Morin inhibits the activity of pancreatic lipase and adipogenesis.

V P, Venkateish; Rajamanikandan, Sundarraj; Perumal, Madan Kumar

V P, Venkateish; Rajamanikandan, Sundarraj; Perumal, Madan Kumar.

Afiliación

V P V; Department of Biochemistry, CSIR-Central Food Technological Research Institute, Mysore, 570020, India; Academy of Scientific and Innovative Research (AcSIR), Ghaziabad, 201002, India.
Rajamanikandan S; Centre for Drug Discovery, Department of Biochemistry, Karpagam Academy of Higher Education, Coimbatore, 641021, Tamil Nadu, India.
Perumal MK; Department of Biochemistry, CSIR-Central Food Technological Research Institute, Mysore, 570020, India; Academy of Scientific and Innovative Research (AcSIR), Ghaziabad, 201002, India. Electronic address: madanperumal@cftri.res.in.

Eur J Pharmacol ; 977: 176705, 2024 Aug 15.

Article en En | MEDLINE | ID: mdl-38830457

ABSTRACT

ABSTRACT

Obesity is a major health issue that contributes significantly to increased mortality and morbidity worldwide. Obesity is caused by uncontrolled adipogenesis and lipogenesis, leading to several metabolism-associated problems. Pancreatic lipase, an enzyme that breaks down dietary lipids, is a prominent target for obesity. Orlistat, a known inhibitor of pancreatic lipase, is commonly employed for the management of obesity. However, its side effects, such as diarrhoea, nausea and bladder pain, urge to look out for safer alternatives. Morin is a pentahydroxyflavone, exerts a broad spectrum of pharmacological effects including antioxidant, anti-inflammatory, lipid lowering, anti-diabetic, anti-fibrotic, anti-cancer, etc. This study investigated the effect of morin on pancreatic lipase activity, in vitro and in vivo adipogenesis. Molecular docking and simulation studies showed morin to have a higher binding affinity towards pancreatic lipase compared with orlistat, which also inhibited its activity in vitro. Morin also reduced lipid droplet accretion and downregulated the expression of adipogenic and lipogenic genes. The acute oral toxicity of morin was determined in C57BL/6 mice, where morin did not show toxicity up to 2000 mg/kg body weight dose. Oral administration of morin to high fat diet fed mice reduced body weight, glucose and insulin levels. Also, the histopathological examination revealed reduction in adipocyte size and decreased mRNA expression of adipogenesis markers in white adipose tissue of morin administered group compared to high fat diet group. Overall, the results suggested morin inhibited pancreatic lipase activity, adipogenesis and further studies are warranted to explore its therapeutic potential for obesity.

Asunto(s)

Adipogénesis; Flavonoides; Lipasa; Ratones Endogámicos C57BL; Simulación del Acoplamiento Molecular; Animales; Adipogénesis/efectos de los fármacos; Flavonoides/farmacología; Ratones; Lipasa/antagonistas & inhibidores; Lipasa/metabolismo; Masculino; Células 3T3-L1; Dieta Alta en Grasa/efectos adversos; Páncreas/efectos de los fármacos; Páncreas/patología; Fármacos Antiobesidad/farmacología; Obesidad/tratamiento farmacológico; Obesidad/metabolismo; Adipocitos/efectos de los fármacos; Adipocitos/metabolismo; Humanos; Orlistat/farmacología; Flavonas

Palabras clave

Acute oral toxicity; Adipogenesis; High fat diet; Morin; Obesity; Pancreatic lipase

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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Flavonoides / Adipogénesis / Simulación del Acoplamiento Molecular / Lipasa / Ratones Endogámicos C57BL Límite: Animals / Humans / Male Idioma: En Revista: Eur J Pharmacol Año: 2024 Tipo del documento: Article País de afiliación: India Pais de publicación: Países Bajos

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