scholarly journals LC-QTOF-MS/MS Based Molecular Networking Approach for the Isolation of α-Glucosidase Inhibitors and Virucidal Agents from Coccinia grandis (L.) Voigt

Foods ◽  
2021 ◽  
Vol 10 (12) ◽  
pp. 3041
Author(s):  
Maharani A. Astiti ◽  
Akanitt Jittmittraphap ◽  
Pornsawan Leaungwutiwong ◽  
Nopporn Chutiwitoonchai ◽  
Patcharee Pripdeevech ◽  
...  

Coccinia grandis or ivy gourd is an edible plant. Its leaves and fruits are used as vegetable in many countries. Many works on antidiabetic activity of a crude extract of C. grandis, i.e., in vitro, in vivo, and clinical trials studies, have been reported. Profiles of the antidiabetic compounds were previously proposed by using LC-MS or GC-MS. However, the compounds responsible for antidiabetic activity have rarely been isolated and characterized by analysis of 1D and 2D NMR data. In the present work, UHPLC-ESI-QTOF-MS/MS analysis and GNPS molecular networking were used to guide the isolation of α-glucosidase inhibitors from an extract of C. grandis leaves. Seven flavonoid glycosides including rutin (1), kaempferol 3-O-rutinoside (2) or nicotiflorin, kaempferol 3-O-robinobioside (3), quercetin 3-O-robinobioside (4), quercetin 3-O-β-D-apiofuranosyl-(1→2)-[α-L-rhamnopyranosyl-(1→6)]-β-D-glucopyranoside (5) or CTN-986, kaempferol 3-O-β-D-api-furanosyl-(1→2)-[α-L-rhamnopyranosyl-(1→6)]-β-D-glucopyranoside (6), and kaempferol 3-O-β-D-apiofuranosyl-(1→2)-[α-L-rhamnopyranosyl-(1→6)]-β-D-galactopyranoside (7) were isolated from C. grandis leaves. This is the first report of glycosides containing apiose sugar in the genus Coccinia. These glycosides exhibited remarkable α-glucosidase inhibitory activity, being 4.4–10.3 times more potent than acarbose. Moreover, they also displayed virucidal activity against influenza A virus H1N1, as revealed by the ASTM E1053-20 method.

2012 ◽  
Vol 2012 ◽  
pp. 1-10 ◽  
Author(s):  
Sougata Ghosh ◽  
Mehul Ahire ◽  
Sumersing Patil ◽  
Amit Jabgunde ◽  
Meenakshi Bhat Dusane ◽  
...  

Diabetes is a metabolic disorder affecting about 220 million people worldwide. One of the most critical complications of diabetes is post-prandial hyper-glycemia (PPHG). Glucosidase inhibitor andα-amylase inhibitors are class of compounds that help in managing PPHG. Low-cost herbal treatment is recommended due to their lesser side effect for treatment of diabetes. Two plants with significant traditional therapeutic potential, namely,Gnidia glaucaandDioscorea bulbifera, were tested for their efficiency to inhibitα-amylase andα-glucosidase. Stem, leaf, and flower ofG. glaucaand bulb ofD. bulbiferawere sequentially extracted with petroleum ether, ethyl acetate, and methanol as well as separately with 70% ethanol. Petroleum ether extract of flower ofG. glaucawas found to inhibitα-amylase significantly (78.56%). Extracts were further tested against crude murine pancreatic, small intestinal, and liver glucosidase enzyme which revealed excellent inhibitory properties.α-glucosidase inhibition provided a strongin vitroevidence for confirmation of bothG. glaucaandD. bulbiferaas excellent antidiabetic remedy. This is the first report of its kind that provides a strong biochemical basis for management of type II diabetes usingG. glaucaandD. bulbifera. These results provide intense rationale for furtherin vivoand clinical study.


2020 ◽  
Vol 26 ◽  
Author(s):  
Shaik Ibrahim Khalivulla ◽  
Arifullah Mohammed ◽  
Kokkanti Mallikarjuna

Background: Diabetes is a chronic disease affecting a large population worldwide and stands as one of the major global health challenges to be tackled. According to World Health Organization, about 400 million are having diabetes worldwide and it is the seventh leading cause of deaths in 2016. Plant based natural products had been in use from ancient time as ethnomedicine for the treatment of several diseases including diabetes. As a result of that, there are several reports on plant based natural products displaying antidiabetic activity. In the current review, such antidiabetic potential compounds reported from all plant sources along with their chemical structures are collected, presented and discussed. This kind of reports are essential to pool the available information to one source followed by statistical analysis and screening to check the efficacy of all known compounds in a comparative sense. This kind of analysis can give rise to few numbers of potential compounds from hundreds, whom can further be screened through in vitro and in vivo studies, and human trails leading to the drug development. Methods: Phytochemicals along with their potential antidiabetic property were classified according to their basic chemical skeleton. The chemical structures of all the compounds with antidiabetic activities were elucidated in the present review. In addition to this, the distribution and their other remarkable pharmacological activities of each species is also included. Results: The scrutiny of literature led to identification of 44 plants with antidiabetic compounds (70) and other pharmacological activities. For the sake of information, the distribution of each species in the world is given. Many plant derivatives may exert antidiabetic properties by improving or mimicking the insulin production or action. Different classes of compounds including sulfur compounds (1-4), alkaloids (5-11), phenolic compounds (12-17), tannins (18-23), phenylpropanoids (24-27), xanthanoids (28-31), amino acid (32), stilbenoid (33), benzofuran (34), coumarin (35), flavonoids (36-49) and terpenoids (50-70) were found to be active potential compounds for antidiabetic activity. Of the 70 listed compounds, majorly 17 compounds are from triterpenoids, 13 flavonoids and 7 are from alkaloids. Among all the 44 plant species, maximum number (7) of compounds are reported from Lagerstroemia speciosa followed by Momordica charantia (6) and S. oblonga with 5 compounds. Conclusion: This is the first paper to summarize the established chemical structures of phytochemicals that have been successfully screened for antidiabetic potential and their mechanisms of inhibition. The reported compounds could be considered as potential lead molecules for the treatment of type-2 diabetes. Further, molecular and clinical trials are required to select and establish the therapeutic drug candidates.


Chemotherapy ◽  
1995 ◽  
Vol 41 (6) ◽  
pp. 455-461 ◽  
Author(s):  
Robert W. Sidwell ◽  
Kevin W. Bailey ◽  
Min Hui Wong ◽  
John H. Huffman
Keyword(s):  

2011 ◽  
Vol 46 (6) ◽  
pp. 2243-2251 ◽  
Author(s):  
Juan José Ramírez-Espinosa ◽  
Maria Yolanda Rios ◽  
Sugey López-Martínez ◽  
Fabian López-Vallejo ◽  
José L. Medina-Franco ◽  
...  

2014 ◽  
Vol 5 ◽  
Author(s):  
Emanuel Haasbach ◽  
Carmen Hartmayer ◽  
Alice Hettler ◽  
Alicja Sarnecka ◽  
Ulrich Wulle ◽  
...  

Plants ◽  
2022 ◽  
Vol 11 (2) ◽  
pp. 208
Author(s):  
Ahlam Elwekeel ◽  
Dalia El Amir ◽  
Enas I. A. Mohamed ◽  
Elham Amin ◽  
Marwa H. A. Hassan ◽  
...  

The current study accentuates the significance of performing the multiplex approach of LC-HRESIMS, biological activity, and docking studies in drug discovery, taking into consideration a review of the literature. In this regard, the investigation of antioxidant and cytotoxic activities of Trigonella stellata collected from the Egyptian desert revealed a significant antioxidant capacity using DPPH with IC50 = 656.9 µg/mL and a moderate cytotoxicity against HepG2, MCF7, and CACO2, with IC50 values of 53.3, 48.3, and 55.8 µg/mL, respectively. The evaluation of total phenolic and flavonoid contents resulted in 32.8 mg GAE/g calculated as gallic acid equivalent and 5.6 mg RE/g calculated as rutin equivalent, respectively. Chemical profiling of T. stellata extract, using LC-HRESIMS analysis, revealed the presence of 15 metabolites, among which eleven compounds were detected for the first time in this species. Interestingly, in vitro testing of the antidiabetic activity of the alcoholic extract noted an α-glucosidase enzyme inhibitory activity (IC50 = 559.4 µg/mL) better than that of the standard Acarbose (IC50 = 799.9 µg/mL), in addition to a moderate inhibition of the α-amylase enzyme (IC50 = 0.77 µg/mL) compared to Acarbose (IC50 = 0.21 µg/mL). α-Glucosidase inhibition was also virtualized by binding interactions through the molecular docking study, presenting a high binding activity of six flavonoid glycosides, as well as the diterpenoid compound graecumoside A and the alkaloid fenugreekine. Taken together, the conglomeration of LC-HRESIMS, antidiabetic activity, and molecular docking studies shed light on T. stellata as a promising antidiabetic herb.


2021 ◽  
Vol 22 (17) ◽  
pp. 9508
Author(s):  
Nhung Thi Phuong Nong ◽  
Jue-Liang Hsu

Diabetes, a glucose metabolic disorder, is considered one of the biggest challenges associated with a complex complication of health crises in the modern lifestyle. Inhibition or reduction of the dipeptidyl peptidase IV (DPP-IV), alpha-glucosidase, and protein-tyrosine phosphatase 1B (PTP-1B) enzyme activities or expressions are notably considered as the promising therapeutic strategies for the management of type 2 diabetes (T2D). Various food protein-derived antidiabetic bioactive peptides have been isolated and verified. This review provides an overview of the DPP-IV, PTP-1B, and α-glucosidase inhibitors, and updates on the methods for the discovery of DPP-IV inhibitory peptides released from food-protein hydrolysate. The finding of novel bioactive peptides involves studies about the strategy of separation fractionation, the identification of peptide sequences, and the evaluation of peptide characteristics in vitro, in silico, in situ, and in vivo. The potential of bioactive peptides suggests useful applications in the prevention and management of diabetes. Furthermore, evidence of clinical studies is necessary for the validation of these peptides’ efficiencies before commercial applications.


Author(s):  
Fatma Zahra Sakhri ◽  
Sakina Zerizer ◽  
Chawki Bensouici

Dietary natural antioxidant consumption can protect the human body from several diseases induced by free radicals. The aim of this study was to evaluate the antioxidant, antidiabetic and immunomodulatory properties of Cydonia oblonga fruit. For this; hydroethanolic extract of Cydonia oblonga fruit (HECO) was examined for antioxidant activity using DPPH free radical sc avenging, ABTS cation radical decolorization, Cupric reducing antioxidant capacity (CUPRAC), and Metal Chelating on ferrous ions activities. The inhibitory activity of the extract against α-glucosidase enzyme was also investigated. HECO was tested in vivo for the immunomodulatory activity on non-specific immunity by the carbon clearance test. The content of the nonenzymatic antioxidant reduced glutathione (GSH) in liver tissue of used mice was estimated. in vitro studies revealed that the HECO has an inhibitory concentration (IC50) value of 249.26 ± 3.75μg/mL, 117.34 ± 1.41 μg/ml for DPPH and ABTS scavenging activity respectively. As well as the ability to reduce cupric (167.17 ± 1.15μg/mL) and iron (Fe) (417.98 ± 48.82μg/mL). The extract showed antidiabetic activity as evidenced by its capacity to inhibit the α-glucosidase enzyme (IC50: 326.48 ± 18.56 µg/mL) near the acarbose (IC50: 275.98 ± 1.57 µg/mL) used as a positive control. In addition, our results showed that HECO at the concentration of 50 and 100 mg/kg significantly increased the clearance rate of carbon from the bloodstream concomitant with increased liberation of GSH from liver cells. This study demonstrates that HECO is effective in scavenging free radicals and can serve as potent antioxidants that provide potential treatment and prevention for diabetes with benefits on the innate defense system. Keywords: Antidiabetic, Antioxidant, Cydonia oblonga, Hydroethanolic extract, Phagocytic activity


Sign in / Sign up

Export Citation Format

Share Document