Leny Heliawati 1 , Husnul Khatimah2 , Elvira Hermawati2 , And Yana Maolana Syah

Judul	:	Four Dammarane Triterpenes and Their Inhibitory Properties Against Eight Receptor Tyrosine Kinases
Abstrak	:	In recent years, tyrosine kinases (TKs) have been the target to combat cancers, and most of the developed inhibitors are of synthetic origin. Natural compounds that have the properties as the TK’s inhibitors are very limited. This paper described the isolation of a new dammarane triterpene from the tree bark of Sandoricum koetjape, along with three known related dammaranes from the damar resin of Shorea javanica, as well as their inhibitory properties against eight receptor TKs (RTKs: EGFR, HER2, HER4, IGF1R, InsR, KDR, PDGFR, and PDGFR). Based on the NMR and mass spectral data the new compound was identified as (12,20S)-12,20- dihydroxy-3,4-seco-dammaran-4,24-dien-3-oic acid (12-hydroxydammarenolic acid) (1), while the three known compounds were identified as (20S)-20-hydroxy-3,4-seco-dammaran-4,24-dien-3-oic acid (dammarenolic acid) (2), (3,20S)-3,20-dihydroxydammaran-24-ene (3), and (20S)-3-oxo-20-hydroxydammaran-24-ene (4). The tyrosine kinase assay of the four compounds resulted only 1 and 2 at concentration of 10 M that had weak activity against EGFR and InsR, with their % inhibitory were 30%, 27% (1), 45%, and 32% (2), respectively. The results suggested that the presence of a linear carboxylic acid group in both compounds could be of significance to the inhibitory properties against the two RTKs
Tahun	:	2021	Media Publikasi	:	Jurnal Internasional
Kategori	:	Jurnal	No/Vol/Tahun	:	4 / 23 / 2020
ISSN/ISBN	:	https://doi.org/10.20307/nps.2020.26.4.345 345
PTN/S	:	Universitas Pakuan	Program Studi	:	KIMIA
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