Affiliation:
1. College of Pharmaceutical Sciences, Anhui Xinhua University, Hefei 230088,China
2. Proctology Department, Nanjing Hospital of Chinese Medicine affiliated to Nanjing University of Chinese Medicine, Nanjing University of Chinese Medicine, Nanjing, 210022,China
Abstract
Background:
Paclitaxel, a natural diterpenoid compound, has anti-tumor effect by acting on tubulin,
whereas coumarin, another kind of natural product, has anti-tumor effect, along with some other effects, such as
anti-bacterial-., Moreover, it also possesses fluorescence.
Objective:
Multi targeting is an effective strategy in drug design to combat tumor. Therefore, a combination of
paclitaxel with other active molecular drugs for exploring the novel lead with multi-functions is in demand.
Materials and Methods:
To synthsize paclitaxel-coumarin conjugate via click chemistry and to investigate anticancer
activity by MTT assay and the scratch test.
Results and Discussion:
The results of MTT assay showed that compared tothe paclitaxel, the anti-tumor activity
of the conjugate was significantly improved. The results of flow cytometry showed that the conjugate had a
stronger ability to induce apoptosis. The scratch test results showed that the conjugate had better anti- metastasis
ability than paclitaxel.
Conclusion:
These findings indicated that paclitaxel and coumarin had a synergistic effect, which paved the way
for the development of paclitaxel through fluorescence.
Funder
Quality Engineering Project of Anhui Xinhua University
Scientific research team of Anhui Xinhua University
Natural Science Research Foundation of the Department of Education of Anhui Province
Publisher
Bentham Science Publishers Ltd.
Subject
Organic Chemistry,Biochemistry
Cited by
3 articles.
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