ANTI-DIABESITY PRINCIPLE FROM THE SEEDS OF PHYLLANTHUS EMBLICA L.

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.

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.


INDIAN DRUGS ◽  
2018 ◽  
Vol 55 (12) ◽  
pp. 60-68
Author(s):  
R. R Shahu ◽  
◽  
P. Rathod ◽  
C Kulkarni ◽  
S. Mhatre ◽  
...  

Pancreatic lipase inhibitory effect of methanolic extract of florets Aster sp. was studied. In case of Aster sp. (White florets) the pancreatic lipase inhibition recorded was 82.75% with an IC50 value of 38μg/mL. Aster sp. (light pink) showed 80.04 % inhibition with an IC50 of 72 μg/mL. On 2 h dialysis, both the extracts lost their significant pancreatic lipase inhibitory activity, indicating the reversible nature of inhibition. pH slightly affected the performance of pancreatic lipase inhibitory activity. Extract (white florets) also showed 22.03% superoxide radical scavenging activity and 22.73% free radical scavenging activity indicating the multifunctional nature of the extract. Light pink florets showed 40.67% superoxide radical scavenging activity and 24.10% free radical scavenging activity. Saponin and alkaloid molecule in white florets of Aster sp. and alkaloid in light pink florets were identified as active principles for pancreatic lipase inhibitory activity.


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.


2021 ◽  
Vol 51 (11) ◽  
Author(s):  
Elisa dos Santos Pereira ◽  
Juliana Rocha Vinholes ◽  
Taiane Mota Camargo ◽  
Chirle de Oliveira Raphaelli ◽  
Núbia Marilin Lettnin Ferri ◽  
...  

ABSTRACT: “Araçá” has been reported with different biological activities such as antioxidant, antiproliferative and antimicrobial as well as inhibitors of digestive enzymes. The digestive pancreatic lipase enzyme plays a fundamental role in lipid metabolism, and its inhibition has been studied as a target for obesity treatment. This study quantified the bioactive compounds present in different parts of “araçá” fruit and evaluated their antioxidant activity and lipase inhibition properties. Three samples were analyzed for total anthocyanins, total phenolic content, antioxidant activity and pancreatic lipase inhibition. Anthocyanins were reported only in pulp-peel of red “araçá” sample. Phenolic compounds concentration was higher in pulp-peel than in seeds for all samples. The antioxidant activity followed the same trend. A positive correlation was observed between total phenolic content and both antioxidant activity and lipase inhibition. Lipase inhibition activity was higher for pulp-peel compared to the seeds. Overall, the results showed that “araçá” fruit extracts could be beneficial for the treatment of obesity.


2018 ◽  
Vol 2018 ◽  
pp. 1-21 ◽  
Author(s):  
Rana M. Jamous ◽  
Salam Y. Abu-Zaitoun ◽  
Rola J. Akkawi ◽  
Mohammed S. Ali-Shtayeh

We evaluated the antioxidant and porcine pancreatic lipase inhibition (PPLI) activities of 90 plants extracts. The antioxidant activity was measured using the free-radical scavenging capacity (DPPH) and reducing power (RP) assays. The pancreatic lipase inhibition assay was used to determine the PPLI activity of plant extracts. Among the 90 plant extracts examined, 41.0 % crude extracts showed antilipase activity of more than 50%. The most active plants by means of IC50 value were Camellia sinensis (0.5 mg/ml), Ceratonia siliqua (leaves) (0.8 mg/mL), Curcuma longa (0.8 mg/mL), Sarcopoterium spinosum (1.2 mg/mL), and Mentha spicata (1.2 mg/mL). The antioxidant activity of plant extracts using the DPPH and RP assays reveals comparable results. The most active antioxidant extracts using both assays were the leaves and fruit epicarp of Rhus coriaria, areal parts of Sarcopoterium spinosum, and leaves of Ceratonia siliqua. Our results suggest natural resources that possess strong antioxidant and pancreatic lipase inhibitory activities with potential applications in the treatment and prevention of obesity and overweight. The extracts of Camellia sinensis, Ceratonia siliqua, Curcuma longa, Sarcopoterium spinosum, and Mentha spicata were proved to have a great potential as antioxidants and antiobesity agents.


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 


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