Antitumor Activity of New Olivacine Derivatives
Olivacine is an alkaloid-containing pyridocarbazole structure. It is isolated from the bark of the evergreen timber tree, <i>Aspidosperma olivaceum.</i> Its well-documented anticancer activity led to the synthesis of new derivatives, which are semisynthetic and fully synthetic pyridocarb...
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MDPI AG
2020-05-01
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| Series: | Molecules |
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| Online Access: | https://www.mdpi.com/1420-3049/25/11/2512 |
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| author | Janusz Piasny Benita Wiatrak Agnieszka Dobosz Beata Tylińska Tomasz Gębarowski |
| author_facet | Janusz Piasny Benita Wiatrak Agnieszka Dobosz Beata Tylińska Tomasz Gębarowski |
| author_sort | Janusz Piasny |
| collection | DOAJ |
| description | Olivacine is an alkaloid-containing pyridocarbazole structure. It is isolated from the bark of the evergreen timber tree, <i>Aspidosperma olivaceum.</i> Its well-documented anticancer activity led to the synthesis of new derivatives, which are semisynthetic and fully synthetic pyridocarbazoles. This study aimed to evaluate the potential antineoplastic activity of four newly synthesized olivacine derivatives. Multidrug resistance is a common phenomenon causing failure in the chemotherapy of many tumors. It is mainly related to increased function of P-glycoprotein, an efflux pump removing cytostatic out of the cells. The cell lines used in the study were colorectal carcinoma cell lines: LoVo (doxorubicin-sensitive) and LoVo/DX (doxorubicin-resistant). The NHDF cell line was used to assess cell viability. First, the cells were incubated with olivacine derivatives. In the next step, the following assays were performed: DCF-DA assay, MTT assay, rhodamine 123 assay, detection of apoptosis, proliferation inhibition-mitotic index. The tested compounds showed higher antineoplastic potential and lower toxicity than the reference compound ellipticine. The results indicate that the new olivacine derivatives are good candidates for future anticancer drugs. |
| first_indexed | 2024-03-10T19:33:03Z |
| format | Article |
| id | doaj.art-c5bf23961b0d4b85945766544c8c1be9 |
| institution | Directory Open Access Journal |
| issn | 1420-3049 |
| language | English |
| last_indexed | 2024-03-10T19:33:03Z |
| publishDate | 2020-05-01 |
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| spelling | doaj.art-c5bf23961b0d4b85945766544c8c1be92023-11-20T02:00:47ZengMDPI AGMolecules1420-30492020-05-012511251210.3390/molecules25112512Antitumor Activity of New Olivacine DerivativesJanusz Piasny0Benita Wiatrak1Agnieszka Dobosz2Beata Tylińska3Tomasz Gębarowski4Department of Basic Medical Sciences, Wroclaw Medical University, 50-556 Wroclaw, PolandDepartment of Basic Medical Sciences, Wroclaw Medical University, 50-556 Wroclaw, PolandDepartment of Basic Medical Sciences, Wroclaw Medical University, 50-556 Wroclaw, PolandDepartment of Organic Chemistry, Wroclaw Medical University, 50-556 Wroclaw, PolandDepartment of Basic Medical Sciences, Wroclaw Medical University, 50-556 Wroclaw, PolandOlivacine is an alkaloid-containing pyridocarbazole structure. It is isolated from the bark of the evergreen timber tree, <i>Aspidosperma olivaceum.</i> Its well-documented anticancer activity led to the synthesis of new derivatives, which are semisynthetic and fully synthetic pyridocarbazoles. This study aimed to evaluate the potential antineoplastic activity of four newly synthesized olivacine derivatives. Multidrug resistance is a common phenomenon causing failure in the chemotherapy of many tumors. It is mainly related to increased function of P-glycoprotein, an efflux pump removing cytostatic out of the cells. The cell lines used in the study were colorectal carcinoma cell lines: LoVo (doxorubicin-sensitive) and LoVo/DX (doxorubicin-resistant). The NHDF cell line was used to assess cell viability. First, the cells were incubated with olivacine derivatives. In the next step, the following assays were performed: DCF-DA assay, MTT assay, rhodamine 123 assay, detection of apoptosis, proliferation inhibition-mitotic index. The tested compounds showed higher antineoplastic potential and lower toxicity than the reference compound ellipticine. The results indicate that the new olivacine derivatives are good candidates for future anticancer drugs.https://www.mdpi.com/1420-3049/25/11/2512pyridocarbazoleolivacineP-glycoproteinmultiple drug resistance |
| spellingShingle | Janusz Piasny Benita Wiatrak Agnieszka Dobosz Beata Tylińska Tomasz Gębarowski Antitumor Activity of New Olivacine Derivatives Molecules pyridocarbazole olivacine P-glycoprotein multiple drug resistance |
| title | Antitumor Activity of New Olivacine Derivatives |
| title_full | Antitumor Activity of New Olivacine Derivatives |
| title_fullStr | Antitumor Activity of New Olivacine Derivatives |
| title_full_unstemmed | Antitumor Activity of New Olivacine Derivatives |
| title_short | Antitumor Activity of New Olivacine Derivatives |
| title_sort | antitumor activity of new olivacine derivatives |
| topic | pyridocarbazole olivacine P-glycoprotein multiple drug resistance |
| url | https://www.mdpi.com/1420-3049/25/11/2512 |
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