Cucurbitacins: A Systematic Review of the Phytochemistry and Anticancer Activity.
Cucurbitacins are highly oxidized tetracyclic triterpenoids that are widely present in traditional Chinese medicines (Cucurbitaceae family), possess strong anticancer activity, and are divided into 12 classes from A to T with over 200 derivatives. The eight most active cucurbitacin components against cancer are cucurbitacin B, D, E, I, IIa, L glucoside, Q, and R. Their mechanisms of action include antiproliferation, inhibition of migration and invasion, proapoptosis, and cell cycle arrest promotion. Cucurbitacins are also found to be the inhibitors of JAK-STAT3, Wnt, PI3K/Akt, and MAPK signaling pathways, which play important roles in the apoptosis and survival of cancer cells. Recently, new studies have discovered synergistic anticancer effects by using cucurbitacins together with clinically approved chemotherapeutic drugs, such as docetaxel and methotrexate. This paper provides a summary of recent research progress on the anticancer property of cucurbitacins and the various intracellular signaling pathways involved in the regulation of cancer cell proliferation, death, invasion, and migration. Therefore, cucurbitacins are a class of promising anticancer drugs to be used alone or be intergraded in current chemotherapies and radiotherapies to treat many types of cancers.
* State Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese Medical Sciences, University of Macau, Macau 999078, P.R. China.
Yuee
Y
Cai
† Department of Pediatrics, College of Medicine, University of Florida, Gainesville, FL 32610, USA.
Xiefan
X
Fang
* State Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese Medical Sciences, University of Macau, Macau 999078, P.R. China.
Chengwei
C
He
* State Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese Medical Sciences, University of Macau, Macau 999078, P.R. China.
Peng
P
Li
* State Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese Medical Sciences, University of Macau, Macau 999078, P.R. China.|‡ Department of Pharmacology, School of Medicine, Jinan University, Guangzhou 510632, P.R. China.
Fei
F
Xiao
* State Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese Medical Sciences, University of Macau, Macau 999078, P.R. China.
Yitao
Y
Wang
* State Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese Medical Sciences, University of Macau, Macau 999078, P.R. China.
Meiwan
M
Chen
D000818:Animals; D000972:Antineoplastic Agents, Phytogenic; D017209:Apoptosis / Q000187:drug effects; D059447:Cell Cycle Checkpoints / Q000187:drug effects; D045744:Cell Line, Tumor; D002465:Cell Movement / Q000187:drug effects; D049109:Cell Proliferation / Q000187:drug effects; D002471:Cell Transformation, Neoplastic / Q000187:drug effects; D054728:Cucurbitacins / Q000737:chemistry / Q000145:classification / Q000494:pharmacology* / Q000627:therapeutic use*; D000077143:Docetaxel; D004359:Drug Therapy, Combination; D006801:Humans; D008727:Methotrexate / Q000627:therapeutic use; D008968:Molecular Conformation; D009361:Neoplasm Invasiveness; D009369:Neoplasms / Q000188:drug therapy* / Q000473:pathology*; D008517:Phytotherapy; D015398:Signal Transduction / Q000187:drug effects; D013329:Structure-Activity Relationship; D043823:Taxoids / Q000627:therapeutic use
D000972:Antineoplastic Agents, Phytogenic; D043823:Taxoids; D000077143:Docetaxel; D054728:Cucurbitacins; D008727:Methotrexate
Anticancer; Cucurbitacins; Mechanism; Phytochemistry