Shinji Kume, Caroline Kumsta, Chanakya N. Kundu, Mondira Kundu, Ajaikumar B. Kunnumakkara, Lukasz Kurgan, Tatiana G. Kutateladze, Ozlem Kutlu, SeongAe Kwak, Ho Jeong Kwon, Taeg Kyu Kwon, Yong Tae Kwon, Irene Kyrmizi, Albert La Spada, Patrick Labonte, Sylvain Ladoire, Ilaria Laface, Frank Lafont, Diane C. Lagace, Vikramjit Lahiri, Zhibing Lai, Angela S. Laird, Aparna Lakkaraju, Trond Lamark, Sheng-Hui Lan, Ane Landajuela, Darius J. R. Lane, Jon D. Lane, Charles H. Lang, Carsten Lange, Rupert Langer, Pierre Lapaquette, Jocelyn Laporte, Nicholas F. LaRusso, Isabel Lastres-Becker, Wilson Chun Yu Lau, Gordon W. Laurie, Sergio Lavandero, Betty Yuen Kwan Law, Helen Ka-wai Law, Rob Layfield, Weidong Le, Herve Le Stunff, Alexandre Y. Leary, Jean-Jacques Lebrun, Lionel Y. W. Leck, Jean-Philippe Leduc-Gaudet, Changwook Lee, Chung-Pei Lee, Da-Hye Lee, Edward B. Lee, Erinna F. Lee, Gyun Min Lee, He-Jin Lee, Heung Kyu Lee, Jae Man Lee, Jason S. Lee, Jin-A Lee, Joo-Yong Lee, Jun Hee Lee, Michael Lee, Min Goo Lee, Min Jae Lee, Myung-Shik Lee, Sang Yoon Lee, Seung-Jae Lee, Stella Y. Lee, Sung Bae Lee, Won Hee Lee, Ying-Ray Lee, Yong-ho Lee, Youngil Lee, Christophe Lefebvre, Renaud Legouis, Yu L. Lei, Yuchen Lei, Sergey Leikin, Gerd Leitinger, Leticia Lemus, Shuilong Leng, Olivia Lenoir, Guido Lenz, Heinz Josef Lenz, Paola Lenzi, Yolanda Leon, Andreia M. Leopoldino, Christoph Leschczyk, Stina Leskela, Elisabeth Letellier, Chi-Ting Leung, Po Sing Leung, Jeremy S. Leventhal, Beth Levine, Patrick A. Lewis, Klaus Ley, Bin Li, Da-Qiang Li, Jianming Li, Jing Li, Jiong Li, Ke Li, Liwu Li, Mei Li, Min Li, Min Li, Ming Li, Mingchuan Li, Pin-Lan Li, MingQing Li, Qing Li, Sheng Li, Tiangang Li, Wei Li, Wenming Li, Xue Li, Yi-Ping Li, Yuan Li, Zhiqiang Li, Zhiyong Li, Zhiyuan Li, Jiqin Lian, Chengyu Liang, Qiangrong Liang, Weicheng Liang, Yongheng Liang, YongTian Liang, Guanghong Liao, Lujian Liao, Mingzhi Liao, Yung-Feng Liao, Mariangela Librizzi, Pearl P. Y. Lie, Mary A. Lilly, Hyunjung J. Lim, Thania R. R. Lima, Federica Limana, Chao Lin, Chih-Wen Lin, Dar-Shong Lin, Fu-Cheng Lin, Jiandie D. Lin, Kurt M. Lin, Kwang-Huei Lin, Liang-Tzung Lin, Pei-Hui Lin, Qiong Lin, Shaofeng Lin, Su-Ju Lin, Wenyu Lin, Xueying Lin, Yao-Xin Lin, Yee-Shin Lin, Rafael Linden, Paula Lindner, Shuo-Chien Ling, Paul Lingor, Amelia K. Linnemann, YihCherng Liou, Marta M. Lipinski, Saska Lipovsek, Vitor A. Lira, Natalia Lisiak, Paloma B. Liton, Chao Liu, Ching-Hsuan Liu, Chun-Feng Liu, Cui Hua Liu, Fang Liu, Hao Liu, Hsiao-Sheng Liu, Hua-feng Liu, Huifang Liu, Jia Liu, Jing Liu, Julia Liu, Leyuan Liu, Longhua Liu, Meilian Liu, Qin Liu, Wei Liu, Wende Liu, Xiao-Hong Liu, Xiaodong Liu, Xingguo Liu, Xu Liu, Xuedong Liu, Yanfen Liu, Yang Liu, Yang Liu, Yueyang Liu, Yule Liu, J. Andrew Livingston, Gerard Lizard, Jose M. Lizcano, Senka Ljubojevic-Holzer, Matilde E. LLeonart, David Llobet-Navas, Alicia Llorente, Chih Hung Lo, Damian Lobato-Marquez, Qi Long, Yun Chau Long, Ben Loos, Julia A. Loos, Manuela G. Lopez, Guillermo Lopez-Domenech, Jose Antonio Lopez-Guerrero, Ana T. Lopez-Jimenez, Israel Lopez-Valero, Magdalena J. Lorenowicz, Mar Lorente, Peter Lorincz, Laura Lossi, Sophie Lotersztajn, Penny E. Lovat, Jonathan F. Lovell, Alenka Lovy, Guang Lu, Haocheng Lu, Jia-Hong Lu, Jin-Jian Lu, Mengji Lu, Shuyan Lu, Alessandro Luciani, John M. Lucocq, Paula Ludovico, Micah A. Luftig, Morten Luhr, Diego Luis-Ravelo, Julian J. Lum, Liany Luna-Dulcey, Anders H. Lund, Viktor K. Lund, Jan D. Lunemann, Patrick Luningschror, Honglin Luo, Rongcan Luo, Shouqing Luo, Zhi Luo, Claudio Luparello, Bernhard Luscher, Luan Luu, Alex Lyakhovich, Konstantin G. Lyamzaev, Alf Hakon Lystad, Lyubomyr Lytvynchuk, Alvin C. Ma, Changle Ma, Mengxiao Ma, Ning-Fang Ma, Quan-Hong Ma, Xinliang Ma, Yueyun Ma, Zhenyi Ma, Ormond A. MacDougald, Fernando Macian, Gustavo C. MacIntosh, Jeffrey P. MacKeigan, Kay F. Macleod, Sandra Maday, Frank Madeo, Muniswamy Madesh, Tobias Madl, Julio Madrigal-Matute, Akiko Maeda, Yasuhiro Maejima, Marta Magarinos, Poornima Mahavadi, Emiliano Maiani, Kenneth Maiese, Panchanan Maiti, Maria Chiara Maiuri, Barbara Majello, Michael B. Major, Elena Makareeva, Fayaz Malik, Karthik Mallilankaraman, Walter Malorni, Alina Maloyan, Najiba Mammadova, Gene Chi Wai Man, Federico Manai, Joseph D. Mancias, Eva-Maria Mandelkow, Michael A. Mandell, Angelo A. Manfredi, Masoud H. Manjili, Ravi Manjithaya, Patricio Manque, Bella B. Manshian, Raquel Manzano, Claudia Manzoni, Kai Mao, Cinzia Marchese, Sandrine Marchetti, Anna Maria Marconi, Fabrizio Marcucci, Stefania Mardente, Olga A. Mareninova, Marta Margeta, Muriel Mari, Sara Marinelli, Oliviero Marinelli, Guillermo Marino, Sofia Mariotto, Richard S. Marshall, Mark R. Marten, Sascha Martens, Alexandre P. J. Martin, Katie R. Martin, Sara Martin, Shaun Martin, Adrian Martin-Segura, Miguel A. Martin-Acebes, Inmaculada Martin-Burriel, Marcos Martin-Rincon, Paloma Martin-Sanz, Jose A. Martina, Wim Martinet, Aitor Martinez, Ana Martinez, Jennifer Martinez, Moises Martinez Velazquez, Nuria Martinez-Lopez, Marta Martinez-Vicente, Daniel O. Martins, Ulo Lange, Oscar Lopez-Perez, Joilson O. Martins, Waleska K. Martins, Tania Martins-Marques, Emanuele Marzetti, Shashank Masaldan, Celine Masclaux-Daubresse, Douglas G. Mashek, Valentina Massa, Lourdes Massieu, Glenn R. Masson, Laura Masuelli, Anatoliy Masyuk, Tetyana Masyuk, Paola Matarrese, Ander Matheu, Satoaki Matoba, Sachiko Matsuzaki, Pamela Mattar, Alessandro Matte, Domenico Mattoscio, Jose L. Mauriz, Mario Mauthe, Caroline Mauvezin, Emanual Maverakis, Paola Maycotte, Johanna Mayer, Gianluigi Mazzoccoli, Cristina Mazzoni, Joseph R. Mazzulli, Nami McCarty, Christine McDonald, Mitchell R. McGill, Sharon L. McKenna, BethAnn McLaughlin, Fionn McLoughlin, Mark A. McNiven, Thomas G. McWilliams, Fatima Mechta-Grigoriou, Tania Catarina Medeiros, Diego L. Medina, Lynn A. Megeney, Klara Megyeri, Maryam Mehrpour, Jawahar L. Mehta, Alfred J. Meijer, Annemarie H. Meijer, Jakob Mejlvang, Alicia Melendez, Annette Melk, Gonen Memisoglu, Alexandrina F. Mendes, Delong Meng, Fei Meng, Tian Meng, Rubem Menna-Barreto, Manoj B. Menon, Carol Mercer, Anne E. Mercier, Jean-Louis Mergny, Adalberto Merighi, Seth D. Merkley, Giuseppe Merla, Volker Meske, Ana Cecilia Mestre, Shree Padma Metur, Christian Meyer, Hemmo Meyer, Wenyi Mi, Jeanne Mialet-Perez, Junying Miao, Lucia Micale, Yasuo Miki, Enrico Milan, Dana L. Miller, Samuel Miller, Silke Miller, Steven W. Millward, Ira Milosevic, Elena A. Minina, Hamed Mirzaei, Hamid Reza Mirzaei, Mehdi Mirzaei, Amit Mishra, Nandita Mishra, Paras Kumar Mishra, Maja Misirkic Marjanovic, Roberta Misasi, Amit Misra, Gabriella Misso, Claire Mitchell, Geraldine Mitou, Tetsuji Miura, Shigeki Miyamoto, Makoto Miyazaki, Mitsunori Miyazaki, Taiga Miyazaki, Keisuke Miyazawa, Noboru Mizushima, Trine H. Mogensen, Baharia Mograbi, Reza Mohammadinejad, Yasir Mohamud, Abhishek Mohanty, Sipra Mohapatra, Torsten Mohlmann, Asif Mohmmed, Anna Moles, Kelle H. Moley, Maurizio Molinari, Vincenzo Mollace, Andreas Buch Muller, Bertrand Mollereau, Faustino Mollinedo, Costanza Montagna, Mervyn J. Monteiro, Andrea Montella, L. Ruth Montes, Barbara Montico, Vinod K. Mony, Giacomo Monzio Compagnoni, Michael N. Moore, Mohammad A. Moosavi, Ana L. Mora, Marina Mora, David Morales-Alamo, Rosario Moratalla, Paula Moreira, Elena Morelli, Sandra Moreno, Daniel Moreno-Blas, Viviana Moresi, Benjamin Morga, Alwena H. Morgan, Fabrice Morin, Hideaki Morishita, Orson L. Moritz, Mariko Moriyama, Yuji Moriyasu, Manuela Morleo, Eugenia Morselli, Jose F. Moruno-Manchon, Jorge Moscat, Serge Mostowy, Elisa Motori, Andrea Felinto Moura, Naima Moustaid-Moussa, Maria Mrakovcic, Gabriel MucinoHernandez, Anupam Mukherjee, Subhadip Mukhopadhyay, Jean M. Mulcahy Levy, Victoriano Mulero, Sylviane Muller, Christian Munch, Ashok Munjal, Pura Munoz-Canoves, Teresa Munoz-Galdeano, Christian Munz, Tomokazu Murakawa, Claudia Muratori, Brona M. Murphy, J. Patrick Murphy, Aditya Murthy, Timo T. Myohanen, Indira U. Mysorekar, Jennifer Mytych, Seyed Mohammad Nabavi, Massimo Nabissi, Peter Nagy, Jihoon Nah, Aimable Nahimana, Ichiro Nakagawa, Ken Nakamura, Hitoshi Nakatogawa, Shyam S. Nandi, Meera Nanjundan, Monica Nanni, Gennaro Napolitano, Roberta Nardacci, Masashi Narita, Melissa Nassif, Ilana Nathan, Manabu Natsumeda, Ryno J. Naude, Christin Naumann, Olaia Naveiras, Fatemeh Navid, Steffan T. Nawrocki, Taras Y. Nazarko, Francesca Nazio, Florentina Negoita, Thomas Neill, Amanda L. Neisch, Luca M. Neri, Mihai G. Netea, Patrick Neubert, Thomas P. Neufeld, Dietbert Neumann, Albert Neutzner, Phillip T. Newton, Paul A. Ney, Ioannis P. Nezis, Charlene C. W. Ng, Tzi Bun Ng, Hang T. T. Nguyen, Long T. Nguyen, Hong-Min Ni, Cliona Ni Cheallaigh, Zhenhong Ni, M. Celeste Nicolao, Francesco Nicoli, Manuel Nieto-Diaz, Per Nilsson, Shunbin Ning, Rituraj Niranjan, Hiroshi Nishimune, Mireia Niso-Santano, Ralph A. Nixon, Annalisa Nobili, Clevio Nobrega, Takeshi Noda, Uxia Nogueira-Recalde, Trevor M. Nolan, Ivan Nombela, Ivana Novak, Beatriz Novoa, Takashi Nozawa, Nobuyuki Nukina, Carmen Nussbaum-Krammer, Jesper Nylandsted, ,

Summary: The guidelines presented in this article aim to assist researchers in selecting and interpreting methods to examine autophagy, as well as to help reviewers provide constructive critiques of reports focused on these processes. It emphasizes that no single assay is perfect for every situation, and multiple techniques may be needed to properly monitor autophagy in different experimental settings. The article also highlights the importance of targeting multiple autophagy-related genes in genetic approaches to block autophagy effectively.

AUTOPHAGY (2021)

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Review Medicine, Research & Experimental

Selective autophagy of intracellular organelles: recent research advances

Wen Li, Pengcheng He, Yuge Huang, Yi-Fang Li, Jiahong Lu, Min Li, Hiroshi Kurihara, Zhuo Luo, Tian Meng, Mashun Onishi, Changle Ma, Lei Jiang, Yongquan Hu, Qing Gong, Dongxing Zhu, Yiming Xu, Rong Liu, Lei Liu, Cong Yi, Yushan Zhu, Ningfang Ma, Koji Okamoto, Zhiping Xie, Jinbao Liu, Rong-Rong He, Du Feng

Summary: Autophagy is a physiological process that degrades over-abundant or damaged organelles via the lysosomal system, induced by stress and occurring in both non-selective and selective manners. Selective autophagy plays a crucial role in maintaining cellular homeostasis and its dysfunction is implicated in various diseases.

THERANOSTICS (2021)

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Article Chemistry, Medicinal

Design and synthesis of a library of C2-substituted sulfamidoadenosines to probe bacterial permeability

Shibin Zhao, Julian Maceren, Mia Chung, Samantha Stone, Raphael Geiben, Melissa L. Boby, Bradley S. Sherborne, Derek S. Tan

Summary: Antibiotic resistance is a major threat to public health, with Gram-negative bacteria presenting unique challenges due to their low permeability and efflux pumps. Limited understanding of the chemical rules for overcoming these barriers hinders antibacterial drug discovery. Efforts to address this issue, such as screening compound libraries and using cheminformatic analysis, have led to the design of sulfamidoadenosines with diverse substituents, showing potential utility in accumulation in Escherichia coli.

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2024)

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Article Chemistry, Medicinal

Design of MERS-CoV entry inhibitory short peptides based on helix-stabilizing strategies

Jichun Li, Qing Li, Shuai Xia, Jiahuang Tu, Longbo Zheng, Qian Wang, Shibo Jiang, Chao Wang

Summary: This study successfully developed a short peptide mimetic as a MERS-CoV fusion inhibitor by reproducing the key recognition features of the HR2 helix. The resulting 23-mer lipopeptide showed comparable inhibitory effect to the 36-mer HR2 peptide HR2P-M2. This has important implications for developing short peptide-based antiviral agents to treat MERS-CoV infection.

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2024)

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Article Chemistry, Medicinal

Development of novel β2-adrenergic receptor agonists for the stimulation of glucose uptake - The importance of chirality and ring size of cyclic amines

Krista Jaunsleine, Linda Supe, Jana Spura, Sten van Beek, Anna Sandstrom, Jessica Olsen, Carina Halleskog, Tore Bengtsson, Ilga Mutule, Benjamin Pelcman

Summary: Beta(2)-adrenergic receptor agonists can stimulate glucose uptake by skeletal muscle cells and are therefore potential treatments for type 2 diabetes. The chirality of compounds has a significant impact on the activity of these agonists. This study found that certain synthesized compounds showed higher glucose uptake activity. These findings provide important information for the design of novel beta(2)AR agonists for T2D treatment.

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2024)

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Article Chemistry, Medicinal

Conformationally constrained potent inhibitors for enhancer of zeste homolog 2 (EZH2)

Xin Xu, Jia Chen, Guan Wang, Xiaojuan Zhang, Qiang Li, Xiaobo Zhou, Fengying Guo, Min Li

Summary: The study focuses on EZH2, a promising therapeutic target for various types of cancers. Researchers designed and synthesized a series of novel derivatives aiming to enhance the EZH2 inhibition activity. Among them, compound 28 displayed potent EZH2 inhibition activity and showed high anti-proliferative effects in lymphoma cell lines and xenograft mouse models. The study suggests that compound 28 has potential as a therapeutic candidate for EZH2-associated cancers.

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2024)

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Article Chemistry, Medicinal

The potential of Rhein's aromatic amines for Parkinson's disease prevention and treatment: α-Synuclein aggregation inhibition and disaggregation of preformed fibers

Wei Zhang, Wei Liu, Ya-Dong Zhao, Li-Zi Xing, Ji Xu, Rui-Jun Li, Yun-Xiao Zhang

Summary: This study developed a series of aromatic amide derivatives based on Rhein and investigated their inhibitory activity against alpha-Syn aggregation. Two of these compounds showed promising potential in treating Parkinson's disease by stabilizing alpha-Syn's conformation and disassembling alpha-Syn oligomers and fibrils.

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2024)

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Article Chemistry, Medicinal

Design, synthesis and biological evaluation of novel cationic liposomes loaded with melphalan for the treatment of cancer

Mani Sharma, S. S. S. S. Sudha Ambadipudi, Neeraj Kumar Chouhan, V. Lakshma Nayak, Srihari Pabbaraja, Sai Balaji Andugulapati, Ramakrishna Sistla

Summary: Therapeutically active lipids in drug delivery systems can enhance the safety and efficacy of treatment. The liposome formulation created using synthesized biologically active lipids showed additive anti-cancer effects and reduced tumorigenic potential.

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2024)

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