scholarly journals Chemical Composition andα-Glucosidase Inhibitory Activity of VietnameseCitrusPeels Essential Oils

2016 ◽  
Vol 2016 ◽  
pp. 1-5 ◽  
Author(s):  
Nguyen Hai Dang ◽  
Pham Huong Nhung ◽  
Bui Thi Mai Anh ◽  
Dinh Thi Thu Thuy ◽  
Chau Van Minh ◽  
...  

Background. Inhibition ofα-glucosidase is an important factor to control postprandial hyperglycemia in type 2 diabetes mellitus.Citrusessential oils (CEO) are among the most widely used essential oils, and some of them exhibited promising antidiabetic effect. However, theα-glucosidase inhibition of CEO has not been investigated so far. The present work aims to evaluate theα-glucosidase inhibition of essential oils from six VietnameseCitruspeels.Methods. The chemical composition of essential oils obtained by hydrodistillation from sixCitruspeels was analyzed by GC-MS. All essential oils were tested for their inhibitory activity onα-glucosidase usingp-nitrophenyl-α-D-glucopyranoside as substrate.Results. In Buddha’s hand and lime peels, the major components were limonene (59.0–61.31%) andγ-terpinene (13.98–23.84%) while limonene (90.95–95.74%) was most abundant in pomelo, orange, tangerine, and calamondin peels. Among the essential oils, the Buddha’s hand oil showed the most significantα-glucosidase inhibitory effect with the IC50value of 412.2 μg/mL. The combination of the Buddha’s hand essential oil and the antidiabetic drug acarbose increased the inhibitory effect.Conclusions. The results suggested the potential use of Buddha’s hand essential oil as an alternative in treatment of type 2 diabetes mellitus.

Molecules ◽  
2019 ◽  
Vol 24 (9) ◽  
pp. 1776 ◽  
Author(s):  
Zhihua Liu ◽  
Ying Yang ◽  
Wujun Dong ◽  
Quan Liu ◽  
Renyun Wang ◽  
...  

α-glucosidase inhibitors (AGIs) have been an important category of oral antidiabetic drugs being widely exploited for the effective management of type 2 diabetes mellitus. However, the marketed AGIs not only inhibited the disaccharidases, but also exhibited an excessive inhibitory effect on α-amylase, resulting in undesirable gastrointestinal side effects. Compared to these agents, Ramulus Mori alkaloids (SZ-A), was a group of effective alkaloids from natural Morus alba L., and showed excellent hypoglycemic effect and fewer side effects in the Phase II/III clinical trials. Thus, this paper aims to investigate the selective inhibitory effect and mechanism of SZ-A and its major active ingredients (1-DNJ, FA and DAB) on different α-glucosidases (α-amylase and disaccharidases) by using a combination of kinetic analysis and molecular docking approaches. From the results, SZ-A displayed a strong inhibitory effect on maltase and sucrase with an IC50 of 0.06 μg/mL and 0.03 μg/mL, respectively, which was similar to the positive control of acarbose with an IC50 of 0.07 μg/mL and 0.68 μg/mL. With regard to α-amylase, SZ-A exhibited no inhibitory activity at 100 μg/mL, while acarbose showed an obvious inhibitory effect with an IC50 of 1.74 μg/mL. The above analysis demonstrated that SZ-A could selectively inhibit disaccharidase to reduce hyperglycemia with a reversible competitive inhibition, which was primarily attributed to the three major active ingredients of SZ-A, especially 1-DNJ molecule. In the light of these findings, molecular docking study was utilized to analyze their inhibition mechanisms at molecular level. It pointed out that acarbose with a four-ring structure could perform desirable interactions with various α-glucosidases, while the three active ingredients of SZ-A, belonging to monocyclic compounds, had a high affinity to the active site of disaccharidases through forming a wide range of hydrogen bonds, whose affinity and consensus score with α-amylase was significantly lower than that of acarbose. Our study illustrates the selective inhibition mechanism of SZ-A on α-glucosidase for the first time, which is of great importance for the treatment of type 2 diabetes mellitus.


2021 ◽  
Vol 65 (4) ◽  
Author(s):  
Hafsa Chouit ◽  
Ouassila Touafek ◽  
Moussa Brada ◽  
Chawki Benssouici ◽  
Marie-Laure Fauconnier ◽  
...  

Abstract. Salvia microphylla is a known species due to its broad uses in traditional medicine against memory loss and rheumatism. The knowledge regarding the chemical composition and biological activities of the species collected in Algeria, no studies have been reported in the literature. Therefore, the present work focuses on the characterization of the chemical composition of the essential oils (EOs) and the determination of the antioxidant, anticholinesterase, α-glucosidase, and antimicrobial activities of Salvia microphylla. The EOs were obtained by hydrodistillation from the aerial parts, leaves and stems and submitted to chemical analysis by GC and GC/MS. The β-Caryophyllene was identified as the main constituent in the aerial parts and leaves essential oils with 16.75 ± 0.02 % and 17.86 ± 0.07 %, respectively. Likewise, the α-Eudesmol was the predominant component in the stems oil with (21.47 ± 0.20 %). The antioxidant activity of EOs was estimated through using four comparative methods: DPPH, ABTS•+, Reducing power and CUPRAC assays. The Stems oil was the most active one in CUPRAC assay, with an IC50 value with 7.72 ± 0.43 µg/mL. The enzyme inhibitory activity of the essential oils was realized against key enzymes involved in type 2 diabetes (α-glucosidase) using 4-Nitrophenyl-α-d-glucopyranoside as substrate and in neurodegenerative (AChE and BChE) diseases. The highest anticholinesterase activity against acetylcholinesterase was observed in the EO of aerial parts essential  (IC50: 23.65 ± 0.73 µg/mL). The EO isolated from stems (IC50: 37.07 ± 1.44 µg/mL) exhibited a butyrylcholinesterase activity very close to that of analytical standard galantamine (IC50: 34.75 ± 1.99 µg/mL). Furthermore, all EOs displayed high inhibitory activity against α-glucosidase, better to that of the standard acarbose. The EOs of Salvia microphylla display potential properties against type 2 diabetes. A broth microdilution method was used to evaluate the antimicrobial activity of Salvia microphylla EOs, against eleven microbial strains and two yeast. The EOs showed better antibacterial activity against Gram-positive and Gram-negative bacteria except for Pseudomonas aeruginosa, with the stems essential oil being more efficient. Moreover, significant antifungal activity was observed against Candida albicans.   Resumen. Salvia microphylla es una specie conocida debido a su amplio uso en medicina tradicional, contra la pérdida de memoria y el reumatismo. En el caso de la especie de planta recolectada en Algeria, no hay datos publicados sobre su composición química y sus actividades biológicas. Por ello, el presente trabajo ha sido enfocado en la caracterización de la composición química de aceites esenciales (EOs) de Salvia microphylla y en la determinación de sus actividades antioxidante, anticolinesterasa, α-glucosidasa y antimicrobiano. Los EOs fueron obtenidos mediante hidrodestilación de las partes aéreas, ojas y tallos, y fueron sometidos al análisis por cromatografía de gases con detección por ionización en flama y por espectrometría de masas. Se identificó a β-cariofileno como el componente principal de los aceites de las partes aéreas y de tallos con concentraciones de 16.75 ± 0.02 % y 17.86 ± 0.07 %, respectivamente. Por su parte, el α-Eudesmol fue encontrado como componente predominante en aceite de tallos (21.47 ± 0.20 %). La actividad antioxidante de los EOs fue estimada en base a cuatro métodos compartivos: DPPH, ABTS•+, poder reductor y ensayo CUPRAC. El aceite de tallos resultó ser el más activo en ensayo CUPRAC, con el valor IC50 de 7.72 ± 0.43 µg/mL. La actividad inhibitora de enzimas de los EOs fue evaluada contra principales enzimas involucrados en diabetes tipo 2 (α-glucosidasa), utilizando 4-Nitrofenil-α-d-glucopiranosida como sustrato, y en enfermedades neurodergenerativas (AChE y BChE). La mayor actividad anticolinesterasa y acetilcolinesterasa fue observada en el EO de partes aéreas (IC50: 23.65 ± 0.73 µg/mL). El EO islado de tallos (IC50: 37.07 ± 1.44 µg/mL) presentó actividad de butirilcolinestarasa muy similar a la del estándar analítico, galantamina (IC50: 34.75 ± 1.99 µg/mL). Aunado a ello, todos EOs presentaron una alta actividad inhibitora contra α-glucosidasa, que era mejor comparando con la del estándar de acarbosa. Los EOs de Salvia microphylla presentan potenciales propiedades contra diabetes tipo 2. Para evaluar la actividad antimicrobiana de los EOs de Salvia microphylla, se utilizó el método de microdulución en caldo, contra once sepas microbianas y dos de levadura. La mejor actividad se observó contra bacterias Gram-positivas y Gram-negativas, excepto Pseudomonas aeruginosa, los cuales presentaron alta resistencia. Los EOs presentaron también importante actividad antifungica contra Candida albicans.


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