Thapsigargin-From Traditional Medicine to Anticancer Drug

被引：88

作者：

Jaskulska, Agata ^{[1
,2
]}

Janecka, Anna Ewa ^{[2
]}

Gach-Janczak, Katarzyna ^{[2
]}

机构：

[1] Lodz Univ Technol, Inst Organ Chem, Zeromskiego 116, PL-90924 Lodz, Poland

[2] Med Univ Lodz, Dept Biomol Chem, Mazowiecka 6-8, PL-92215 Lodz, Poland

来源：

INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES | 2021年 / 22卷 / 01期

关键词：

thapsigargin; cytotoxin; anticancer activity; sarcoplasmic/endoplasmic reticulum Ca2+ ATPase; unfold protein response; apoptosis; prodrug; prostate-specific antigen; prostate-specific membrane antigen; mipsagargin; ENDOPLASMIC-RETICULUM STRESS; UNFOLDED-PROTEIN-RESPONSE; PROSTATE-SPECIFIC ANTIGEN; ER CA2+ DEPLETION; CELL-DEATH; THERAPEUTIC TARGET; INDUCED APOPTOSIS; NATURAL-PRODUCTS; TROJAN HORSE; SERCA PUMP;

D O I：

10.3390/ijms22010004

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

A sesquiterpene lactone, thapsigargin, is a phytochemical found in the roots and fruits of Mediterranean plants from Thapsia L. species that have been used for centuries in folk medicine to treat rheumatic pain, lung diseases, and female infertility. More recently thapsigargin was found to be a potent cytotoxin that induces apoptosis by inhibiting the sarcoplasmic/endoplasmic reticulum Ca2+ ATPase (SERCA) pump, which is necessary for cellular viability. This biological activity encouraged studies on the use of thapsigargin as a novel antineoplastic agent, which were, however, hampered due to high toxicity of this compound to normal cells. In this review, we summarized the recent knowledge on the biological activity and molecular mechanisms of thapsigargin action and advances in the synthesis of less-toxic thapsigargin derivatives that are being developed as novel anticancer drugs.

引用

页码：1 / 12

页数：12

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