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Research and anti-cancer effects of new indole alkaloid derivatives


Cancer is a group of diseases characterized by uncontrolled development and the spread of abnormal cells. An estimated 14 million new cases of cancer are reported each year worldwide. In 2017, about 600,920 American people die from cancer, with nearly 1,650 deaths each day. Some typical natural compounds, such as alkaloid indole, show significant anti-cancer activity. Periwinkle alkaloid, a family of indole dimer compounds isolated from the periwinkle of Catharanthus roseus, the Apocynaceae family, represents one of the most important anti-cancer layers.

The anti-cancer activity of periwinkle alkaloid was discovered in the 1950s. More than 40 years later, two kinds of drug, vinblastine 1 and vincristine 2, were used on a large scale for cancer treatment. Semi synthetic derivatives, such as vindesine (3; Eldesine®), vinorelbine (4; Navelbine®), and the latest, a fluorine derivative, vinflunine (5; Javlor®) have been studied and put into clinical use. The research efforts are continuing scientists to seek other compounds with lower toxicity and higher treatment ability.


Some periwinkle alkaloid in clinical use

Necessity and links to previous research, a group of scientists from the Vietnam – United Kingdom Center for interdisciplinary excellence research in natural compounds led by Assoc. Prof. Dr. Ngo Quoc Anh, under the Institute of Chemistry, the Vietnam Academy of Science and Technology, carried out the project “Research and anti-cancer effects of new indole alkaloid derivatives”, in order to synthesize new derivatives of periwinkle alkaloid and assess their anti-cancer activity. After 2 years of implementation, the main results achieved were:

• Successfully synthesizing 20 new indole alkaloid compounds from natural periwinkle alkaloid such as catharanthine, vindoline, vinblastine and vincristine; checking on toxic activity on two KB and Hep-G2 cancer cells by the new 20 pathogens. Most substances have good activity levels of 1-10 μM, some substances have activity equivalent to vinblastine (1 - 10 nM) and better than elipcitine.
• Selecting eight highly potent cell toxic compounds on in vitro to simulate links on docking experiment using a number of specialized softwares. Results showed that 02 new periwinkle alkaloid with the strongest toxicity have the strongest affinity for tubulin, the equivalent of vinblastine.

 Simulation of the docking experiment

• Studying in vitro biological mechanism of two chlorochablastine and chlorochacristine compounds on such characters as apoptosis, cell cycle and anti-proliferation, over commercial periwinkle alkaloid medicine such as vinblastine, vincristine, vinorelbine and vinflunine. As a result, the two selected compounds have the same functions as vinflunine, which is a commercially available semi-synthetic periwinkle alkaloid, the latest generation, opening up the possibility of further research for clinical use.


Chlorochablastine and chlorochacristine

The project published an article in ISI journal and two articles in Journal of Chemistry. In addition, the topic contributed to the training of a doctor and a master.

The subject was accepted at excellent level by a checking council of the Vietnam Academy of Science and Technology on October 3.

Translated by Phuong Huyen
Link to Vietnamese Version

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