scholarly journals In vitro lipase enzyme inhibitory activities of green tea and other herbs

2020 ◽  
Vol 9 (1) ◽  
pp. 48-52
Author(s):  
Megawati Megawati ◽  
Nina Artanti ◽  
Hani Mulyani ◽  
Akhmad Darmawan ◽  
Heri Syahrian ◽  
...  

Background: Increased lipase activity can increase the amount of monoglycerides and fatty acids absorbed by the body, this is what affects obesity. If pancreatic lipase activity is inhibited, the production of fatty acids will decrease, consequently the level of fat in the blood will also decrease.Objective: To study anti obesity potential of a single herb or a mixture of green tea and other herbs (Syzygium polyanthum. Lv, Artocarpus communis.Lv, Cinnamomum verum..Lv, Manilkara zapota.Lv, Tectona grandis.Lv) by the in vitro inhibition assay of the lipase enzyme activityMethod: A single (8 herbs) or a mixture of three herbs powder (12 formulas) was put into a tea bag with a total weight of 1.5 g to be brewed in 100 mL bottled mineral water at 70⁰-90⁰C for 10 minutes. In vitro lipase enzyme inhibition assay were conducted to measure the ability of these samples as lipase inhibitor. Orlistat used as positive lipase inhibitor. Results: There was a difference results of lipase inhibition activity between the sample of a single and a mixture of herbs. Interestingly, the results shows that formula 3 (mixture of green tea, Manilkara zapota and cinnamon). has 53.942 % inhibition, formula 9 (a mixture of green tea, Syzygium polyanthum and cinnamon) has 67.322 % inhibition and formula 12 (a mixture of green tea, Tectona grandis and cinnamon) has 56.612 % inhibition which close to lipase inhibitory activity by standard Orlistat.Conclusion: The mixture of green tea and two other herbs has a lipase inhibitory activity similar to Orlistat, when compared to the single herb. The highest lipase inhibitory activity is found in formula 9.

Molecules ◽  
2021 ◽  
Vol 26 (9) ◽  
pp. 2433
Author(s):  
Nesren Elsayed ◽  
Hatem Sharaf El-Din ◽  
Ammar B. Altemimi ◽  
Hanaa Y. Ahmed ◽  
Anubhav Pratap-Singh ◽  
...  

In this study, Egyptian beebread (EBB) was investigated for its nutritive value, chemical composition, antioxidant properties, antimicrobial and antitumor activities. Results indicated that EBB was a good source of protein (23.58 ± 0.183 g/100 g BB), total free sugar (20.266 ± 0.930) and potassium (290.202 ± 2.645 mg/100 g). Additionally, 14 fatty acids were identified in EBB, wherein polyunsaturated and monounsaturated fatty acids represented 51.06% ± 0.09% and 9.86% ± 0.01%, respectively. The EBB extract exhibited almost 400% better antiradical activity than BHT, with IC50 of EBB extract being 10.7 µg/mL compared to 39.5 µg/mL for BHT. EBB exhibited higher inhibitory activity than the reference compound against Staphylococcus aureus and Escherichia coli, followed by Bacillus subtilis. No inhibitory activity was observed against Aspergillus Niger. Additionally, the highest inhibitory activity was recorded against Caco-2 cells, followed by PC3 and HepG-2 cancer cell lines with IC50 values 262, 314 and 386 μg/mL, respectively. These findings establish the potential of EBB as an antioxidant, antimicrobial and antitumor agent, with possible applications as natural food supplements and natural preservatives.


Nutrients ◽  
2020 ◽  
Vol 12 (6) ◽  
pp. 1601 ◽  
Author(s):  
Hiroki Saito ◽  
Yu Toyoda ◽  
Tappei Takada ◽  
Hiroshi Hirata ◽  
Ami Ota-Kontani ◽  
...  

The beneficial effects of fatty acids (FAs) on human health have attracted widespread interest. However, little is known about the impact of FAs on the handling of urate, the end-product of human purine metabolism, in the body. Increased serum urate levels occur in hyperuricemia, a disease that can lead to gout. In humans, urate filtered by the glomerulus of the kidney is majorly re-absorbed from primary urine into the blood via the urate transporter 1 (URAT1)-mediated pathway. URAT1 inhibition, thus, contributes to decreasing serum urate concentration by increasing net renal urate excretion. Here, we investigated the URAT1-inhibitory effects of 25 FAs that are commonly contained in foods or produced in the body. For this purpose, we conducted an in vitro transport assay using cells transiently expressing URAT1. Our results showed that unsaturated FAs, especially long-chain unsaturated FAs, inhibited URAT1 more strongly than saturated FAs. Among the tested unsaturated FAs, eicosapentaenoic acid, α-linolenic acid, and docosahexaenoic acid exhibited substantial URAT1-inhibitory activities, with half maximal inhibitory concentration values of 6.0, 14.2, and 15.2 μM, respectively. Although further studies are required to investigate whether the ω-3 polyunsaturated FAs can be employed as uricosuric agents, our findings further confirm FAs as nutritionally important substances influencing human health.


1961 ◽  
Vol 201 (5) ◽  
pp. 915-922 ◽  
Author(s):  
B. Shore ◽  
V. Shore

The enzymes released into both human and rabbit plasmas by heparin injection hydrolyzed, in addition to triglyceride moieties of lipoproteins, a number of mono- and diglycerides of C16 and C18 fatty acids after in vitro addition of the unemulsified glycerides to the plasma. In human postheparin plasma, these enzymes also hydrolyzed glycerides of butyric and caproic acids. The pure triglycerides and methyl or ethyl esters of C16 and C18 fatty acids were not substrates. The heparin-released activities for the hydrolysis of glycerides added in vitro persisted after all activity for the lipolysis of lipoproteins had been destroyed by heat. These activities also differed from lipoprotein lipase activity with respect to the effects of 1 m NaCl, dialysis, and aging the plasma at 4 C. It appears that heparin releases into the blood more than one enzyme or more than one form of an enzyme which may be involved in a stepwise degradation to fatty acids and glycerol of the triglyceride moieties of lipoproteins of density less than 1.007 g/ml.


Molecules ◽  
2020 ◽  
Vol 25 (10) ◽  
pp. 2340 ◽  
Author(s):  
Agnieszka Szkudlarek ◽  
Michał Wilk ◽  
Małgorzata Maciążek-Jurczyk

The interaction of drugs with human serum albumin (HSA) is an important element of therapy. Albumin affects the distribution of the drug substance in the body, as well as its pharmacokinetic and pharmacodynamic properties. On the one hand, inflammation and protein glycation, directly associated with many pathological conditions and old age, can cause structural and functional modification of HSA, causing binding disorders. On the other hand, the widespread availability of various dietary supplements that affect the content of fatty acids in the body means that knowledge of the binding activity of transporting proteins, especially in people with chronic diseases, e.g., diabetes, will achieve satisfactory results of the selected therapy. Therefore, the aim of the present study was to evaluate the effect of a mixture of fatty acids (FA) with different saturated and unsaturated acids on the affinity of acetohexamide (AH), a drug with hypoglycaemic activity for glycated albumin, simulating the state of diabetes in the body. Based on fluorescence studies, we can conclude that the presence of both saturated and unsaturated FA disturbs the binding of AH to glycated albumin. Acetohexamide binds more strongly to defatted albumin than to albumin in the presence of fatty acids. The competitive binding of AH and FA to albumin may influence the concentration of free drug fraction and thus its therapeutic effect.


Foods ◽  
2020 ◽  
Vol 9 (7) ◽  
pp. 844
Author(s):  
Razia Sultana ◽  
Adeola M. Alashi ◽  
Khaleda Islam ◽  
Md Saifullah ◽  
C. Emdad Haque ◽  
...  

The aim of the study was to determine the in vitro enzyme inhibition activities of aqueous polyphenolic extracts of nine popular Bangladeshi vegetables, namely ash gourd, bitter gourd, brinjal, Indian spinach, kangkong, okra, ridge gourd, snake gourd, and stem amaranth. Polyphenolic glycosides were the major compounds present in the extracts. Inhibition of α-amylase (up to 100% at 1 mg/mL) was stronger than α-glucosidase inhibition (up to 70.78% at 10 mg/mL). The Indian spinach extract was the strongest inhibitor of pancreatic lipase activity (IC50 = 276.77 µg/mL), which was significantly better than that of orlistat (381.16 µg/mL), a drug. Ash gourd (76.51%), brinjal (72.48%), and snake gourd (66.82%) extracts were the most effective inhibitors of angiotensin-converting enzyme (ACE), an enzyme whose excessive activities have been associated with hypertension. Brinjal also had a significantly higher renin-inhibitory activity than the other vegetable extracts. We conclude that the vegetable extracts may have the ability to reduce enzyme activities that have been associated with hyperglycemia, hyperlipidemia, and hypertension.


2020 ◽  
Vol 2020 ◽  
pp. 1-7 ◽  
Author(s):  
Minsu Jang ◽  
Yea-In Park ◽  
Yeo-Eun Cha ◽  
Rackhyun Park ◽  
Sim Namkoong ◽  
...  

COVID-19, a global pandemic, has caused over 750,000 deaths worldwide as of August 2020. A vaccine or remedy for SARS-CoV-2, the virus responsible for COVID-19, is necessary to slow down the spread and lethality of COVID-19. However, there is currently no effective treatment available against SARS-CoV-2. In this report, we demonstrated that EGCG and theaflavin, the main active ingredients of green tea and black tea, respectively, are potentially effective to inhibit SARS-CoV-2 activity. Coronaviruses require the 3CL-protease for the cleavage of its polyprotein to make individual proteins functional. EGCG and theaflavin showed inhibitory activity against the SARS-CoV-2 3CL-protease in a dose-dependent manner, and the half inhibitory concentration (IC50) was 7.58 μg/ml for EGCG and 8.44 μg/ml for theaflavin. In addition, we did not observe any cytotoxicity for either EGCG or theaflavin at the concentrations tested up to 40 μg/ml in HEK293T cells. These results suggest that upon further study, EGCG and theaflavin can be potentially useful to treat COVID-19.


1986 ◽  
Vol 239 (1) ◽  
pp. 121-125 ◽  
Author(s):  
P Newsholme ◽  
R Curi ◽  
S Gordon ◽  
E A Newsholme

Maximum activities of some key enzymes of metabolism were studied in elicited (inflammatory) macrophages of the mouse and lymph-node lymphocytes of the rat. The activity of hexokinase in the macrophage is very high, as high as that in any other major tissue of the body, and higher than that of phosphorylase or 6-phosphofructokinase, suggesting that glucose is a more important fuel than glycogen and that the pentose phosphate pathway is also important in these cells. The latter suggestion is supported by the high activities of both glucose-6-phosphate dehydrogenase and 6-phosphogluconate dehydrogenase. However, the rate of glucose utilization by ‘resting’ macrophages incubated in vitro is less than the 10% of the activity of 6-phosphofructokinase: this suggests that the rate of glycolysis is increased dramatically during phagocytosis or increased secretory activity. The macrophages possess higher activities of citrate synthase and oxoglutarate dehydrogenase than do lymphocytes, suggesting that the tricarboxylic acid cycle may be important in energy generation in these cells. The activity of 3-oxoacid CoA-transferase is higher in the macrophage, but that of 3-hydroxybutyrate dehydrogenase is very much lower than those in the lymphocytes. The activity of carnitine palmitoyltransferase is higher in macrophages, suggesting that fatty acids as well as acetoacetate could provide acetyl-CoA as substrate for the tricarboxylic acid cycle. No detectable rate of acetoacetate or 3-hydroxybutyrate utilization was observed during incubation of resting macrophages, but that of oleate was 1.0 nmol/h per mg of protein or about 2.2% of the activity of palmitoyltransferase. The activity of glutaminase is about 4-fold higher in macrophages than in lymphocytes, which suggests that the rate of glutamine utilization could be very high. The rate of utilization of glutamine by resting incubated macrophages was similar to that reported for rat lymphocytes, but was considerably lower than the activity of glutaminase.


2021 ◽  
Vol 9 (04) ◽  
pp. 21-25
Author(s):  
Syed Ahad Hussain ◽  
◽  
Goutham Kumar Srigadi ◽  
Chamakuri Subba Rao ◽  
Syed Ahmedulla Hussaini ◽  
...  

Aim:The aim of this study was undertaken to assessin vitro H+-K+ ATPase inhibitory activity of different extracts of Cissus quadrangularis Linn. Materials and Methods: Phytochemical and Phyto-analytical studies like total phenolic compound and total flavonoid contents from extract were quantified and H+-K+ ATPase inhibition assay was performed in presence of different concentrations(10,20,50 and 100 μg/ml) of standard (omeprazole),chloroform and methanolic extract. Results:The extract has shown dose dependent significant (*P < 0.05) proton pump inhibitory activity in the goat gastric mucosal homogenate which was compared to standard Omeprazole. Conclusions: Hence, from this study we have concluded that methanolic extract of C.quadrangularis has more inhibitory effect than chloroform extract.


Author(s):  
Dang Kim Thu ◽  
Vu Thi Hoa ◽  
Chu Ngoc Khanh ◽  
Bui Thanh Tung

Xanthine oxidase (XO) is an enzyme that has an improtant role in the synthesis of uric acid. XO is an enzyme allowscatalyzing the hydroxylation of hypoxanthine to xanthine and xanthine to uric acid. These are two reactions in the final stage of metabolism of the purines in the body. Offal, XO enzyme inhibitors reduce biosynthesis of uric acid have been used to prevent and treat gout. In this study, Gompherena celosiodes is extracted by ultrasonic with ethanol 80 % (EtOH)solvents and fractionated with n-hexane, ethyl acetate (EtOAc) and n-butanol (n-BuOH) solvents. These fractions were evaluated xanthine oxidase inhibitory activities in vitro. The results show that n-BuOH fraction from roots bark had the strongest XO enzyme inhibitory activity (IC50: 27,39 ± 0,31µg/mL), followed by EtOH fraction (IC50: 47,37 ± 0,26 µg/mL) and EtOAc fraction (IC50: 33,36 ± 0,51µg/mL) and the lowest is n-hexan fraction (IC50: 81,59 ± 0,21µg/mL). The research results indicated that the n-BuOH fraction and the EtOAc fraction from tree-hatched soil have a potential in the prevention and treatment of gout.


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