α-Glucosidase-IN-2

α-Glucosidase-IN-2 (compound 5d) is a potent α-glucosidase inhibitor with an inhibitory concentration (IC50) of 9.48 μM, functioning as an antidiabetic agent [1].

α-Amylase α-Glucosidase-IN-2 (compound 5) exhibits strong inhibition of α-amylase and α-glucosidase enzymes, with IC50 values of 13.02 μM and 13.09 μM, respectively, showing promise for investigating diabetic complications [1].

α-Glucosidase-IN-23 is an orally active inhibitor of α-glucosidase that can decrease blood glucose levels by inhibiting α-glucosidase (IC50 = 4.48 μM).

α-Glucosidase-IN-22 is a selective inhibitor of α-glucosidase (IC50=0.64 μM). α-Glucosidase-IN-22 has antidiabetic activity and has potential in type 2 diabetes (T2DM) studies.

α-Glucosidase-IN-26 (Compound 7i), with an IC50 value of 4.63 µM, functions as an α-glucosidase inhibitor and is utilized in type 2 diabetes mellitus (T2DM) research [1].

α-Glucosidase-IN-27 (compound 8l), an α-glucosidase inhibitor with an IC50 of 25.78 μM, demonstrates potential for type 2 diabetes (D2M) research [1].

α-Glucosidase-IN-20 (Compound 3B) is a highly effective, orally active α-glucosidase inhibitor with potent anti-diabetic properties, evidenced by an IC50 value of 3.01 μM [1].

α-Glucosidase-IN-21 (Compound 2B) is a highly potent, orally bioavailable α-glucosidase inhibitor with an IC50 value of 2.62 μM, demonstrating remarkable anti-diabetic properties [1].

α-Glucosidase-IN-24 (Compound 13), an α-Glucosidase inhibitor derived from Swertia kouitchensis [1], exhibits an IC50 value of 451 μM.

α-Glucosidase-IN-28 (Compound 18) is an α-glucosidase inhibitor with an IC50 of 0.62 μM and Ki of 3.93 μM, interacting with the enzyme's original binding site (OBS) and forming multiple hydrophobic interactions with adjacent amino acids. This compound is used in diabetes and related diseases research [1].

α-Glucosidase-IN-29 (compound 19) is an inhibitor of α-glucosidases with an IC50 of 1.21 μM and a Ki of 1.80 μM, used in diabetes and related disease research [1].

α-Glucosidase-IN-25 (Compound (R)-8k) acts as a competitive inhibitor for α-glucosidase with an inhibitory concentration 50 (IC50) of 1.19 μM, making it applicable in anti-diabetic research [1].

Vicenin 2 is an angiotensin-converting enzyme (ACE) inhibitor (IC50=43.83 μM) from the aerial parts of Desmodium styracifolium. Vicenin 2 is an inhibitor of α-glucosidase, PTP1B, and RLAR. Vicenin 2 has hepatoprotective, anti-cancer, antioxidant and anti-inflammatory activities, and DTL co-administration is more effective than either of the single agents in androgen-independent prostate cancer. Vicenin 2 might be a useful lead for the development of multiple target-oriented therapeutic modalities for the treatment of diabetes and diabetes-associated complications. Vicenin 2 could act as a UV light barrier to protect the plants.

1. Isovitexin (Apigenin-6-C-Glucoside) exhibits a potential antioxidant activity. 2. Isovitexin shows a strong antihyperglycemic action, inhibits α-glucosidase in vivo.

α-glucosidase PTP1B-IN-1 (compound 8a) is an effective inhibitor of both α-glucosidase and PTP1B, with IC50 values of 66.3 μM and 47.0 μM, respectively. It also exhibits strong inhibitory activity against α-amylase, having an IC50 of 30.62 μM. This compound is capable of binding to the active sites of α-glucosidase and PTP1B. α-glucosidase PTP1B-IN-1 holds potential for reducing postprandial blood glucose levels and may be useful in managing type 2 diabetes.

α-Glucosidase-IN-77 (Compound H7) is a non-competitive α-glucosidase inhibitor with an IC50 of 1.25 μM. It reduces blood glucose levels, improves glucose tolerance, regulates gut microbiota, and exhibits hepatoprotective effects in a mouse model of type 2 diabetes.

α-Glucosidase-IN-79 (Compound 4d9) is a non-competitive α-glucosidase inhibitor with an IC50 of 2.11 μM, demonstrating greater inhibitory potency than the existing α-glucosidase inhibitors Acarbose (IC50 of 327.0 μM) and HXH8r (IC50 of 15.32 μM). It exhibits no cytotoxicity on normal human liver cells (LO2) and shows good metabolic stability in rat plasma. α-Glucosidase-IN-79 holds promise for research in type 2 diabetes.

α-Amylase α-Glucosidase-IN-18 (Compound 9g) is an inhibitor of α-amylase and α-glucosidase, with IC50 values of 49.17 nM and 10.71 nM, respectively. It is suitable for research related to type 2 diabetes.

α-Glucosidase-IN-84 (Compound 7j) is a competitive inhibitor of α-glucosidase, exhibiting an IC50 of 50 μM and a Ki of 32 μM. It shows potential for application in metabolic disease research, particularly in studies related to type 2 diabetes.

Australine is a pyrrolizidine alkaloid originally isolated fromC. australethat has enzyme inhibitory activities.1,2,3It is an inhibitor of glucoamylase (IC50= 5.8 μM) that also inhibits glucosidase I, sucrase, maltase, andA. nigerα-glucosidase (IC50s = 20, 28, 35, and 28 μM, respectively).2,3Australine is selective for these enzymes over glucosidase II, α- and β-mannosidase, and α- and β-galactosidase up to 500 μM, β-glucosidase, with only 5% inhibition at 66 μM, as well as isomaltase and trehalase (IC50= 97 and 160 μM, respectively). Australine (500 μg/ml) inhibits glycoprotein processing of viral glycoproteins in influenza virus-infected MDCK cells and induces the accumulation of glycoproteins.2 1.Molyneux, R.J., Benson, M., Wong, R.Y., et al.Australine, a novel pyrrolizidine alkaloid glucosidase inhibitor from Castanospermum australJ. Nat. Prod.51(6)1198-1206(1988) 2.Tropea, J.E., Molyneux, R.J., Kaushal, G.P., et al.Australine, a pyrrolizidine alkaloid that inhibits amyloglucosidase and glycoprotein processingBiochemistry28(5)2027-2034(1989) 3.Kato, A., Kano, E., Adachi, I., et al.Australine and related alkaloids: easy structural confirmation by 13C NMR spectral data and biological activitiesTetrahedron Asymmetry14(3)325-331(2003)

Collinin is a coumarin that has been found in Z. schinifolium and has diverse biological activities.1,2,3,4 It is active against drug-susceptible and -resistant strains of M. tuberculosis (MIC50s = 3.13-6.25 μg/ml).1 Collinin inhibits LPS-induced nitric oxide (NO) production (IC50 = 5.9 μM) and reduces COX-2 protein levels in RAW 264.7 cells.2 It completely inhibits aggregation of isolated rabbit platelets induced by arachidonic acid , collagen, or platelet activating factor (PAF) when used at a concentration of 100 μM.3 Dietary administration of collinin (0.05% w/w) reduces the number of mice with tumors and the number of tumors per mouse in a mouse model of colitis-related carcinogenesis.4 |1. Kim, S., Seo, H., Al Mahmud, H., et al. In vitro activity of collinin isolated from the leaves of Zanthoxylum schinifolium against multidrug- and extensively drug-resistant Mycobacterium tuberculosis. Phytomedicine 46, 104-110 (2018).|2. Nguyen, P.-H., Zhao, B.T., Kim, O., et al. Anti-inflammatory terpenylated coumarins from the leaves of Zanthoxylum schinifolium with α-glucosidase inhibitory activity. J. Nat. Med. 70(2), 276-281 (2016).|3. I.S., C., Lin, Y.C., Tsai, I.L., et al. Coumarins and anti-platelet aggregation constituents from Zanthoxylum schinifolium. Phytochemistry 39(5), 1091-1097 (1995).|4. Kohno, H., Suzuki, R., Curini, M., et al. Dietary administration with prenyloxycoumarins, auraptene and collinin, inhibits colitis-related colon carcinogenesis in mice. Int. J. Cancer 118(12), 2936-2942 (2006).

7,4'-Di-O-methylapigenin (4',7-DIMETHOXY-5-HYDROXYFLAVONE) can inhibit α-glucosidase and α-amylase enzymes and enhance 2-NBDG uptake in L6 cells, it has hypolipidemic effect on mouse pre-adipocyte (3T3L1) cell lines.

Epicoccone B, originally identified in C. globosum, demonstrates both DPPH free radical scavenging capability, with an IC50 of 10.8 μM, and significant α-glucosidase inhibitory activity, with an IC50 of 27.3 μM. It also possesses anti-HIV activity [1] [2].

α-Glucosidase-IN-33 (compound 7c), with an IC50 of 2.39 μM, is a potent α-glucosidase inhibitor, pertinent to type 2 diabetes and hyperglycemia research [1].