Studies of the inhibition of lipolytic enzymes: I. the inhibition of a canine kidney and liver lipase in vitro and in vivo BY n-butyl carbamic acid methyl ester (U-14641)

1963 ◽  
Vol 12 (10) ◽  
pp. 1117-1130 ◽  
Author(s):  
Donald P. Wallach ◽  
Howard Ko
Author(s):  
Samuel Estrada-Soto ◽  
Litzia Cerón-Romero ◽  
Gabriel Navarrete-Vázquez ◽  
Edgar Rosales-Ortega ◽  
Jaime H. Gómez-Zamudio ◽  
...  

The current study aimed to determine the antidiabetic and antidyslipidemic activities of moronic acid methyl ester (1) by in vivo, in vitro, in silico and molecular biology studies. Compound 1 was evaluated to establish its dose-dependent antidiabetic and antihyperglycemic (50 mg/kg) activities, in diabetic and normoglycemic male CD1 mice, respectively. Also, compound 1 was subjected to a sub-acute study (50 mg/kg/day for eight days) to determine blood biochemical profiles and the expression of PTP-1B, GLUT4, PPAR-α, PPAR-γ, adiponectin, IL-1β, and MCP1 in adipose tissue of animals after treatment. Different doses in acute administration of 1 decreased glycemia (p < 0.05), compared with vehicle, showing greater effectiveness in the range 50-160 mg/kg. Also, the oral glucose tolerance test (OGTT) showed that 1 induced a significant antihyperglycemic action by opposing the hyperglycemic peak (p < 0.05). Moreover, 1 subacute administration decrease glucose and triglycerides levels after treatment (p < 0.05); while the expression of PPAR-α and γ, adiponectin and GLUT4 displayed an increase (p< 0.05) compared with the diabetic control group. In conclusion, compound 1 showed antihyperglycemic, antidiabetic and antidyslipidemic effects in normal and diabetic mice, probably due to insulin sensitization through increase mRNA expression of GLUT4, PPAR-α, PPAR-γ and adiponectin genes.


2018 ◽  
Vol 9 (12) ◽  
pp. 6155-6164 ◽  
Author(s):  
Lang Zhang ◽  
Ya Fan ◽  
Hanwen Su ◽  
Li Wu ◽  
Yuying Huang ◽  
...  

In vivoandin vitrostudies show that chlorogenic acid methyl ester (CME) has been proven to be a potential nutraceutical for preventing inflammation.


Antioxidants ◽  
2020 ◽  
Vol 9 (4) ◽  
pp. 282 ◽  
Author(s):  
Kishor Mazumder ◽  
Afia Nabila ◽  
Asma Aktar ◽  
Asgar Farahnaky

The aim of this present investigation was to analyze bioactive compounds, as well as demonstrate the antioxidant activities of nine cultivars of Australian lupin species accompanied by observing the effect of domestic heat processing on their antioxidant activities adopting in vivo and in vitro approaches. Gas chromatography mass spectroscopy (GC-MS) analysis was performed for profiling bioactive compounds present in lupin cultivars. Multiple assay techniques involving quantification of polyphenolics, flavonoids and flavonol, electron transfer (ET) based assay, hydrogen atom transfer (HAT)-based assay and in vivo assays were performed. The major compounds found were hexadecanoic acid methyl ester, 9,12-octadecadienoic acid methyl ester, methyl stearate, lupanine,13-docosenamide and 11-octadecenoic acid (Z)- methyl ester. Mandelup was found to show excellent antioxidant activity. Moreover, Jurien, Gunyidi and Barlock had strong antioxidant activity. Both positive and negative impacts of heat processing were observed on antioxidant activity. Heating and usage of excess water during processing were the key determinants of loss of antioxidants. Negligible loss of antioxidant activity was observed in most of the assays whereas inhibition of both lipid peroxidation (33.53%) and hemolysis of erythrocytes (37.75%) were increased after processing. In addition, in vitro and in vivo antioxidant assays are found to show statistically significant (* p < 0.05 and ** p < 0.01) results, which are supported by the presence of a number of antioxidant compounds in GC-MS analysis.


2014 ◽  
Vol 2 (5) ◽  
pp. 659-663
Author(s):  
MIN-A KIM ◽  
HYEONG-U SON ◽  
CHEOL-SIK YOON ◽  
SUNG-HEE NAM ◽  
YOUNG-CHEOL CHOI ◽  
...  

2007 ◽  
Vol 4 (2) ◽  
pp. 166-172 ◽  
Author(s):  
Kavita Rathore ◽  
Usha Ameta ◽  
Swati Ojha ◽  
Ranjana Sharma ◽  
G. L. Talesara

Mebendazole is a well known anti-helimintic and belongs to the benzimidazole group of medicines. In order to achieve better medicinal results, i.e. enhanced activity and low toxicity, structural modifications are made in the existing drugs. Some 5-benzoyl-N-[1-(alkoxyphthalimido) benzimidazol-2-yl] carbamic acid methyl ester(3a-c)and 5-benzoyl-N-[1-(2,3-bis oxyphthalimido∕oxysuccinimido propyl benzimidazol-2-yl) carbamic acid methyl ester(7a-b)have been synthesized from two different routes. Structures of the compounds have been established on the basis of elemental analysis and spectral studies. All the synthesized compounds(3a-c)and(7a-b)were assayedin vitrofor antimicrobial activity against mebendazole (itself) and standard [ciprofloxacin (antibacterial) and fluconazole (antifungal)].


Phytomedicine ◽  
2018 ◽  
Vol 48 ◽  
pp. 10-20 ◽  
Author(s):  
He-Zhong Zhang ◽  
Chong-Yong Li ◽  
Jia-Qi Wu ◽  
Rui-Xue Wang ◽  
Ping Wei ◽  
...  

Molecules ◽  
2019 ◽  
Vol 24 (22) ◽  
pp. 4191 ◽  
Author(s):  
Fang-Yao Li ◽  
Lin Huang ◽  
Qian Li ◽  
Xiu Wang ◽  
Xian-Li Ma ◽  
...  

To discover novel potent cytotoxic diterpenoids, a series of hybrids of dehydroabietic acid containing 1,2,3-triazole moiety were designed and synthesized. The target compounds were characterized by means of FT-IR, 1H NMR, 13C NMR, ESI-MS and elemental analysis techniques. The in vitro cytotoxicity of these compounds was evaluated by standard MTT (methyl thiazolytetrazolium) assay against CNE-2 (nasopharynx), HepG2 (liver), HeLa (epithelial cervical), BEL-7402 (liver) human carcinoma cell lines and human normal liver cell (HL-7702). The screening results revealed that most of the hybrids showed significantly improved cytotoxicity over parent compound DHAA. Among them, [1-(3-fluorobenzyl)-1H-1,2,3-triazole-4-yl]dehydroabietic acid methyl ester (3c), and [1-(2-nitrobenzyl)-1H-1,2,3-triazole-4-yl]dehydroabietic acid methyl ester (3k) displayed better antiproliferative activity with IC50 (50% inhibitory concentration) values of 5.90 ± 0.41 and 6.25 ± 0.37 µM toward HepG2 cells compared to cisplatin, while they exhibited lower cytotoxicity against HL-7702. Therefore, the 1,2,3-triazole-hybrids could be a promising strategy for the synthesis of antitumor diterpenoids and it also proved the essential role of 1,2,3-triazole moiety of DHAA in the biological activity.


2019 ◽  
Vol 2019 (18) ◽  
pp. 2928-2932 ◽  
Author(s):  
Mengting Liu ◽  
Yan He ◽  
Ling Shen ◽  
Weaam Hasan Al Anbari ◽  
Huaqiang Li ◽  
...  

2005 ◽  
Vol 60 (9-10) ◽  
pp. 711-716 ◽  
Author(s):  
Julieta Rubio ◽  
José S. Calderón ◽  
Angélica Flores ◽  
Clementina Castro ◽  
Carlos L. Céspedes

Abstract Fractionation with n-hexane/ethyl acetate (1:1 v/v) by open column chromatography of the oleoresin from Pinus oocarpa Schiede yielded two diterpenes, pimaric acid (1) and dehydroabietic acid (5), the sesquiterpene longifolene (3) and a diterpenic mixture containing pimaric acid (1), isopimaric acid (4) and dehydroabietic acid (5). Subsequently, the isolated compounds, the mixture of 1, 4 and 5, the oleoresin and the dehydroabietic acid methyl ester (2), were tested in vitro against epimastigotes of Trypanosoma cruzi, the causative agent of Chagas disease. The most active compounds were 1, 3 and the oleoresin, being as active as nifurtimox, a drug effective in the treatment of acute infection by American trypanosomiasis and used in this work as positive control.


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