ABSTRACT
This study aims to identify the phytochemical profile of Apis mellifera propolis and explore the potential of its anti-diabetic activity through inhibition of α-amylase (α-AE), α-glucosidase(α-GE), as well as novel antidiabetic compounds of propolis. Apis mellifera propolis extract (AMPE) exhibited elevated polyphenol 33.26±0.17 (mg GAE/g) and flavonoid (15.45±0.13â mg RE/g). It also indicated moderate strong antioxidant activity (IC50 793.09±1.94â µg/ml). This study found that AMPE displayed promising α-AE and α-GE inhibition through inâ vitro study. Based on LC-MS/MS screening, 18 unique AMPE compounds were identified, with majorly belonging to anthraquinone and flavonoid compounds. Furthermore, in silico study determined that 8 compounds of AMPE exhibited strong binding to α-AE that specifically interacted with its catalytic residue of ASP197. Moreover, 2 compounds exhibit potential inhibition of α-GE, by interacting with crucial amino acids of ARG315, ASP352, and ASP69. Finally, we suggested that 2,7-Dihydroxy-1-(p-hydroxybenzyl)-4-methoxy-9,10-dihydrophenanthrene and 3(3-(3,4-Dihydroxybenzyl)-7-hydroxychroman-4-one as novel inhibitors of α-AE and α-GE. Notably, these compounds were initially discovered from Apis mellifera propolis in this study. The molecular dynamic analysis confirmed their stable binding with both enzymes over 100â ns simulations. The inâ vivo acute toxicity assay reveals AMPE as a practically non-toxic product with an LD50 value of 16,050â mg/kg. Therefore, this propolis may serve as a promising natural product for diabetes mellitus treatment.
Subject(s)
Antioxidants , Hypoglycemic Agents , Molecular Docking Simulation , Phytochemicals , Propolis , alpha-Amylases , alpha-Glucosidases , Propolis/chemistry , Propolis/pharmacology , Hypoglycemic Agents/chemistry , Hypoglycemic Agents/pharmacology , Antioxidants/pharmacology , Antioxidants/chemistry , Bees , Animals , alpha-Glucosidases/metabolism , alpha-Amylases/antagonists & inhibitors , alpha-Amylases/metabolism , Phytochemicals/chemistry , Phytochemicals/pharmacology , Glycoside Hydrolase Inhibitors/chemistry , Glycoside Hydrolase Inhibitors/pharmacology , Molecular Dynamics Simulation , Enzyme Inhibitors/chemistry , Enzyme Inhibitors/pharmacologyABSTRACT
Curcuma aeruginosa Roxb. is an Indonesian traditional medicinal plant of the Zingiberaceae family. C. aeruginosa is known to have anticancer activity, especially in the rhizomes. Despite many studies on the phytochemical content of this plant with antioxidant and anticancer activity, transcriptomic studies are still limited in terms of genetic information. We ran transcriptome of Curcuma aeruginosa using a paired-end Illumina NextSeq 550 with PE150 mode and generating 12.8 GB of raw data. Raw reads have been filed with NCBI under project number PRJNA918644. This dataset allowed us to identify genes associated with biosynthetic pathways of anticancer drugs. Transcriptome data can also be used to develop new EST-SSR and SNP markers for use in plant breeding programs.
