Anti-diabetic potential of Urena lobata leaf extract through inhibition of dipeptidyl peptidase IV activity

Purnomo, Yudi; Soeatmadji, Djoko Wahono; Sumitro, Sutiman Bambang; Widodo, M. Aris

doi:10.1016/j.apjtb.2015.05.014

Cited by 51 publications

(45 citation statements)

References 17 publications

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“…The effect of active compounds in U. lobata that has potency such as increasing β-cells proliferations and inhibiting β-cells apoptosis through GLP-1 activation 5, 9, 32. Bioavailability of GLP-1 could be retained due to DPP-4 inhibitor substances in the extract such as stigmasterol, mangiferin, and β-sitosterol 13, 26, 31. It affects the integrity of β-cells indirectly in the test group, it is shown in the shape of cells, size, and number which is close to normal groups.…”

Section: Discussionmentioning

confidence: 92%

Incretin effect of Urena lobata leaves extract on structure and function of rats islet β-cells

Purnomo

Soeatmadji

Sumitro

et al. 2017

Journal of Traditional and Complementary Medicine

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This study aims to determine the incretin effects of Urena lobata leaves extract on the structure and function of rats islet β-cells. This study utilizes male Sprague-Dawley rats divided into 2 control group and 3 test group (n = 5). Diabetic rats were induced with High Fructose Diet (HFD) and single dose intraperitoneal streptozotocin 25 mg/kg bw. Aqueous leaves extract of U. lobata was prepared by decoction methods and administrated orally with doses of 250, 500, and 1000 mg/kg bw for 4 weeks then incretin effect was evaluated by measuring serum GLP-1, insulin, and blood glucose levels. Histology of islet β-cells was evaluated using photomicroscopy by analyzing size, shape, and number. Data were analyzed using ANOVA test followed by LSD test and p ≤ 0.05 is considered significant. Oral administration of aqueous extract U. lobata leaves at doses of 250, 500, and 1000 mg/kg body weight were able to prolong GLP-1 bioavailability by 3-fold, 5-fold, and 7-fold respectively when compared to the diabetic group whereas blood glucose level were decreased about 30%, 35%, and 40% respectively (p < 0.05). Extract at doses of 500 and 1000 mg/kg bw also increased insulin level by 4-fold and 8-fold respectively compared to the diabetic group and the islet β-cells were repaired. The active compound in U. lobata leaves extract are suggested to prevent degradation of GLP-1 by inhibition of DPP-4 activity. Aqueous extract of U. lobata also improved the structure and function of islet β-cells by increasing of GLP-1 bioavailability.

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Section: Discussionmentioning

confidence: 92%

Incretin effect of Urena lobata leaves extract on structure and function of rats islet β-cells

Purnomo

Soeatmadji

Sumitro

et al. 2017

Journal of Traditional and Complementary Medicine

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“…However, GLP‐1 has very short half‐lives, approximately for 1–2 min owing to proteolytic cleavage of the N‐terminal dipeptide specifically for L‐alanine or L‐proline at the penultimate position by dipeptidyl peptidase‐IV (DPP‐IV) into inactive forms. Inhibition of enzyme DPP‐IV maintains the level of endogenous active GLP‐1 and prolongs its half‐life (Purnomo, Soeatmadji, Sumitro, & Widodo, ). DPP‐IV is a serine protease localized on cellular surfaces.…”

Section: Introductionmentioning

confidence: 99%

First report of chromenyl derivatives from spineless marine cuttlefish Sepiella inermis : Prospective antihyperglycemic agents attenuate serine protease dipeptidyl peptidase‐IV

2019

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Spineless marine cuttlefish Sepiella inermis has been considered as a popular dietary cephalopod species in Asian and Mediterranean coasts. Bioassay‐directed purification of organic extract of S. inermis ensued in the characterization of two chromenyl derivatives. The studied compounds exhibited significantly greater antioxidant potencies (IC50 ≤ 0.5 mg/ml) when compared with α‐tocopherol. The substituted 1H‐isochromenyloxy‐11‐hydroxyethyl pentanoate isoform (compound 1) efficiently inhibited the carbolytic enzymes along with key regulator of insulin secretion dipeptidyl peptidase‐IV (IC50 0.16 mg/ml). The molecular docking simulations displayed optimum binding affinity of the compound 1 (−10.01 kcal/mol) with dipeptidyl peptidase‐IV and lesser inhibition constant (Ki 46.41 nM), which along with its permissible hydrophobic‐hydrophilic balance (log Pow ~ 2) appeared to play significant roles in its greater antihyperglycemic activity compared to other studied chromenyl isoform. The greater antioxidant and antidiabetic properties of compound 1 could be utilized as an important natural lead against hyperglycemic‐related disorders. Practical applications The edible spineless marine cuttlefish Sepiella inermis are ubiquitously available in Asian and Mediterranean coasts. The sequential chromatographic purification of the organic extract of S. inermis led to the identification of two pure chromenyl chemotypes. The metabolites with substituted 1H‐isochromenyloxy‐11‐hydroxyethyl pentanoate isoform (compound 1) displayed potential antioxidative and antihyperglycemic activities compared to the chemotype (2) bearing 3H‐isochromen‐5‐yl moiety. The attenuating potential of chromenyl chemotype 1 against carbohydrate hydrolyzing enzymes and insulin secretion regulator attributed towards its efficiency as an important natural lead against postprandial hyperglycemia and incretin hormone regulation to maintain glucose homeostasis in the biological system. The chromenyl metabolites isolated from S. inermis could be utilized as a functional food ingredient in the nutraceutical formulations against hyperglycemic‐related disorders.

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“…Some plants reported as anti-hyperglycemia. 7,8 Studies on different types of tea as anti-diabetic that has done on green tea, black tea and oolong tea, but white tea has not known well. White tea (Camellia sinensis (L.) Kuntze) is a tea bud that still rolls processed without fermentation.…”

Section: Introductionmentioning

confidence: 99%

Dipeptidyl peptidase IV Inhibitory Activity of Fraction from White Tea Ethanolic Extract (Camellia sinensis (L.) Kuntze) ex vivo

Ekayanti¹,

Sauriasari²,

Elya³

2017

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Background: Treatment for type-2 diabetes mellitus focuses on the incretin hormone, Glucagon-Like Peptide-1 (GLP-1). However, it has a short half-life. Inhibition of the enzyme Dipeptidyl peptidase IV (DPP IV) required maintaining the active form of GLP-1. Based on the previous studies on the highest activity of DPP IV enzyme inhibition of white tea extract, this study conducted on the fraction of white tea extract using rat blood serum (ex vivo). Objectives: This study aims to evaluate the inhibitory activity of fraction from white tea extract. Methods: White tea leaves extracted with ethanol. The inhibitory activity determined by using rat blood serum as DPP IV enzyme source (ex vivo), AMC (7-amino 4-methyl coumarin) as fluorescence substrate of DPP IV and sitagliptin as the standard reference. The the cleavage of fluorescence reaction product observed by a microplate reader with λ ex = 360 nm and λ em =460 nm at 37 o C. Data expressed as mean ± SD and the IC 50 value determined by nonlinear regression curve and fit using Prism Graph 7. Result: methanol fraction (250 μg/mL) has the greater inhibition percentage (50.487%), and the fraction of n-hexane and ethyl acetate are 32.417% and 36.541%. The methanol fraction IC 50 value is 227 μg /mL. Conclusion: The methanol fraction is the most active to inhibit DPP IV enzyme.

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Anti-diabetic potential of Urena lobata leaf extract through inhibition of dipeptidyl peptidase IV activity

Cited by 51 publications

References 17 publications

Incretin effect of Urena lobata leaves extract on structure and function of rats islet β-cells

Incretin effect of Urena lobata leaves extract on structure and function of rats islet β-cells

First report of chromenyl derivatives from spineless marine cuttlefish Sepiella inermis : Prospective antihyperglycemic agents attenuate serine protease dipeptidyl peptidase‐IV

Dipeptidyl peptidase IV Inhibitory Activity of Fraction from White Tea Ethanolic Extract (Camellia sinensis (L.) Kuntze) ex vivo

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