α-Glucosidase Inhibitors from <i>Malbranchea flavorosea</i>

Verastegui-Omaña, Brisa; Rebollar-Ramos, Daniela; Pérez-Vásquez, Araceli; Martı́nez, Ana; Madariaga-Mazón, Abraham; Flores‐Bocanegra, Laura; Mata, Rachel

doi:10.1021/acs.jnatprod.6b00977

Cited by 23 publications

(24 citation statements)

References 30 publications

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“…Docking of 32 to hNt-MGAM and hCt-MGAM as well as to hNt-SI and y-IM predicted that it would bind to them far from the catalytic site; the interacting forces were mainly by hydrophobic contacts and hydrogen bonding (HB). The overall docking results were consistent with the in vitro α-glucosidase inhibitory properties of compound 32 and predicted that its inhibitory action could be exerted throughout an allosteric interaction with the enzymes [25]. Further research is in progress to assess how it is absorbed, distributed, metabolized, and excreted.…”

Section: Fungal Endophytes From Hintonia Latiflorasupporting

confidence: 68%

“…The last fungus selected for the search of α-glucosidase inhibitors was M. flavorosea. From the active extract prepared from the grain-based culture, two new polyketides, namely, 8-chloroxylarinol A (27) and flavoroseoside (28), along with the known compounds xylarinol A (29), xylarinol B (30), massarigenins B and C (31 and 32), and clavatol (33), were isolated [25] (▶ Fig. 5).…”

Section: Fungal Endophytes From Hintonia Latifloramentioning

confidence: 99%

“…Thus, a few showed potential as antidiabetic drugs with α-glucosidase inhibitory activity. Preclinical pharmacological evidence indicated that most of them were more active than acarbose, and some, like benzomalvin A (25), also possess antihyperalgesic properties of utility for treating diabetic neuropathies. Another, malbrancheamide (75), is a vasorelaxant compound with a maximum effect of almost 100 %, which is unusual for a natural product.…”

Section: Concluding Remarks and Outlookmentioning

confidence: 99%

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Insights in Fungal Bioprospecting in Mexico

et al. 2018

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Fungi have consistently been one of the richest sources of natural products, with unprecedented chemical scaffolds and potent biological activities. During the last 20 years, pharmacognosy researchers in Mexico, in collaboration with mycologists, have discovered many novel bioactive fungi natural products and new fungal species. To date, more than 100 bioactive secondary metabolites from 20 fungi from different ecosystems throughout Mexico have been documented in peer-reviewed literature according to Scopus and SciFinder databases. These include compounds from different biosynthetic origins and structural cores with the potential for the development of anticancer, antidiabetic, and/or pesticide agents.

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Section: Fungal Endophytes From Hintonia Latiflorasupporting

confidence: 68%

Section: Fungal Endophytes From Hintonia Latifloramentioning

confidence: 99%

Section: Concluding Remarks and Outlookmentioning

confidence: 99%

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Insights in Fungal Bioprospecting in Mexico

et al. 2018

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“…As a result of this side effects and other constraints; patients now prefer to use locally available herbs to treat diabetes, especially those plant and plant parts that are already consumed as food or food condiments since these plants have been seen to have lower side effects and are quite affordable. Several plants have been reported to have alphaglucosidase inhibitory activity (32)(33)(34)(35). Momordica charantia being one of such plants, also the fact that several types of research (13)(14)(15)(16)(17) have shown the potency of the plant in the management of diabetes, it, therefore, justifies the focus of this particular research.…”

Section: Discussionmentioning

confidence: 93%

IN VITRO EFFECT OF TERPENOIDS - RICH EXTRACT OF Momordica charantia ON ALPHA GLUCOSIDASE ACTIVITY

Sallau

Yakubu

Aliyu

et al. 2018

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Background: Momordica charantia is a vine, native to tropics and subtropics that has found use in herbal medicine. In Nigeria, the plant is locally used in the treatment of diabetes. Objective: To investigate the inhibitory effect of terpenoid-rich extract from Momordica charantia on α-glucosidase activity. Method: The inhibitory effect of the terpenoid-rich extract from Momordica charantia on the activity of alpha-glucosidase from Saccharomyces cerevisiae as well as the determination of the mode of inhibition were investigated using in vitro assay methods. Results: The results revealed that the terpenoid-rich extract had a high IC 50 of 1.60 mg/mL. The Lineweaver-Burk plot revealed that the extract exhibited partially mixed-type inhibition of α-glucosidase. Conclusions: It can be inferred from this study that although terpenoid-rich extract inhibited α-glucosidase, further purification will be necessary on the extract so as to increase its potency as an inhibitor of α-glucosidase. The action of the extract on α-glucosidase provided an insight into the probable mechanism of action of Momordica charantia in reducing hyperglycemia.

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“…As shown for a few examples in Tables 2-4 which consist in a sampling of recently reported works on natural compounds, this "Systematism" is already used by a few groups who catalogued the chemical compounds in a given organ of a given plant (Batista et al, 2017;Sendker et al, 2017;Ma et al, 2018;Sharma et al, 2018), in a fungus (Chang et al, 2017), or in a microorganism (McMullin et al, 2017;Verastegui-Omana et al, 2017). In such cases, an idea of the possible diversity of those sources is given.…”

Section: At the Development Stage: Systematic Inventories Of Natural mentioning

confidence: 99%

Unraveling Plant Natural Chemical Diversity for Drug Discovery Purposes

Lautie

Russo

Ducrot³

2020

Front. Pharmacol.

156

120

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The screening and testing of extracts against a variety of pharmacological targets in order to benefit from the immense natural chemical diversity is a concern in many laboratories worldwide. And several successes have been recorded in finding new actives in natural products, some of which have become new drugs or new sources of inspiration for drugs. But in view of the vast amount of research on the subject, it is surprising that not more drug candidates were found. In our view, it is fundamental to reflect upon the approaches of such drug discovery programs and the technical processes that are used, along with their inherent difficulties and biases. Based on an extensive survey of recent publications, we discuss the origin and the variety of natural chemical diversity as well as the strategies to having the potential to embrace this diversity. It seemed to us that some of the difficulties of the area could be related with the technical approaches that are used, so the present review begins with synthetizing some of the more used discovery strategies, exemplifying some key points, in order to address some of their limitations. It appears that one of the challenges of natural product-based drug discovery programs should be an easier access to renewable sources of plant-derived products. Maximizing the use of the data together with the exploration of chemical diversity while working on reasonable supply of natural product-based entities could be a way to answer this challenge. We suggested alternative ways to access and explore part of this chemical diversity with in vitro cultures. We also reinforced how important it was organizing and making available this worldwide knowledge in an "inventory" of natural products and their sources. And finally, we focused on strategies based on synthetic biology and syntheses that allow reaching industrial scale supply. Approaches based on the opportunities lying in untapped natural plant chemical diversity are also considered.

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α-Glucosidase Inhibitors from Malbranchea flavorosea

Cited by 23 publications

References 30 publications

Insights in Fungal Bioprospecting in Mexico

Insights in Fungal Bioprospecting in Mexico

IN VITRO EFFECT OF TERPENOIDS - RICH EXTRACT OF Momordica charantia ON ALPHA GLUCOSIDASE ACTIVITY

Unraveling Plant Natural Chemical Diversity for Drug Discovery Purposes

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