Evaluation of the Antidiabetic Activity and Chemical Composition of Geranium collinum Root Extracts—Computational and Experimental Investigations
Sodik Numonov,
Salamet Edirs,
Khayrulla Bobakulov,
Muhammad Nasimullah Qureshi,
Khurshed Bozorov,
Farukh Sharopov,
William N. Setzer,
Haiqing Zhao,
Maidina Habasi,
Mizhgona Sharofova,
Haji Akber Aisa
Affiliations
Sodik Numonov
Key Laboratory of Plant Resources and Chemistry in Arid Regions, Xinjiang Technical Institute of Physics and Chemistry, Chinese Academy of Sciences, Urumqi 830011, China
Salamet Edirs
Key Laboratory of Plant Resources and Chemistry in Arid Regions, Xinjiang Technical Institute of Physics and Chemistry, Chinese Academy of Sciences, Urumqi 830011, China
Khayrulla Bobakulov
Institute of the Chemistry of Plant Substances, Academy of Sciences of the Republic of Uzbekistan, Tashkent 100170, Uzbekistan
Muhammad Nasimullah Qureshi
Department of Chemistry, Abdul Wali Khan University, Mardan 23200, Pakistan
Khurshed Bozorov
Key Laboratory of Plant Resources and Chemistry in Arid Regions, Xinjiang Technical Institute of Physics and Chemistry, Chinese Academy of Sciences, Urumqi 830011, China
Farukh Sharopov
Key Laboratory of Plant Resources and Chemistry in Arid Regions, Xinjiang Technical Institute of Physics and Chemistry, Chinese Academy of Sciences, Urumqi 830011, China
William N. Setzer
Department of Chemistry, University of Alabama in Huntsville, Huntsville, AL 35899, USA
Haiqing Zhao
Key Laboratory of Plant Resources and Chemistry in Arid Regions, Xinjiang Technical Institute of Physics and Chemistry, Chinese Academy of Sciences, Urumqi 830011, China
Maidina Habasi
Key Laboratory of Plant Resources and Chemistry in Arid Regions, Xinjiang Technical Institute of Physics and Chemistry, Chinese Academy of Sciences, Urumqi 830011, China
Mizhgona Sharofova
Institute of Avicenna’s Medicine and Pharmacology, Academy of the Tajik Traditional Medicine, Dushanbe 734062, Tajikistan
Haji Akber Aisa
Key Laboratory of Plant Resources and Chemistry in Arid Regions, Xinjiang Technical Institute of Physics and Chemistry, Chinese Academy of Sciences, Urumqi 830011, China
The root of Geranium collinum Steph is known in Tajik traditional medicine for its hepatoprotective, antioxidant, and anti-inflammatory therapeutic effects. The present study was conducted to evaluate of potential antidiabetic, antioxidant activities, total polyphenolic and flavonoid content from the different extracts (aqueous, aqueous-ethanolic) and individual compounds isolated of the root parts of G. collinum. The 50% aqueous-ethanolic extract possesses potent antidiabetic activity, with IC50 values of 0.10 μg/mL and 0.09 μg/mL for the enzymes protein-tyrosine phosphatase (1B PTP-1B) and α-glucosidase, respectively. Phytochemical investigations of the 50% aqueous-ethanolic extract of G. collinum, led to the isolation of ten pure compounds identified as 3,3′,4,4′-tetra-O-methylellagic acid (1), 3,3′-di-O-methylellagic acid (2), quercetin (3), caffeic acid (4), (+)-catechin (5), (–)-epicatechin (6), (–)-epigallocatechin (7), gallic acid (8), β-sitosterol-3-O-β-d-glucopyranoside (9), and corilagin (10). Their structures were determined based on 1D and 2D NMR and mass spectrometric analyses. Three isolated compounds exhibited strong inhibitory activity against PTP-1B, with IC50 values below 0.9 μg/mL, more effective than the positive control (1.46 μg/mL). Molecular docking analysis suggests polyphenolic compounds such as corilagin, catechin and caffeic acid inhibit PTP-1B and β-sitosterol-3-O-β-d-gluco-pyranoside inhibits α-glucosidase. The experimental results suggest that the biological activity of G. collinum is related to its polyphenol contents. The results are also in agreement with computational investigations. Furthermore, the potent antidiabetic activity of the 50% aqueous-ethanolic extract from G. collinum shows promise for its future application in medicine. To the best of our knowledge, we hereby report, for the first time, the antidiabetic activity of G. collinum.
