Isolation of Actinomycetes and Screening for Lipase Inhibitors Production

2021 ◽  
Vol 17 ◽  
Author(s):  
Shivabai Chandwad ◽  
Chandrasen Chandwad ◽  
Sudhakar Gutte

Background: Obesity is a growing global health problem. Obesity leads to cardiovascular disorders, musculoskeletal disorders, diabetes, and certain types of cancer. One of the approach to control and treatment of obesity has involved inhibition of dietary lipid digestion by pancreatic lipase inhibitors. Microbes and plant source provide a rich source of enzyme inhibitors including pancreatic lipase inhibitors that can be developed as a drug for obesity treatment. Objective: Objective of the work mainly focuses and highlights on the isolation of actinomycetes and screening for pancreatic lipase inhibitors production. Methods: Actinomycetes were isolated from soil samples by pre-treatment of samples and using selective growth medium with and without antibiotics. Isolated actinomycetes were grown in fermentation condition and metabolites were extracted with isopropyl alcohol and solvent evaporated to get crude material. Extract of each isolate screened for pancreatic lipase inhibition using p- nitrophenyl palmitate as substrate by spectroscopic method. Results: Total 86 actinomycetes strains were isolated from soil samples. Out of 86 extracts,10 extracts have shown positive results for porcine pancreatic lipase inhibition and inhibition activity was in the range of 10-80%. 50 % inhibitory concentration determined using 1 to 8 mg/mL extract in the assay. Extract of isolate A9, B3 and C6 having 50 % inhibitory activity below 3 mg/mL concentration and Orlistat as a standard has shown 50 % inhibitory activity at below 1 mg/mL concentration. Conclusion: The results conclude that actinomycetes are potential source of lipase inhibitors, which may lead to valuable novel drugs for obesity treatment.

2013 ◽  
Vol 8 (2) ◽  
pp. 1934578X1300800 ◽  
Author(s):  
Dilip Kumar ◽  
Aniket Karmase ◽  
Sneha Jagtap ◽  
Ruchi Shekhar ◽  
Kamlesh K Bhutani

In continuation towards the discovery of potential antiobesity lead(s) from natural products, we have screened n-hexane, dichloromethane (DCM), ethyl acetate (EtOAc) and methanol (MeOH) extracts of 33 Indian medicinal plants (200 extracts) for in vitro pancreatic lipase inhibitory activity. Of the screened extracts, the EtOAc extract of Cassia siamea roots showed 74.3±1.4% enzyme inhibition at 250 μg/mL concentration. Bioassay guided fractionation of the active extract afforded 6 known compounds viz. chrysophanol (1), physcion (2), emodin (3), cassiamin A (4), friedelin (5) and cycloart-25-en-3β,24-diol (6). These compounds were further evaluated for pancreatic lipase inhibitory activity. Cassiamin A (4), a bianthraquinone, was found to be most active with an IC50 value of 41.8±1.2 μM and compounds 2 and 5 were found to be moderate enzyme inhibitors. Results indicate the antiobesity potential of C. siamea through pancreatic lipase inhibition.


2020 ◽  
Vol 44 (28) ◽  
pp. 12355-12369
Author(s):  
Sridhar S. N. C. ◽  
Saksham Palawat ◽  
Atish T. Paul

Twenty-one indolyl oxoacetamides were designed and synthesized inspired by conophylline. Analogues 12c and 12b with N-geranyl substitution on indole exhibited potent pancreatic lipase inhibition.


INDIAN DRUGS ◽  
2021 ◽  
Vol 57 (12) ◽  
pp. 41-50
Author(s):  
Priyanka Rathod ◽  
Chandana Kulkarni ◽  
Raman P. Yadav

In recent years, pancreatic lipase inhibitor and α- glucosidase inhibitor have been highlighted as potential anti-diabesity principles. In the present study, seeds of Phyllanthus emblica L. (Family: Phyllanthaceae) was studied for anti-diabesity potential in terms of pancreatic lipase inhibitory activity, α-glucosidase inhibitory activity and antioxidant activity. At 100μg/ml concentration, pancreatic lipase inhibition of the methanolic extract using synthetic substrate obtained was 73.2±0.1% (IC50 59.1μg/ml), whereas pancreatic lipase inhibition using natural substrate was 87.9 ± 2.62%. α- glucosidase inhibition of the extract at 50μg/ml was measured as 94.4±0.37% (IC50 34.4μg/ml). The superoxide scavenging activity of the extract was found to be 81.5±0.41%. Interestingly, upon TLC fingerprinting, only one band with Rf 0.70 showed multifunctional activity. The phytochemical found to be present was an alkaloid. The results evidenced the presence of multifunctional smart molecule in methanolic extract of P. emblica L and showed an alkaloid as the component responsible for anti-diabesity potential.


2019 ◽  
Vol 15 (1) ◽  
pp. 41-45
Author(s):  
Shivabai Chandwad ◽  
Sudhakar Gutte

Background:Diabetes mellitus is the most common and fastest growing disease in the world. One of the therapies to treat diabetes is the inhibition of α-amylase activity by inhibitors from microbial and plant source. Actinomycetes are potential sources of enzyme inhibitors, drugs, amino acids, vitamins etc.Objective:Our work mainly highlights the isolation of actinomycetes from soil samples of different habitats and screening of α -amylase inhibitors.Methods:Actinomycetes were isolated from soil samples of different habitats by different methods; these include a variety of pre-treatment of soil samples in combination with an appropriate supplement medium with selective antibacterial agents. Isolated actinomycetes grown in fermentation condition and metabolites were extracted with Isopropyl alcohol and concentrated to obtain solid material. The extract of each isolate was tested for α -amylase inhibition using starch Iodine plate method and DNS- spectroscopic method.Results:Total 110 actinomycetes strains were isolated from various sources. Among 110 extracts of actinomycetes, eight extracts have shown positive results for α-amylase inhibition in starch Iodine plate assay method. Extracts selected from primary results were used for the confirmation of inhibitory activity using DNS- spectroscopic method. Out of eight extracts, six extracts showed Porcine pancreatic α -amylase inhibitory activity ranging from 40-86%. The actinomycetes strains that produce α -amylase inhibitory activity are A-24, A-29, B-5, B-18, C-15 and D-24.Conclusion:These results show that actinomycetes are a potential source for α -amylase inhibitors, which may lead to valuable novel drugs for diabetic treatment.


2015 ◽  
Vol 49 ◽  
pp. 18-24 ◽  
Author(s):  
David Houghton ◽  
Matthew D. Wilcox ◽  
Peter I. Chater ◽  
Iain A. Brownlee ◽  
Chris J. Seal ◽  
...  

Author(s):  
Matheus Gabriel de Oliveira ◽  
Waléria Ramos Nogueira de Souza ◽  
Ricardo Pereira Rodrigues ◽  
Daniel F. Kawano ◽  
Leonardo Luiz Borges ◽  
...  

2020 ◽  
Vol 15 (3) ◽  
pp. 818-828
Author(s):  
Miradatul Najwa Muhd Rodhi ◽  
Fazlena Hamzah ◽  
Ku Halim Ku Hamid

Gallic acid and quercetin equivalent were determined in the crude extract of matured leaves Aquilaria malaccensis and Aquilaria subintegra. The leaves of both Aquilaria species were dried at 60 °C for 24 hours, ground and sieved into particle size of 250, 300, 400, 500, and 1000 µm. Then, each particle size of leaves was soaked in distilled water with a ratio of 1:100 (w/v) for 24 hours and undergoes the pre-treatment method by using ultrasonicator (37 kHz), at the temperature of 60 °C for 30 minutes. The crude extracts were obtained after about 4 hours of hydrodistillation process. The highest concentration of gallic acid and quercetin equivalent was determined in the crude extract from the particle size of 250 µm. The kinetics of pancreatic lipase inhibition was further studied based using the Lineweaver-Burk plot, wherein the concentration of p-NPP as the substrate and pancreatic lipase were varied. Based on the formation of the lines in the plot, the crude leaves extract of both Aquilaria species exhibit the mixed-inhibition on pancreatic lipase, which indicates that in the reaction, the inhibitors were not only attached to the free pancreatic lipase, but also to the pancreatic lipase-(p-NPP) complex. The reaction mechanism was similar to non-competitive inhibition; however the value of dissociation constant, Ki, for both inhibition pathways was different. The inhibition shows an increment in Michaelis-Menten constant (Km) and a reduction in the maximum pancreatic lipase activity (Vm) compared to the reaction without Aquilaria spp. crude extracts (control). This proved that the inhibition occurred in this reaction. Copyright © 2020 BCREC Group. All rights reserved 


2021 ◽  
Vol 29 (1) ◽  
pp. 76-86
Author(s):  
Wendi Nurul Fadillah ◽  
Nampiah Sukarno ◽  
Dyah Iswantini ◽  
Min Rahminiwati ◽  
Novriyandi Hanif ◽  
...  

This study aimed to evaluate the potential of marine fungus Purpureocillium lilacinum isolated from an Indonesian marine sponge Stylissa sp. as an anti-obesity agent through pancreatic lipase inhibition assay. The fungus was identified as P. lilacinum through morphological and molecular characteristics. The fungal extract’s inhibition activity and kinetics were evaluated using spectrophotometry and Lineweaver-Burk plots. Ethyl acetate and butanol were used for extraction. Both extracts showed pancreatic lipase inhibition in a concentration-dependent manner. Both crude extracts were then fractionated once. All fractionated extracts showed inhibitory activity above 50%, with the highest activity found in fraction 5 of ethyl acetate at 93.41% inhibition. The best fractionated extract had an IC50value of 220.60 µg.mL-1. The most active fraction of P. lilacinum had a competitive-type inhibitor behavior as shown by the value of Vmax not significantly changing from 388.80 to 382.62 mM pNP.min-1, and the Michaelis-Menten constant (KM) increased from 2.02 to 5.47 mM in the presence of 500 µg.mL-1 fractionated extract. Metabolite identification with LC-MS/MS QTOF suggested that galangin, kaempferol, and quercetin were responsible for the observed lipase inhibition.


2018 ◽  
Vol 48 ◽  
pp. 1-8 ◽  
Author(s):  
Tzu-Yin Chen ◽  
Miki M.C. Wang ◽  
Sheng-Kuo Hsieh ◽  
Meng-Huang Hsieh ◽  
Wen-Ying Chen ◽  
...  

2019 ◽  
pp. 149-191
Author(s):  
S. N. C. Sridhar ◽  
Ginson George ◽  
Aanchal Verma ◽  
Atish Tulshiram Paul

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