Thapsigargin—From Traditional Medicine to Anticancer Drug
A sesquiterpene lactone, thapsigargin, is a phytochemical found in the roots and fruits of Mediterranean plants from <i>Thapsia</i> L. species that have been used for centuries in folk medicine to treat rheumatic pain, lung diseases, and female infertility. More recently thapsigargin was...
| Main Authors: | , , |
|---|---|
| Format: | Article |
| Language: | English |
| Published: |
MDPI AG
2020-12-01
|
| Series: | International Journal of Molecular Sciences |
| Subjects: | |
| Online Access: | https://www.mdpi.com/1422-0067/22/1/4 |
| _version_ | 1797543930835763200 |
|---|---|
| author | Agata Jaskulska Anna Ewa Janecka Katarzyna Gach-Janczak |
| author_facet | Agata Jaskulska Anna Ewa Janecka Katarzyna Gach-Janczak |
| author_sort | Agata Jaskulska |
| collection | DOAJ |
| description | A sesquiterpene lactone, thapsigargin, is a phytochemical found in the roots and fruits of Mediterranean plants from <i>Thapsia</i> 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 Ca<sup>2+</sup> 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. |
| first_indexed | 2024-03-10T13:52:27Z |
| format | Article |
| id | doaj.art-99bbd25b6a48458e82e8c88fe3fe0722 |
| institution | Directory Open Access Journal |
| issn | 1661-6596 1422-0067 |
| language | English |
| last_indexed | 2024-03-10T13:52:27Z |
| publishDate | 2020-12-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | International Journal of Molecular Sciences |
| spelling | doaj.art-99bbd25b6a48458e82e8c88fe3fe07222023-11-21T01:59:54ZengMDPI AGInternational Journal of Molecular Sciences1661-65961422-00672020-12-01221410.3390/ijms22010004Thapsigargin—From Traditional Medicine to Anticancer DrugAgata Jaskulska0Anna Ewa Janecka1Katarzyna Gach-Janczak2Institute of Organic Chemistry, Lodz University of Technology, Żeromskiego 116, 90-924 Lodz, PolandDepartment of Biomolecular Chemistry, Medical University of Lodz, Mazowiecka 6/8, 92-215 Lodz, PolandDepartment of Biomolecular Chemistry, Medical University of Lodz, Mazowiecka 6/8, 92-215 Lodz, PolandA sesquiterpene lactone, thapsigargin, is a phytochemical found in the roots and fruits of Mediterranean plants from <i>Thapsia</i> 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 Ca<sup>2+</sup> 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.https://www.mdpi.com/1422-0067/22/1/4thapsigargincytotoxinanticancer activitysarcoplasmic/endoplasmic reticulum Ca<sup>2+</sup> ATPaseunfold protein responseapoptosis |
| spellingShingle | Agata Jaskulska Anna Ewa Janecka Katarzyna Gach-Janczak Thapsigargin—From Traditional Medicine to Anticancer Drug International Journal of Molecular Sciences thapsigargin cytotoxin anticancer activity sarcoplasmic/endoplasmic reticulum Ca<sup>2+</sup> ATPase unfold protein response apoptosis |
| title | Thapsigargin—From Traditional Medicine to Anticancer Drug |
| title_full | Thapsigargin—From Traditional Medicine to Anticancer Drug |
| title_fullStr | Thapsigargin—From Traditional Medicine to Anticancer Drug |
| title_full_unstemmed | Thapsigargin—From Traditional Medicine to Anticancer Drug |
| title_short | Thapsigargin—From Traditional Medicine to Anticancer Drug |
| title_sort | thapsigargin from traditional medicine to anticancer drug |
| topic | thapsigargin cytotoxin anticancer activity sarcoplasmic/endoplasmic reticulum Ca<sup>2+</sup> ATPase unfold protein response apoptosis |
| url | https://www.mdpi.com/1422-0067/22/1/4 |
| work_keys_str_mv | AT agatajaskulska thapsigarginfromtraditionalmedicinetoanticancerdrug AT annaewajanecka thapsigarginfromtraditionalmedicinetoanticancerdrug AT katarzynagachjanczak thapsigarginfromtraditionalmedicinetoanticancerdrug |