CD Disertasi
Kajian Senyawa Bioaktif Sebagai Antioksidan Dan Inhibitor Alfa-Glukosidase Dari Tumbuhan Obat Etnis Talang Mamak Khususnya Tumbuhan Flacourtia Rukam Dan Lithocarpus Bancanus
Talang Mamak is one of proto Malay tribe in Indragiri Hulu Regency, Riau Province. This tribe has local wisdom in the use of plants. As a native tribe they have long history of using plants as medicine, including antidiabetic medicines. Therefore, a scientific investigation on their local wisdom is needed. The objectives of research are: 1) To analyze the antioxidant and α-glucosidase inhibitors avtivities from the extracts of Talang Mamak tribe medicinal plants, namely A. disticha, M. bancana, L. bancanus, F. rukam and A. bunius 2) To analyze bioactive compounds as antioxidants from F. rukam and L. bancanus plants and 3) To analyze bioactive compounds as α-glucosidase inhibitors from F. rukam and L. bancanus plants by in vitro and in silico.
The research was conducted using an exploratory method with an ethnomedicinal approach. Extraction was performed using maceration method and purification was conducted using chromatography techniques. The Quantitative tests of some isolated metabolites were also performed using HPLC methods. The antioxidant activity assay was analyzed quantitatively using the 2.2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging method and α -glucosidase inhibitor bioactivity assay was carried out by in vitro and in silico methods. The research stages are: 1) Ethnomedicine studies and plants collection of medicinal plant of Talang Mamak tribe, 2) Extraction, antioxidant activity assay and α-glucosidase inhibitor by in vitro assay extract of medicinal plants from Talang Mamak tribe, 3) Isolation and characterization of bioactive compounds of F.rukam and L. bancanus plants, 4) Bioactivity assay of Antioxidant and α-glucosidase inhibitor of bioactive compounds and 5) In silico test of bioactive compounds and models of pillion-O-glycoside compounds by molecular docking method to α-glucosidase receptors (PDB ID: 5nn5, Resolution: 1.2 Å) using AutoDock 4.2 application (The Scripps Research Institute).
The methanol extract and ethyl acetate fraction of all test plant extracts showed antioxidant and α-glucosidase inhibitor activities. The methyl caffeate (114) (Content: 2.8%) was obtained from F. rukam leaves have very strong antioxidant activity with Antioxidant Activity Index (AAI): 10.9. The pillion (115) (Content: 4.5%) was obtained from L. bancanus leaves have strong antioxidant activity with AAI: 1.4 as well as other compounds such as tarxerol (116), betulinic acid (117) and 3-acetyl betulinic acid (118) which did not have antioxidant activity
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against DPPH radicals. The methyl caffeate and pilloin possessed good competitive α-glucosidase inhibitor activities with IC50 were 61.5 ± 0.7 dan 72.5 ± 0.5 μg/mL respectively, while taraxerol (116), betulinic acid (117) and 3-acetyl betulinic acid (118) possessed moderate activities. The results of the in silico test showed that the methyl caffeate (114) and pillion (115) had a ligand-receptor binding and interaction model fairly similar to the ligand-receptor binding and interaction model in 1-deoxynojirimycin (DNJ) and acarbose as standard compounds of α-glucosidase inhibitors, while taraxerol (116), betulinic acid (117) and 3-acetyl betulinic acid (118) was less similar to that of the standard. The results of the in silico test of the structural models of piloin-5-O-glycoside (120) and pilloin-3ʹ-O-glycoside (121) possessed a binding model and ligand-receptor interaction similar to the standard compound, and the values of free bond energy were more negative than of pillion (115) and α-glucosidase inhibitor standard.
The medicinal plant extracts of Talang Mamak tribe possessed antioxidant and α-glucosidase inhibitor properties, especially methanol extract and ethyl acetate fraction. The methyl caffeate compound (114) have a very strong antioxidant activity exceeding the activity of quercetin. Pilloin (115) have strong antioxidant activity, while taraxerol (116), betulinic acid (117) and 3-acetyl betulinic acid (118) were inactive. Based on in vitro and in silico experiment, methyl caffeate (114) and pilloin (115) had good competitive α-glucosidase inhibitor bioactivity. Based on in silico experiment, designing of pilloin (115) derivatives including pilloin-5-O-glycoside (120) and pilloin-3ʹ-O-glycoside (122) had increased competitiveness of α-glucosidase inhibitor activities.
Keywords: Antioxidant, α-glucosidase Inhibitor, Talang Mamak
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