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BMC Complementary Medicine and Therapies
Published in: BMC Complementary Medicine and Therapies 1/2021

Open Access 01-12-2021 | Acarbose | Research

Crude extract and isolated bioactive compounds from Notholirion thomsonianum (Royale) Stapf as multitargets antidiabetic agents: in-vitro and molecular docking approaches

Authors: Mater H. Mahnashi, Yahya S. Alqahtani, Ali O. Alqarni, Bandar A. Alyami, Muhammad Saeed Jan, Muhammad Ayaz, Farhat Ullah, Umer Rashid, Abdul Sadiq

Published in: BMC Complementary Medicine and Therapies | Issue 1/2021

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Abstract

Background

Diabetes mellitus is a common disease effecting the lifestyles of majority world population. In this research work, we have embarked the potential role of crude extracts and isolated compounds of Notholirion thomsonianum for the management diabetes mellitus.

Methods

The crude extracts of N. thomsonianum were initially evaluated for α-glucosidase, α-amylase and antioxidant activities. The compounds were isolated from the activity based potent solvent fraction. The structures of isolated compounds were confirmed with NMR and MS analyses. The isolated compounds were tested for α-glucosidase, α-amylase, protein tyrosine phosphatase 1B (PTP1B) and DPPH activities. The molecular docking studies were carried out to find the binding interactions of isolated compounds for α-glucosidase, α-amylase and PTP1B.

Results

Initially, we screened out crude extracts and subfractions of N. thomsonianum against different in-vitro targets. Among all, Nt.EtAc was observed a potent fraction among all giving IC50 values of 67, 70, < 0.1, 89 and 16 μg/mL against α-glucosidase, α-amylase, DPPH, ABTS and H2O2 respectively. Three compounds (Nt01, Nt02 and Nt03) were isolated from Nt.EtAc of N. thomsonianum. The isolated compounds Nt01, Nt02 and Nt03 exhibited IC50 values of 58.93, 114.93 and 19.54 μM against α-glucosidase, while 56.25, 96.54 and 24.39 μM against α-amylase respectively. Comparatively, the standard acarbose observed IC50 values were 10.60 and 12.71 μM against α-glucosidase, α-amylase respectively. In PTP1B assay, the compounds Nt01, Nt02 and Nt03 demonstrated IC50 values of 12.96, 36.22 and 3.57 μM in comparison to the standard ursolic acid (IC50 of 3.63 μM). The isolated compounds also gave overwhelming results in DPPH assay. Molecular docking based binding interactions for α-glucosidase, α-amylase and PTP1B were also encouraging.

Conclusions

In the light of current results, it is obvious that N. thomsonianum is potential medicinal plant for the treatment of hyperglycemia. Overall, Nt.EtAc was dominant fraction in all in-vitro activities. Three compounds Nt01, Nt02 and Nt03 were isolated from ethyl acetate fraction. The Nt03 specifically was most potent in all in-vitro assays. The molecular docking studies supported our in-vitro results. It is concluded that N. thomsonianum is a rich source of bioactive antidiabetic compounds which can be further extended to in-vivo based experiments.
Appendix
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Literature
1.
2.
3.
Rahim H, Sadiq A, Khan S, Amin F, Ullah R, Shahat AA, et al. Fabrication and characterization of glimepiride nanosuspension by ultrasonication-assisted precipitation for improvement of oral bioavailability and in vitro α-glucosidase inhibition. Int J Nanomedicine. 2019;14:6287.PubMedPubMedCentralCrossRef
4.
Fonseca V. Clinical significance of targeting postprandial and fasting hyperglycemia in managing type 2 diabetes mellitus. Curr Med Res Opinion. 2003;19(7):635–1.CrossRef
5.
Nichols BL, Avery SE, Karnsakul W, Jahoor F, Sen P, Swallow DM, et al. Congenital maltase-glucoamylase deficiency associated with lactase and sucrase deficiencies. J Pediatr Gastroenterol Nutr. 2002;35(4):573–9.PubMedCrossRef
6.
Nugent TC, Bibi A, Sadiq A, Shoaib M, Umar MN, Tehrani FN. Chiral picolylamines for Michael and aldol reactions: probing substrate boundaries. Org Biomol Chem. 2012;10(46):9287–94.PubMedCrossRef
7.
Mahnashi MH, Elgazwi SM, Ahmed MS, Halaweish FT. Cucurbitacins inspired organic synthesis: potential dual inhibitors targeting EGFR–MAPK pathway. Eur J Med Chem. 2019;173:294–304.PubMedCrossRef
8.
Hussain F, Khan Z, Jan MS, Ahmad S, Ahmad A, Rashid U, et al. Synthesis, in-vitro α-glucosidase inhibition, antioxidant, in-vivo antidiabetic and molecular docking studies of pyrrolidine-2, 5-dione and thiazolidine-2, 4-dione derivatives. Bioorg Chem. 2019;91:103128.PubMedCrossRef
9.
Aslam H, Khan AU, Naureen H, Ali F, Ullah F, Sadiq A. Potential application of Conyza canadensis (L) Cronquist in the management of diabetes: in vitro and in vivo evaluation. Trop J Pharm Res. 2018;17(7):1287–93.CrossRef
10.
Murali C, Mudgil P, Gan CY, Tarazi H, El-Awady R, Abdalla Y, Amin A, Maqsood S. Camel whey protein hydrolysates induced G2/M cellcycle arrest in human colorectal carcinoma. Sci Rep 2021, 11(1):1–4.
11.
Farooq U, Naz S, Shams A, Raza Y, Ahmed A, Rashid U, et al. Isolation of dihydrobenzofuran derivatives from ethnomedicinal species Polygonum barbatum as anticancer compounds. Biol Res. 2019;52(1):1–2.PubMedPubMedCentralCrossRef
12.
Shah SM, Sadiq A, Shah SM, Ullah F. Antioxidant, total phenolic contents and antinociceptive potential of Teucrium stocksianum methanolic extract in different animal models. BMC Complement Altern Med. 2014;14(1):1–7.CrossRef
13.
Inouye S, Tsuruoka T, Ito T, Niida T. Structure and synthesis of nojirimycin. Tetrahedron. 1968;24(5):2125–44.PubMedCrossRef
14.
Sadiq A, Rashid U, Ahmad S, Zahoor M, AlAjmi MF, Ullah R, et al. Treating Hyperglycemia From Eryngium caeruleum M. Bieb: In-vitro α-Glucosidase, Antioxidant, in-vivo Antidiabetic and Molecular Docking-Based Approaches. Front Chem. 2020;8:1064.CrossRef
15.
Zafar R, Zubair M, Ali S, Shahid K, Waseem W, Naureen H, et al. Zinc metal carboxylates as potential anti-Alzheimer’s candidate: in vitro anticholinesterase, antioxidant and molecular docking studies. J Biomol Str Dyn. 2020;12:1–1.
16.
Alqahtani YS. Bioactive Stigmastadienone from Isodon rugosus as potential anticholinesterase, α-glucosidase and COX/LOX inhibitor: in-vitro and molecular docking studies. Steroids. 2021;1:108857.CrossRef
17.
Ajaib: Antioxidant and antimicrobial activities of an ethnobotanically important plant Notholirion thomsonianum from district kotli, azad jammu & Kashmir. J Animals Plant Sci 2014, 24(3):115–121.
18.
Sadiq A, Ahmad S, Ali R, Ahmad F, Ahmad S, Zeb A, et al. Antibacterial and antifungal potentials of the solvents extracts from Eryngium caeruleum, Notholirion thomsonianum and Allium consanguineum. BMC Complement Altern Med. 2016;16(1):1–8.CrossRef
19.
Mahmood F, Ali R, Jan MS, Chishti KA, Ahmad S, Zeb A, et al. Chemical characterization and analgesic potential of Notholirion thomsonianum extract. Lat Am J Pharm. 2019;38(4):807–12.
20.
Shah S, Shah SM, Ahmad Z, Yaseen M, Shah R, Sadiq A, et al. Phytochemicals, in vitro antioxidant, total phenolic contents and phytotoxic activity of Cornus macrophylla wall bark collected from the north-west of Pakistan. Pak J Pharm Sci. 2015;28(1):23–8.PubMed
21.
Zhang S, Zhang ZY. PTP1B as a drug target: recent developments in PTP1B inhibitor discovery. Drug Disc Today. 2007;12(9–10):373–81.CrossRef
22.
Bibi A, Shah T, Sadiq A, Khalid N, Ullah F, Iqbal A. L-isoleucine-catalyzed michael synthesis of N-alkylsuccinimide derivatives and their antioxidant activity assessment. Russian J Org Chem. 2019;55(11):1749–54.CrossRef
23.
Sadiq A, Mahmood F, Ullah F, Ayaz M, Ahmad S, Haq FU, et al. Synthesis, anticholinesterase and antioxidant potentials of ketoesters derivatives of succinimides: a possible role in the management of Alzheimer’s. Chem Cent J. 2015;9(1):1–9.CrossRef
24.
Sadiq A, Zeb A, Ullah F, Ahmad S, Ayaz M, Rashid U, et al. Chemical characterization, analgesic, antioxidant, and anticholinesterase potentials of essential oils from Isodon rugosus Wall. ex. Benth. Front Pharmacol. 2018;9:623.PubMedPubMedCentralCrossRef
25.
Jabeen M, Ahmad S, Shahid K, Sadiq A, Rashid U. Ursolic acid hydrazide based organometallic complexes: synthesis, characterization, antibacterial, antioxidant, and docking studies. Front Chem. 2018;6:55.PubMedPubMedCentralCrossRef
26.
Zeb A, Sadiq A, Ullah F, Ahmad S, Ayaz M. Investigations of anticholinestrase and antioxidant potentials of methanolic extract, subsequent fractions, crude saponins and flavonoids isolated from Isodon rugosus. Biol Res. 2014;47(1):1.CrossRef
27.
Ahmad S, Mahnashi MH, Alyami BA, Alqahtani YS, Ullah F, Ayaz M, et al. Synthesis of Michael adducts as key building blocks for potential analgesic drugs: in vitro, in vivo and in silico explorations. Drug Des Devel Ther. 2021;15:1299.PubMedPubMedCentralCrossRef
28.
Sadiq A, Mahnashi MH, Alyami BA, Alqahtani YS, Alqarni AO, Rashid U. Tailoring the substitution pattern of Pyrrolidine-2,5-dione for discovery of new structural template for dual COX / LOX inhibition. Bioorg Chem. 2021.
29.
Tufail MB, Javed MA, Ikram M, Mahnashi MH, Alyami BA, Alqahtani YS, et al. Synthesis, pharmacological evaluation and molecular modelling studies of pregnenolone derivatives as inhibitors of human dihydrofolate reductase. Steroids. 2021;168:108801.CrossRef
30.
Williams L, Zhang X, Caner S, et al. The amylase inhibitor montbretin a reveals a new glycosidase inhibition motif. Nat Chem Biol. 2015;11:691–6.PubMedCrossRef
31.
Mahnashi MH. Knowledge, Attitude, Practice, and the Perceived Barriers with Respect to the Use of Herbal Medicines. Curr Top Nutraceutical Res. 2021;19:1.
32.
Mahnashi MH, Alyami BA, Alqahtani YS, Jan MS, Rashid U, Sadiq A, et al. Phytochemical profiling of bioactive compounds, anti-inflammatory and analgesic potentials of Habenaria digitata Lindl.: Molecular docking based synergistic effect of the identified compounds. J Ethnopharmacol. 2021;273:113976.PubMedCrossRef
33.
Zahoor M, Shafiq S, Ullah H, Sadiq A, Ullah F. Isolation of quercetin and mandelic acid from Aesculus indica fruit and their biological activities. BMC Biochem. 2018;19(1):1–4.CrossRef
34.
Shah SM, Ullah F, Shah SM, Zahoor M, Sadiq A. Analysis of chemical constituents and antinociceptive potential of essential oil of Teucrium Stocksianum bioss collected from the north west of Pakistan. BMC Complement Altern Med. 2012;12(1):1–6.CrossRef
35.
Zafar R, Ullah H, Zahoor M, Sadiq A. Isolation of bioactive compounds from Bergenia ciliata (haw.) Sternb rhizome and their antioxidant and anticholinesterase activities. BMC Complement Altern Med. 2019;19(1):1–3.CrossRef
36.
Begum HA, Asad F, Sadiq A, Mulk S, Ali K. Antioxidant, antimicrobial activity and phytochemical analysis of the seeds extract of Cucumis sativus Linn. Pure App Biol. 2019;8(1):433–41.
37.
Devasagayam TPA, Tilak JC, Boloor KK. Review: free radicals and antioxidants in human health: current statistics and future Prospectives. JAPI. 2004;53:794–804.
38.
Jan MS, Ahmad S, Hussain F, Ahmad A, Mahmood F, Rashid U, et al. Design, synthesis, in-vitro, in-vivo and in-silico studies of pyrrolidine-2, 5-dione derivatives as multitarget anti-inflammatory agents. Eur J Med Chem. 2020;186:111863.PubMedCrossRef
Metadata
Title
Crude extract and isolated bioactive compounds from Notholirion thomsonianum (Royale) Stapf as multitargets antidiabetic agents: in-vitro and molecular docking approaches
Authors
Mater H. Mahnashi
Yahya S. Alqahtani
Ali O. Alqarni
Bandar A. Alyami
Muhammad Saeed Jan
Muhammad Ayaz
Farhat Ullah
Umer Rashid
Abdul Sadiq
Publication date
01-12-2021
Publisher
BioMed Central
Keyword
Acarbose
Published in
BMC Complementary Medicine and Therapies / Issue 1/2021
Electronic ISSN: 2662-7671
DOI
https://doi.org/10.1186/s12906-021-03443-7

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