http://jcps.bjmu.edu.cn

中国药学(英文版) ›› 2019, Vol. 28 ›› Issue (4): 217-228.DOI: 10.5246/jcps.2019.04.022

• 【综 述】 •    下一篇

A synopsis on flavonoids from the roots of Scutellaria baicalensis with some insights on baicalein and its anti-cancer properties

Eric Wei Chiang Chan1*, Siu Kuin Wong2, Joseph Tangah3, Tomomi Inoue4, Hung Tuck Chan5   

  1. 1. Faculty of Applied Sciences, UCSI University, 56000 Cheras, Kuala Lumpur, Malaysia
    2. School of Science, Monash University Sunway, 46150 Petaling Jaya, Selangor, Malaysia
    3. Forest Research Centre, Sabah Forestry Department, Sandakan 90009, Sabah, Malaysia
    4. Centre for Environmental Biology and Ecosystem Studies, National Institute for Environmental Studies (NIES), Onogawa, Tsukuba 305-0053, Japan
    5. Secretariat of the International Society for Mangrove Ecosystems, Faculty of Agriculture, University of the Ryukyus, Okinawa 903-0129, Japan
  • 收稿日期:2018-12-15 修回日期:2019-01-31 出版日期:2019-04-30 发布日期:2019-03-22
  • 通讯作者: Tel.: +60-3-9101-8880, E-mail: chanwc@ucsiuniversity.edu.my, erchan@yahoo.com

A synopsis on flavonoids from the roots of Scutellaria baicalensis with some insights on baicalein and its anti-cancer properties

Eric Wei Chiang Chan1*, Siu Kuin Wong2, Joseph Tangah3, Tomomi Inoue4, Hung Tuck Chan5   

  1. 1. Faculty of Applied Sciences, UCSI University, 56000 Cheras, Kuala Lumpur, Malaysia
    2. School of Science, Monash University Sunway, 46150 Petaling Jaya, Selangor, Malaysia
    3. Forest Research Centre, Sabah Forestry Department, Sandakan 90009, Sabah, Malaysia
    4. Centre for Environmental Biology and Ecosystem Studies, National Institute for Environmental Studies (NIES), Onogawa, Tsukuba 305-0053, Japan
    5. Secretariat of the International Society for Mangrove Ecosystems, Faculty of Agriculture, University of the Ryukyus, Okinawa 903-0129, Japan
  • Received:2018-12-15 Revised:2019-01-31 Online:2019-04-30 Published:2019-03-22
  • Contact: Tel.: +60-3-9101-8880, E-mail: chanwc@ucsiuniversity.edu.my, erchan@yahoo.com

摘要:

Flavones are the most dominant type of flavonoids isolated from the roots of Scutellaria baicalensis (Radix Scutellariae),which is a traditional medicinal plant in East Asian countries, including China, Japan and Korea. Most of the flavones are derivativeswith methoxyl and hydroxyl groups, and they include baicalein, baicalin, chrysin, norwogonin, oroxylin A and wogonin. Baicalein possesses anti-cancer activities against a wide spectrum of human cancer cells by inducing apoptosis and cell cycle arrest, and by inhibiting angiogenesis, metastasis and inflammation. Some examples of the effects of baicalein on apoptosis, cell cycle arrest and metastasis are presented with discussion on the molecular targets and pathways. Studies on the structure-activity relationships of flavonoid cytotoxicity towards human cancer cells show that the potent cytotoxic activities of baicalein can be attributed to its -OH groupsat C5, C6 and C7 (triple hydroxylation) of ring A, carbonyl group at C4 of ring C, and C2–C3 double bond of ring C.Studies on structural modifications of baicalein have shown that the configurations at C6 of ring A are critical factors influencing its anti-proliferative activity. Considering the remarkable anti-cancer properties, the future prospects for developing baicalein into an anti-cancer drug are promising.

关键词: Radix Scutellariae, Baicalein, Flavones, Structure-activity relationships

Abstract:

Flavones are the most dominant type of flavonoids isolated from the roots of Scutellaria baicalensis (Radix Scutellariae),which is a traditional medicinal plant in East Asian countries, including China, Japan and Korea. Most of the flavones are derivativeswith methoxyl and hydroxyl groups, and they include baicalein, baicalin, chrysin, norwogonin, oroxylin A and wogonin. Baicalein possesses anti-cancer activities against a wide spectrum of human cancer cells by inducing apoptosis and cell cycle arrest, and by inhibiting angiogenesis, metastasis and inflammation. Some examples of the effects of baicalein on apoptosis, cell cycle arrest and metastasis are presented with discussion on the molecular targets and pathways. Studies on the structure-activity relationships of flavonoid cytotoxicity towards human cancer cells show that the potent cytotoxic activities of baicalein can be attributed to its -OH groupsat C5, C6 and C7 (triple hydroxylation) of ring A, carbonyl group at C4 of ring C, and C2–C3 double bond of ring C.Studies on structural modifications of baicalein have shown that the configurations at C6 of ring A are critical factors influencing its anti-proliferative activity. Considering the remarkable anti-cancer properties, the future prospects for developing baicalein into an anti-cancer drug are promising.

Key words: Radix Scutellariae, Baicalein, Flavones, Structure-activity relationships

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