In vitro inhibitory effect of oriental melon (Cucumis melo L. var. makuwa Makino) seed on key enzyme linked to type 2 diabetes

2013 ◽  
Vol 5 (2) ◽  
pp. 981-986 ◽  
Author(s):  
Lei Chen ◽  
Young-Hwa Kang
Keyword(s):  
Type 2 Diabetes ◽  
Cucumis Melo ◽  
Inhibitory Effect ◽  
Oriental Melon ◽  
Key Enzyme ◽  
Cucumis Melo L

scholarly journals Azadirachta indica inhibits key enzyme linked to type 2 diabetes in vitro, abates oxidative hepatic injury and enhances muscle glucose uptake ex vivo

2019 ◽  
Vol 109 ◽  
pp. 734-743 ◽  
Author(s):  
Olakunle Sanni ◽  
Ochuko L. Erukainure ◽  
Chika I. Chukwuma ◽  
Neil A. Koorbanally ◽  
Collins U. Ibeji ◽  
...  
Keyword(s):  
Type 2 Diabetes ◽  
Glucose Uptake ◽  
Azadirachta Indica ◽  
Hepatic Injury ◽  
Ex Vivo ◽  
Key Enzyme

scholarly journals Inhibitory Effect of the Leaf of Psidium guajava Grown in Vietnam on α-Glucosidase and Protein Tyrosine Phosphatase 1B in vitro

2019 ◽  
Vol 35 (1) ◽  
Author(s):  
Dang Kim Thu ◽  
Le Thi Thu Huong ◽  
Tran Trong Nghia ◽  
Bui Thanh Tung
Keyword(s):  
Type 2 Diabetes ◽  
Protein Tyrosine Phosphatase ◽  
Tyrosine Phosphatase ◽  
Psidium Guajava ◽  
Inhibitory Effect ◽  
Diabetic Rats ◽  
Protein Tyrosine Phosphatase 1B ◽  
Protein Tyrosine

Type 2 diabetes is a fairly common chronic disease. α-glucosidase and protein tyrosine phosphatase, as enzymes, play an important role in type 2 diabetes. This study evaluates the inhibitory effect of the two enzymes in vitro of ethanol extract and fractions of Vietnam Psidium guajava’s leaves. The leaves were collected, dried and extracted with 96% ethanol and successively fractionated with n-hexane, ethyl acetate and butanol solvents. The results show that the EtOH extract, n-nexan, EtOAc and BuOH fractions had high α-glucosidase inhibitory effect with IC50 values ​​of 2.20; 2.53; 2.24 and 2.16 µg/mL, respectively. In addition, EtOAc and BuOH fractions also show strong inhibitory PTP1B effect with IC50 at 120.22 mg/mL and 97.72 mg/mL, respectively. The study results show that Psidium guajava leaves are a potential source of material to inhibit α-glucosidase and PTP1B in the treatment of diabetes. Keywords Psidium guajava, α-glucosidase, protein tyrosine phosphatase 1B, diabetes, extraction. References [1] A. Chaudhury, C. Duvoor, R. Dendi, V. Sena, S. Kraleti, A. Chada, et al. Clinical review of antidiabetic drugs: Implications for type 2 diabetes mellitus management, Frontiers in endocrinology. 8 (2017) 6.[2] F.A. Van de Laar, P.L. Lucassen, R.P. Akkermans, E. H. Van de Lisdonk, G.E. Rutten,C. Van, Alpha - glucosidase inhibitors for type 2 diabetes mellitus. The Cochrane Library (2005).[3] J. Montalibet, B.P. Kennedy. Therapeutic strategies for targeting PTP1B in diabetes. Drug Discovery Today: Therapeutic Strategies 2(2) (2005) 129.[4] S.M. Barbalho, Farinazzi-Machado, R. De Alvares Goulart, A.C.S. Brunnati, A. Otoboni, B. Ottoboni. Psidium guajava (Guava): A plant of multipurpose medicinal applications, Med Aromat Plants. 1(104) (2012) 2167.[5] R.M.P. Gutiérrez, S. Mitchell, Solis R. V. Psidium guajava: a review of its traditional uses, phytochemistry and pharmacology. Journal of ethnopharmacology 117(1) (2008) 1.[6] B. T. Tùng, Đ.K. Thu, P.T. Hải, N.T. Hải. Đánh giá tác dụng ức chế enzym α-glucosidase của các phân đoạn dịch chiết quả Lựu (Punica granatum Linn), Tạp chí Y Dược cổ truyền Việt Nam. 5(18) (2018) 59.[7] P.H. Nguyen, J.L. Yang, M.N. Uddin, S.L. Park, S.I. Lim, D.W. Jung, et al. Protein tyrosine phosphatase 1B (PTP1B) inhibitors from Morinda citrifolia (Noni) and their insulin mimetic activity, Journal of natural products. 76(11) (2013) 2080.[8] H.B.H. Khan, D. Rajendran, M.R. Bai, Sorimuthu S. Protective effect of Psidium guajava leaf extract on altered carbohydrate metabolism in streptozotocin-induced diabetic rats, Journal of dietary supplements. 10(4) (2013) 335.[9] H. Mukhtar, S. Ansari, M. Ali, T. Naved, Z. Bhat Effect of water extract of Psidium guajava leaves on alloxan-induced diabetic rats. Die Pharmazie-An International Journal of Pharmaceutical Sciences. 59(9) (2004) 734.[10] W. K. Oh, C. H. Lee, M. S. Lee, E. Y. Bae, C. B. Sohn, H. Oh, et al. Antidiabetic effects of extracts from Psidium guajava, Journal of ethnopharmacology. 96(3) (2005) 411.[11] B. Wang, H. Liu, J. Hong, H. Li, C. Huang, Effect of Psidium guajava leaf extract on alpha-glucosidase activity in small intestine of diabetic mouse. Sichuan da xue xue bao Yi xue ban, Journal of Sichuan University Medical science edition. 38(2) (2007) 298.[12] S. C. Shen, F. C. Cheng, N. J. Wu. Effect of guava (Psidium guajava Linn.) leaf soluble solids on glucose metabolism in type 2 diabetic rats, Phytotherapy Research. 22(11) (2008) 1458.      

Metformin Inhibits N-Methyl-N-Nitrosourea Induced Gastric Tumorigenesis in db/db Mice

2017 ◽  
Vol 125 (06) ◽  
pp. 392-399 ◽  
Author(s):  
Shan Zhuang ◽  
Yongmei Jian ◽  
Yongning Sun
Keyword(s):  
Gastric Cancer ◽  
Type 2 Diabetes ◽  
Inflammatory Cytokines ◽  
Serum Insulin ◽  
Inhibitory Effect ◽  
Increased Risk ◽  
Pro Inflammatory Cytokines

Abstract Type 2 diabetes can elevate risk of gastric cancer and metformin, an anti-diabetic agent, has an inhibitory effect against gastric cancer cell in vitro. However, the effect of metformin on type 2 diabetes-related gastric tumorigenesis in vivo is still not clear. In the present study, we aim to detect whether metformin can inhibit increased risk of gastric cancer in diabetic db/db mice and which the potential anti-cancer mechanisms of metformin are. 4-week-old mice were divided into 3 groups (2 db/db mice groups and one wild type mice group). All diabetic and non-diabetic mice were treated with N-Methyl-N-Nitrosourea (MNU) for 20 weeks to induce gastric tumorigenesis. At week 21, one db/db mice group were treated with metformin (5 mg/ml) for 10 weeks and the other 2 groups were treated with saline. Blood samples were collected for testing insulin and insulin-like growth factor (IGF)-1. Stomach tissues were collected for histopathological evaluation and mRNAs analysis. Metformin significantly decreased incidence of MNU-induced gastric dysplasia and cancer in diabetic db/db mice. Furthermore, metformin reduced serum insulin as well as IGF-1, and also suppressed expression of insulin receptor, IGF-1, IGF-1 receptor and several pro-inflammatory cytokines mRNAs in stomach of db/db mice, but did not significantly influence IGF-2 and IGF-2 receptor expressions. The results show that metformin can prevent the risk of gastric cancer in type 2 diabetes and the protective mechanisms may involve in an inhibitory effect of metformin on insulin as well as IGF-1 signals and cancer related pro-inflammatory cytokines.

scholarly journals An In Silico and an In Vitro Inhibition Analysis of Glycogen Phosphorylase by Flavonoids, Styrylchromones, and Pyrazoles

Nutrients ◽  
2022 ◽  
Vol 14 (2) ◽  
pp. 306
Author(s):  
Sónia Rocha ◽  
Natália Aniceto ◽  
Rita C. Guedes ◽  
Hélio M. T. Albuquerque ◽  
Vera L. M. Silva ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
In Silico ◽  
Glycogen Phosphorylase ◽  
Inhibitory Effect ◽  
Docking Studies ◽  
Potent Inhibitory Effect ◽  
Key Enzyme ◽  
Experimental Findings

Glycogen phosphorylase (GP) is a key enzyme in the glycogenolysis pathway. GP inhibitors are currently under investigation as a new liver-targeted approach to managing type 2 diabetes mellitus (DM). The aim of the present study was to evaluate the inhibitory activity of a panel of 52 structurally related chromone derivatives; namely, flavonoids, 2-styrylchromones, 2-styrylchromone-related derivatives [2-(4-arylbuta-1,3-dien-1-yl)chromones], and 4- and 5-styrylpyrazoles against GP, using in silico and in vitro microanalysis screening systems. Several of the tested compounds showed a potent inhibitory effect. The structure–activity relationship study indicated that for 2-styrylchromones and 2-styrylchromone-related derivatives, the hydroxylations at the A and B rings, and in the flavonoid family, as well as the hydroxylation of the A ring, were determinants for the inhibitory activity. To support the in vitro experimental findings, molecular docking studies were performed, revealing clear hydrogen bonding patterns that favored the inhibitory effects of flavonoids, 2-styrylchromones, and 2-styrylchromone-related derivatives. Interestingly, the potency of the most active compounds increased almost four-fold when the concentration of glucose increased, presenting an IC50 < 10 µM. This effect may reduce the risk of hypoglycemia, a commonly reported side effect of antidiabetic agents. This work contributes with important considerations and provides a better understanding of potential scaffolds for the study of novel GP inhibitors.

scholarly journals In vitro antioxidant potential and inhibitory effect of hydro-ethanolic extract from African black velvet tamarind (Dialium indium) pulp on type 2 diabetes linked enzymes

10.5219/911 ◽  
2018 ◽  
Vol 12 (1) ◽  
Author(s):  
Olakunle Bamikole Afolabi ◽  
Omotade Ibidun Oloyede ◽  
Abiodun Ayodele Ojo ◽  
Amos Adeyinka Onansanya ◽  
Shadrach Oludare Agunbiade ◽  
...  
Keyword(s):  
Type 2 Diabetes ◽  
Ethanolic Extract ◽  
Inhibitory Effect ◽  
Antioxidant Potential ◽  
African Black

Caffeic and chlorogenic acids inhibit key enzymes linked to type 2 diabetes (in vitro): a comparative study

2015 ◽  
Vol 26 (2) ◽  
Author(s):  
Ganiyu Oboh ◽  
Odunayo M. Agunloye ◽  
Stephen A. Adefegha ◽  
Ayodele J. Akinyemi ◽  
Adedayo O. Ademiluyi
Keyword(s):  
Type 2 Diabetes ◽  
Chlorogenic Acid ◽  
Caffeic Acid ◽  
Phenolic Acids ◽  
Quinic Acid ◽  
Inhibitory Effect ◽  
Dependent Manner ◽  
Key Enzymes

AbstractChlorogenic acid is a major phenolic compound that forms a substantial part of plant foods and is an ester of caffeic acid and quinic acid. However, the effect of the structures of both chlorogenic and caffeic acids on their antioxidant and antidiabetic potentials have not been fully understood. Thus, this study sought to investigate and compare the interaction of caffeic acid and chlorogenic acid with α-amylase and α-glucosidase (key enzymes linked to type 2 diabetes) activities in vitro.The inhibitory effect of the phenolic acids on α-amylase and α-glucosidase activities was evaluated. Thereafter, their antioxidant activities as typified by their 1,1-diphenyl-2 picrylhydrazyl radical scavenging ability and ferric reducing antioxidant properties were determined.The results revealed that both phenolic acids inhibited α-amylase and α-glucosidase activities in a dose-dependent manner (2–8 μg/mL). However, caffeic acid had a significantly (p<0.05) higher inhibitory effect on α-amylase [ICThe esterification of caffeic acid with quinic acid, producing chlorogenic acid, reduces their ability to inhibit α-amylase and α-glucosidase activities. Thus, the inhibition of α-amylase and α-glucosidase activities by the phenolic acids could be part of the possible mechanism by which the phenolic acids exert their antidiabetic effects.

Sign in / Sign up

Export Citation Format

Share Document