4.4 Article

In vitro antiproliferative activity of alkaloids isolated from Tabernaemontana catharinensis A.DC (Apocynaceae)

Journal

NATURAL PRODUCT RESEARCH
Volume 36, Issue 22, Pages 5808-5812

Publisher

TAYLOR & FRANCIS LTD
DOI: 10.1080/14786419.2021.2017928

Keywords

Tabernaemontana catharinensis; Apocynaceae; indole alkaloids; antiproliferative activity; affinisine

Funding

  1. CAPES (Coordenacao de Aperfeicoamento de Pessoal de Nivel Superior)
  2. CNPq (Conselho Nacional de Desenvolvimento Cientifico e Tecnologico)

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Four alkaloids were isolated from the stem bark of T. catharinensis and tested for antiproliferative activity in tumor cell lines. The alkaloid affinisine showed the most promising results with cytotoxic effects against various tumor cell strains and high selectivity rates compared to non-tumor cells.
In this work, four alkaloids from the stem bark of T. catharinensis were isolated, namely: voacangine (1); ethyl apovincaminate (2); affinisine (3) and voachalotine (4). The alkaloids were tested in vitro for antiproliferative capacity in eight tumor cell lines: U251 (glioma), MCF-7 (breast), NCI-ADR/RES (drug resistant ovary), 786-0 (kidney), NCI-H460 (lung), HT-29 (colon), K562 (leukemia) and PC-3 (prostate) and a non-tumor keratinocyte cell line (HaCat). Antiproliferative activity was observed after 48 hours and results expressed as the concentration needed to induce 50% growth inhibition (GI50) in mu M. The chemotherapy drug Doxorubicin was used as a standard. The alkaloid affinisine (3) was the most promising, showing moderate inhibition rates in addition to the cytotoxic and cytocidal effect against all strains tested. It also proved to be a very promising compound, showing high selectivity rates when compared to the non-tumor keratinocyte cell line (HaCat).

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