Cytotoxic cardenolides from the latex of Calotropis procera.
Three new cardenolides (3, 9 and 10), along with eight known ones, were isolated from the latex of Calotropis procera. The structural determination was accomplished by the 1D- and 2D-NMR spectra as well as HRESIMS analysis. The growth inhibitory activity of the latex and its sub-fractions as well as isolated compounds was evaluated against human A549 and Hela cell lines. The results exhibited that latex had strong growth inhibitory activity with IC50s of (3.37 μM, A-549) and (6.45 μM, Hela). Among the four extracts (hexane, chloroform, ethyl acetate and aqueous), chloroform extract displayed the highest potential cytotoxic activity, with IC50s of (0.985 μM, A-549) and (1.471 μM, Hela). All the isolated compounds displayed various degrees of cytotoxic activity and the highest activity was observed by calactin (1) with IC50s values of (0.036 μM, A-549) and (0.083 μM, Hela). None of these isolated compounds exhibited good antimicrobial activity evaluated by determination of their MICs using the broth microdilution method against various infectious pathogens. The structure-activity relationships for cytotoxic activity were also discussed.
Department of Botany and Microbiology, Faculty of Science, Assiut University, Assiut, Egypt; Department of Biology, Faculty of Science and Art, Samtah, Jazan University, Saudi Arabia.
Nadia H
NH
Mohamed
Key Laboratory of Pathogenic Microbiology and Immunology, Institute of Microbiology, Chinese Academy of Sciences, Beijing 100101, China; University of Chinese Academy of Sciences, Beijing 100049, China; Eskitis Institute, Griffith University, Brisbane, QLD 4111, Australia.
Miaomiao
M
Liu
Pharmacognosy Department, College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia; Pharmacognosy Department, Faculty of Pharmacy, Assiut University, Assiut 71526, Egypt.
Wael M
WM
Abdel-Mageed
Chemistry Department, Science College, Princess Nora Bint Abdul Rahman University, Riyadh 11671, Saudi Arabia.
Lamya H
LH
Alwahibi
Key Laboratory of Pathogenic Microbiology and Immunology, Institute of Microbiology, Chinese Academy of Sciences, Beijing 100101, China.
Huanqin
H
Dai
Department of Botany and Microbiology, Faculty of Science, Assiut University, Assiut, Egypt.
Mady Ahmed
MA
Ismail
Laboratory of Immunology & Molecular Physiology, Zoology Department, Faculty of Science, Assiut University, 71516 Assiut, Egypt.
Gamal
G
Badr
Eskitis Institute, Griffith University, Brisbane, QLD 4111, Australia.
Ronald J
RJ
Quinn
Key Laboratory of Pathogenic Microbiology and Immunology, Institute of Microbiology, Chinese Academy of Sciences, Beijing 100101, China. Electronic address: zhanglixin@im.ac.cn.
Xueting
X
Liu
Key Laboratory of Pathogenic Microbiology and Immunology, Institute of Microbiology, Chinese Academy of Sciences, Beijing 100101, China. Electronic address: liuxueting_cn@hotmail.com.
Lixin
L
Zhang
Department of Botany and Microbiology, Faculty of Science, Assiut University, Assiut, Egypt. Electronic address: ashoreit1968@yahoo.com.
Ahmed A M
AA
Shoreit
D000900:Anti-Bacterial Agents / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D000935:Antifungal Agents / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D000972:Antineoplastic Agents, Phytogenic / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D001419:Bacteria / Q000187:drug effects; D031107:Calotropis / Q000737:chemistry*; D002298:Cardenolides / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D005658:Fungi / Q000187:drug effects; D006367:HeLa Cells; D006801:Humans; D007840:Latex / Q000737:chemistry*; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D013329:Structure-Activity Relationship
D000900:Anti-Bacterial Agents; D000935:Antifungal Agents; D000972:Antineoplastic Agents, Phytogenic; D002298:Cardenolides; D007840:Latex
Antimicrobial activity; Asclepiadaceae; Calotropis procera; Cardenolides; Cytotoxicity