(E)-4- Aminostyryl Acetate a Novel Pancreatic Lipase Inhibitor Produced by a Streptomyces sp. MTCC 5219

Tokdar, Pradipta; Ranadive, Prafull; Mascarenhas, Malcolm; Patil, Shashikant S.; George, Saji

doi:10.7763/ijcea.2011.v2.90

Cited by 5 publications

(5 citation statements)

References 5 publications

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“…Thirty-nine soil samples were collected from different areas in Egypt; 38.5% of the samples showed PL inhibition activity, 66.67% of which were agriculture soils. This is in accordance with previous studies from India that reported the isolation of PL inhibitor producers from field soils [24,25]. In our study, the active PL inhibitor producer (AspsarO) was identified as Aspergillus oryzae based on its colony morphology, microscopical characteristics together with 18S rDNA sequencing.…”

Section: Discussionsupporting

confidence: 92%

Kojic acid repurposing as a pancreatic lipase inhibitor and the optimization of its production from a local Aspergillus oryzae soil isolate

et al. 2020

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Background Obesity and its related diseases are increasing worldwide. One of the best therapeutic strategies for obesity management is through the inhibition of pancreatic lipase (PL) enzyme. So far orlistat is the only FDA approved PL inhibitor, but with unpleasant side effects. New efficacious anti-obesity drugs are needed to achieve a successful reduction in the incidence and prevalence of obesity. Many microbial metabolites have PL inhibitory activity. Screening soil inhabitants for PL inhibitors could help in increasing the available anti-obesity drugs. We aimed to isolate and identify alternative PL inhibitors from soil flora. Results We screened the crude mycelial methanolic extracts of 39 soil samples for PL inhibitory activity by the quantitative lipase colorimetric assay, using the substrate p-nitrophenyl palmitate and orlistat as positive control. AspsarO, a PL inhibitor producer, was isolated from an agricultural field soil in Giza, Egypt. It was identified as Aspergillus oryzae using colony morphology, microscopical characteristics, 18S rDNA sequencing, and molecular phylogeny. Increasing the PL inhibitor activity, in AspsarO cultures, from 25.9 ± 2% to 61.4 ± 1.8% was achieved by optimizing the fermentation process using a Placket–Burman design. The dried 100% methanolic fraction of the AspsarO culture had an IC50 of 7.48 μg/ml compared to 3.72 μg/ml for orlistat. It decreased the percent weight gain, significantly reduced the food intake and serum triglycerides levels in high-fat diet-fed Sprague–Dawley rats. Kojic acid, the active metabolite, was identified using several biological guided chromatographic and 1H and 13C NMR techniques and had an IC50 of 6.62 μg/ml. Docking pattern attributed this effect to the interaction of kojic acid with the key amino acids (Lys80, Trp252, and Asn84) in PL enzyme binding site. Conclusion Combining the results of the induced obesity animal model, in silico molecular docking and the lipase inhibitory assay, suggests that kojic acid can be a new therapeutic option for obesity management. Besides, it can lower serum triglycerides in obese patients.

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Section: Discussionsupporting

confidence: 92%

Kojic acid repurposing as a pancreatic lipase inhibitor and the optimization of its production from a local Aspergillus oryzae soil isolate

et al. 2020

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“…The species of actinomycetes were known to produce various compounds that have different biomedical applications. Lipase inhibitors such as lipstatin [14,15], panclicins A-E, ebelactones A and B, valilactone [11], esterastin, cyclipostins, (E)-4-aminostyryl acetate [2], streptolysin [12], ε-poly-L-lysine, and shamistatin [16] were reported from actinomycetes species. In the present study, 20 actinomycetes strains were isolated from different parts of Periyar Tiger Reserve.…”

Section: Discussionmentioning

confidence: 99%

“…Obesity is a lipid metabolism disorder and ranks fifth for death caused worldwide. Absorption of dietary lipids is targeted for developing anti-obesity compounds [1,2]. Compounds belonging to certain classes of natural products are broadly studied for antiobesity activities, such compound includes polyphenols, terpenoids, polysaccharides, and glycosides.…”

Section: Introductionmentioning

confidence: 99%

Screening of Actinomycetes Isolated From Natural Ecosystem (Periyar Tiger Reserve, Kerala) for Lipase Inhibitory Activities

KUMARI¹,

SURENDRAN²,

KHYMDEIT³

et al. 2019

Asian J Pharm Clin Res

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Objectives: The present study was undertaken to screen pancreatic lipase inhibitory activity of crude extracts of actinomycetes species isolated from the soil sediments of Periyar Tiger Reserve, Kerala. The identified lipase inhibitory activity was partially purified, and the selected isolate was identified by 16S rRNA sequencing. Methods: The preliminary screening for the extracellular lipase inhibitory activities of actinomycetes isolates was performed by inoculating the culture to the test tubes containing inoculation media in submerged condition. The lipase inhibitory activities were again evaluated based on secondary screening on the production media and the strain which produced consistent highest lipase inhibitory activity was selected for further studies. The crude extract from the selected strain was subjected to solvent extraction and partially purified by plain silica gel column (mesh size 100–200 μm; column 300 mm×18 mm) and eluted with different solvents in the increasing order of polarity and all the solvent fractions were checked for lipase inhibitory activity. Results: Based on the secondary screening on the production of media, DDE6 strain showed highest lipase inhibitory activity (96.2%) and was selected for further studies. The dichloromethane extract showed the highest lipase inhibitory activity (96.38%) when compared to other solvents. The partial 16S rRNA sequence analysis of DDE6 isolate confirmed the strain as Curtobacterium oceanosedimentum. Conclusion: Many research publications have reported the isolation of Curtobacterium species and its type strains. However, this is the first time to report its potential to produce lipase inhibitor metabolite under submerged fermentation conditions. Further, studies are needed to be conducted to characterize the active principle of lipase inhibition as well as to elucidate the structure of the extracted compound.

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“…Streptomyces sp. MTCC 5219 from the soil in India was reported to produce (E)-4-Aminostyryl, which is another type of pancreatic lipase inhibitor substance (Tokdar et al 2011). The study of Kekuda et al (2011) showed that Streptomyces isolated from soil in Karnataka region, India has the ability as an antiobesity with the highest inhibition value 61.67%.…”

Section: Pancreatic Lipase Inhibitory Activitymentioning

confidence: 99%

“…MTCC 5219 and Streptomyces sp. NR 0619 (Kekuda et al 2011;Tokdar et al 2011;Mutoh et al 1994). Actinobacteria as producer of various bioactive compounds have great potential for industrial application (Golinska et al 2015).…”

Section: Introductionmentioning

confidence: 99%

Diversity of endophytic actinobacteria isolated from medicinal plants and their potency as pancreatic lipase inhibitor

Fitri

2017

Biodiversitas

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Endophytic actinobacteria from medicinal plants have high diversity and potency to produce secondary metabolites with various biological functions, including the activity of lipase inhibitor. As it has been widely known that inhibiting fat absorption through the activity of pancreatic lipase inhibitor is one of the most common treatments for weight loss. This study aimed to assess diversity and capability of endophytic actinobacteria in producing pancreatic lipase inhibitor from medicinal plants that were traditionally used as antiobesity. Medicinal plants used in this research were rhizome of Alpinia galanga, Kaempferiae galanga, K. rotunda, Zingiber cassumunar, and leaves of Murraya paniculata. The endophytic actinobacteria were isolated, purified, and assayed for lipase inhibitory activity. The selected isolates were molecularly identified based on 16S rRNA gene and compared for their close relationship with reference strains available in the GenBank. A total of 35 endophytic actinobacteria has been isolated from the five medicinal plants examined. The isolates showed to have various morphological diversity based on their colony and microscopic observations, and also to have various lipase inhibitory activity. The inhibition activity ranged from 6.1 to 96.5%. There were five selected endophytic actinobacteria which have lipase inhibitory activity higher than 90%. At the same concentration of sample (1300 ppm), the crude extract of AEBg12 showed slightly higher activity (95.3%) compared with orlistat (93.6%), used as a positive control. The partial sequences of 16S rRNA analyses showed that AEBg4 (1421 bp) had the highest similarity with Streptomyces sp. S170 (93%), followed by its close relationship with S. lannensis strain SR3-58 (93%), and S. lannensis JCM 16578 T (92%). Both AEBg10 (1051 bp) and AEBg12 (1010 bp) had the highest similarity with Streptomyces sp. S170 by 99% and 98%, respectively. The AEKp9 (1367 bp) had a close relationship with Streptomyces sp. DLDG2 (93%) and S. bellus NBRC 12844 T (93%). While for AELk3 (1033 bp), the similarity with Streptomyces sp. NRLL B-24869 was 98%. These research data can be considered as new information, regarding the capability of endophytic actinobacteria from medicinal plants, which have potency as antiobesity, through their pancreatic lipase inhibitory activity.

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(E)-4- Aminostyryl Acetate a Novel Pancreatic Lipase Inhibitor Produced by a Streptomyces sp. MTCC 5219

Cited by 5 publications

References 5 publications

Kojic acid repurposing as a pancreatic lipase inhibitor and the optimization of its production from a local Aspergillus oryzae soil isolate

Kojic acid repurposing as a pancreatic lipase inhibitor and the optimization of its production from a local Aspergillus oryzae soil isolate

Screening of Actinomycetes Isolated From Natural Ecosystem (Periyar Tiger Reserve, Kerala) for Lipase Inhibitory Activities

Diversity of endophytic actinobacteria isolated from medicinal plants and their potency as pancreatic lipase inhibitor

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