期刊
PHARMACEUTICALS
卷 15, 期 12, 页码 -出版社
MDPI
DOI: 10.3390/ph15121497
关键词
Buddleja saligna; melanoma; antiproliferative activity; angiogenesis; ex ovo YSM
资金
- University of Pretoria
- National Research Foundation-DAAD
- Department of Science and Innovation [SFD13080220333]
- Innovation Hub [DST/CON 0059/2019]
- L'Oreal-UNESCO
- FCT-MCTES
- [UIDP/04378/2020]
- [UIDB/04378/2020]
Melanoma cells secrete pro-angiogenic factors which play a key role in growth, proliferation, and metastasis. In this study, Buddleja saligna and a triterpenoid mixture were found to inhibit the growth of melanoma cells with minimal effects on normal cells. Additionally, these compounds showed inhibitory effects on vascular endothelial growth factor and interleukins, as well as reducing new blood vessel formation.
Melanoma cells secrete pro-angiogenic factors, which stimulates growth, proliferation and metastasis, and therefore are key therapeutic targets. Buddleja saligna (BS), and an isolated triterpenoid mixture (DT-BS-01) showed a fifty percent inhibitory concentration (IC50) of 33.80 +/- 1.02 and 5.45 +/- 0.19 mu g/mL, respectively, against melanoma cells (UCT-MEL-1) with selectivity index (SI) values of 1.64 and 5.06 compared to keratinocytes (HaCat). Cyclooxygenase-2 (COX-2) inhibition was observed with IC50 values of 35.06 +/- 2.96 (BS) and 26.40 +/- 4.19 mu g/mL (DT-BS-01). BS (30 mu g/mL) significantly inhibited interleukin (IL)-6 (83.26 +/- 17.60%) and IL-8 (100 +/- 0.2%) production, whereas DT-BS-01 (5 mu g/mL) showed 51.07 +/- 2.83 (IL-6) and 0 +/- 6.7% (IL-8) inhibition. Significant vascular endothelial growth factor (VEGF) inhibition, by 15.84 +/- 4.54 and 12.21 +/- 3.48%, respectively, was observed. In the ex ovo chick embryo yolk sac membrane assay (YSM), BS (15 mu g/egg) significantly reduced new blood vessel formation, with 53.34 +/- 11.64% newly formed vessels. Silver and palladium BS nanoparticles displayed noteworthy SI values. This is the first report on the significant anti-angiogenic activity of BS and DT-BS-01 and should be considered for preclinical trials as there are currently no US Food and Drug Administration (FDA) approved drugs to inhibit angiogenesis in melanoma.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据