UNAIR NEWS– Angiogenesis is one of the factors that most contribute to the progressive growth of neoplasms and the occurrence of metastases in cancer patients. It occurs the formation of new blood vessels as an extension of existing blood vessels. Its function is to supply oxygen and food to cancer cells, resulting in uncontrolled cell division to provide oxygen and food to cancer cells. Resulting in an uncontrolled cell division process and the spread of cancer cells.
Barriers to angiogenesis are known to inhibit cell proliferation and cancer metastases. Some drugs used to inhibit the occurrence of angiogenesis still shows results that have not been encouraging. One reason is the side effects caused.
In a study conducted to find a new drug candidate for anti-cancer, one of the cinnamic derivatives known to have angiogenesis inhibiting activity is ethyl p-methoxycinamic. This compound was isolated from kencur plants and is known to have anti-inflammatory activity. Ethyl p-methoxycinamat can inhibit the enzyme cyclooxygenase-2 (COX-2) and tyrosine kinase.
“This study was chosen as a starting material because it has the same mechanism of action and a similar structure,” said Dr. Juni Ekowati, M.Si., Apt., As a researcher.
Juni explained that this research was a collaboration between Faculty of Pharmacy, Airlangga University and Hoshi University, Japan. In this study, the m-methoxycinamic acid compound is easily synthesized through the Knoevenagel reaction. The carboxylic acid group from m-methoxycinamic acid changed into thiourea in this study.
“With this structural modification, it is hoped that the resistance to angiogenesis will be even stronger. Besides, it is expected that the newly synthesized compound has low toxicity and can be well absorbed by the body, “explained Juni.
Spectroscopic test of the structural characteristics of the product compound showed that three new compounds of thiourea derivate from m-methoxycinamic acid had been formed. The inhibitory activity of the synthesized thiourea derivative compound was stronger than the initial compound, m-methoxycinamic acid. The physicochemical properties of the compounds also meet the requirements to be developed as candidates for drugs used orally.
“Its absorption in the intestine is predicted to be good, and its toxicity is also low, making it safe to use as a drug. The results of computerized studies also show that the activity of modified compounds in inhibiting COX-2 is stronger than the original compound, “Juni said.
“This compound has good prospects to be developed as a candidate for cancer drugs, especially for prevention in the early phase of cancer cell growth,” she concluded (*).
Author: Sukma Cindra Pratiwi
Editor : Khefti Al Mawalia
Link to scientific article:
Juni Ekowati, Iwan Sahrial Hamid, Kholis Amalia Nofianti, Shigeru Sasaki. Synthesis of Thiourea Derivatives from m-Methoxycinnamic Acid as Antiangiogenic Candidate. Jurnal Teknologi, 81(4) 105–114 |www.jurnalteknologi.utm.my | eISSN 2180–3722