scholarly journals In vivo hypotensive effect and in vitro inhibitory activity of some Cyperaceae species

2013 ◽  
Vol 49 (4) ◽  
pp. 803-809
Author(s):  
Monica Lacerda Lopes Martins ◽  
Henrique Poltronieri Pacheco ◽  
Iara Giuberti Perini ◽  
Dominik Lenz ◽  
Tadeu Uggere de Andrade ◽  
...  

In 1820, French naturalist August Saint Hillaire, during a visit in Espírito Santo (ES), a state in southeastern Brazil, reported a popular use of Cyperaceae species as antidote to snake bites. The plant may even have a hypotensive effect, though it was never properly researched. The in vitro inhibitory of the angiotensin converting enzyme (ACE) activity of eigth ethanolic extracts of Cyperaceae was evaluated by colorimetric assay. Total phenolic and flavonoids were determined using colorimetric assay. The hypotensive effect of the active specie (Rhychonospora exaltata, ERE) and the in vivo ACE assay was measured in vivo using male Wistar Kyoto (ERE, 0.01-100mg/kg), with acetylcholine (ACh) as positive control (5 µg/kg, i.v.). The evaluation of ACE in vivo inhibitory effect was performed comparing the mean arterial pressure before and after ERE (10 mg/kg) in animals which received injection of angiotensin I (ANG I; 0,03, 03 and 300 µg/kg, i.v.). Captopril (30 mg/kg) was used as positive control. Bulbostylis capillaris (86.89 ± 15.20%) and ERE (74.89 ± 11.95%, ERE) were considered active in the in vitro ACE inhibition assay, at 100 µg/mL concentration. ACh lead to a hypotensive effect before and after ERE's curve (-40±5% and -41±3%). ERE showed a dose-dependent hypotensive effect and a in vivo ACE inhibitory effect. Cyperaceae species showed an inhibitory activity of ACE, in vitro, as well as high content of total phenolic and flavonoids. ERE exhibited an inhibitory effect on both in vitro and in vivo ACE. The selection of species used in popular medicine as antidotes, along with the in vitro assay of ACE inhibition, might be a biomonitoring method for the screening of new medicinal plants with hypotensive properties.

Author(s):  
Pınar Ercan ◽  
Sedef Nehir El

Abstract. The goals of this study were to determine and evaluate the bioaccessibility of total anthocyanin and procyanidin in apple (Amasya, Malus communis), red grape (Papazkarası, Vitis vinifera) and cinnamon (Cassia, Cinnamomum) using an in vitro static digestion system based on human gastrointestinal physiologically relevant conditions. Also, in vitro inhibitory effects of these foods on lipid (lipase) and carbohydrate digestive enzymes (α-amylase and α-glucosidase) were performed with before and after digested samples using acarbose and methylumbelliferyl oleate (4MUO) as the positive control. While the highest total anthocyanin content was found in red grape (164 ± 2.51 mg/100 g), the highest procyanidin content was found in cinnamon (6432 ± 177.31 mg/100 g) (p < 0.05). The anthocyanin bioaccessibilities were found as 10.2 ± 1%, 8.23 ± 0.64%, and 8.73 ± 0.70% in apple, red grape, and cinnamon, respectively. The procyanidin bioaccessibilities of apple, red grape, and cinnamon were found as 17.57 ± 0.71%, 14.08 ± 0.74% and 18.75 ± 1.49%, respectively. The analyzed apple, red grape and cinnamon showed the inhibitory activity against α-glucosidase (IC50 544 ± 21.94, 445 ± 15.67, 1592 ± 17.58 μg/mL, respectively), α-amylase (IC50 38.4 ± 7.26, 56.1 ± 3.60, 3.54 ± 0.86 μg/mL, respectively), and lipase (IC50 52.7 ± 2.05, 581 ± 54.14, 49.6 ± 2.72 μg/mL), respectively. According to our results apple, red grape and cinnamon have potential to inhibit of lipase, α-amylase and α-glucosidase digestive enzymes.


Author(s):  
Sri Ningsih ◽  
Fahri Fahrudin

 Objective: Hyperuricemia (high uric acid levels) prevalence increased year by year. This study was aimed to elaborate the in vitro xanthine oxidase (XO) inhibitory activity and in vivo lowering hyperuricemic effect of Uncaria gambir (Hunter) Roxb) (gambir), Caesalpinia sappan L. (secang) and the combined extract of secang and gambir (formulae extract [FE]).Methods: Gambir and secang extracts were prepared by maceration with ethanol and FE was the proportioned combination of these two extracts. XO inhibitory activity was determined by measuring the formation of uric acid in the xanthine/XO system in vitro using allopurinol as a positive control at 100 ug/mL. Antioxidant activity was by 1,1-diphenyl-2-picrylhydrazyl radical reducing methods. The in vivo experiments were conducted in the oxonate-induced hyperuricemia rat model, in which FE was gavaged p.o. at the arrange dose of 75, 150, and 300 mg/kg bw for 2 weeks. Polyphenol content was measured using Folin–Ciocalteu reagent spectrophotometrically.Results: The XO inhibitory activity of FE was 80% of allopurinol, while secang and gambir were 98% and 50%, respectively. The strength was appropriate to the total polyphenol content, in which it decreased in the order of secang (99%) > FE (86%) > gambir (46%). Furthermore, FE at all tested doses was able to decrease uric acid levels. FE also demonstrated antioxidant activity with a value of 74% relative to Vitamin C at 4 ug/mL.Conclusion: These studies could be concluded that FE exhibited the ability to decrease uric acid level so that it was potential to be developed further as a uric acid-lowering agent.


2019 ◽  
Vol 31 (12) ◽  
pp. 2964-2968 ◽  
Author(s):  
Nutthamon Prajudtasri ◽  
Mongkol Nontakitticharoen ◽  
Sujint Anguravirutt

The aim of this study was to perform a phytochemical analysis of Melastoma saigonense seed extracts and to determine their α-glucosidase inhibitory activity. The extracts from seeds of M. saigonense indicated that the total phenolic content was in the range between 233.46 and 967.22 mg GAE/g DE, whereas the flavonoids content was in the range between 359.96 and 850.84 mg QE/g DE. The present study of antidiabetic inhibitory activity by in vitro α-glucosidase revealed that the crude extracts using ethyl acetate (EA), butanol (BU) and final aqueous residue extracts (AQ) exhibited a strong α-glucosidase inhibitory effect (IC50 4.42-11.95 μg/mL). The ethyl acetate and butanol extracts of seeds of Melastoma saigonense (Kuntze) Merr. were further fractionated by silica gel column chromatography into four fractions (EAF1−EAF4) and five fractions (BUF1−BUF5), respectively and their bioactivities were investigated. The nine fractions exhibited significant α-glucosidase inhibitory activity (p < 0.05) with an IC50 between 3.42-34.77 μg/mL which is less than the IC50 for standard acarbose (IC50 = 507.26 μg/mL). Among all the fractions, BUF1 and EAF1 exhibited high inhibitory activity against α-glucosidase with BUF1 showing the highest inhibitory activity (IC50 = 3.42 μg/mL). The dominant phenolic acids were sinapic, gallic, ferrulic, syringic, gallic and caffeic acids and the prominent flavonoids were myricetin and quercetin. These findings suggest that the seeds of M. saigonense have potential as a source of antidiabetic agent (s).


1992 ◽  
Vol 1 (1) ◽  
pp. 49-54 ◽  
Author(s):  
W. M. S. C. Tamashiro ◽  
B. M. Tavares-Murta ◽  
F. Q. Cunha ◽  
M. C. Roque-Barreira ◽  
R. M. D. Nogueira ◽  
...  

Inhibitory effect upon neutrophil migration to the inflammatory focus was previously detected in the cell-free incubation fluid of lipopolysaccharide (LPS)-stimulated macrophage monolayers. In the present study we showed that the neutrophil recruitment inhibitory activity from this supernatant was mainly detected in a fraction (P2) obtained by gel filtration chromatography on Sephacryl S-300. P2 fraction was able to inhibit ‘in vivo’ neutrophil emigration induced by different inflammatory stimuli, but it did not affect ‘in vitro’ neutrophil chemotaxis induced by FMLP. When injected intravenously, P2 inhibited oedema induced by carrageenin or immunological stimulus but not the oedema induced by dextran, thus affecting cell-dependent inflammatory responses. It was observed that P2 also induced neutrophil migration when injected locally in peritoneal cavities. This activity was significantly reduced by pretreatment of the animals with dexamethasone. Cytokines, such as IL-8 and TNF-α that are known to exhibit inhibitory effect upon neutrophil migration, were not detected in P2 fraction by highly sensitive assays. Overall the results suggest the existence of a novel cytokine exhibiting ‘in vivo’ neutrophil inhibitory activity, referred as NRIF.


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.


Foods ◽  
2020 ◽  
Vol 9 (7) ◽  
pp. 847 ◽  
Author(s):  
Henryk Zieliński ◽  
Joanna Honke ◽  
Joanna Topolska ◽  
Natalia Bączek ◽  
Mariusz Konrad Piskuła ◽  
...  

The angiotensin converting enzyme (ACE) inhibitory activity and phenolics profile of fermented flours and of baked and digested buckwheat biscuits was studied. The fermentation of buckwheat flour by select lactic acid bacteria (LAB) caused a decrease in ACE inhibitory activity as compared to the non-fermented flour. The baking process significantly reduced the ACE inhibitory activity of biscuits obtained from fermented flours, whereas digestion significantly increased these properties. In non-fermented and fermented flours and buckwheat biscuits before and after in vitro digestion samples, ten phenolic acids and eight flavonoids were found. Highly significant correlations were found between sample concentration of 50% inhibition of ACE (IC50) and total phenolic compounds of fermented flour and biscuits before and after digestion for each applied LAB, thus indicating a link between phenolic compound content and ACE inhibitory activity. In the digested biscuits, the input to ACE inhibitory activity was provided by p-coumaric, sinapic, syringic, vanillic, and protocatechuic acids as well as by kaempherol, quercetin, apigenin, and orientin. Therefore, it can be concluded that cumulative action of those phenolic acids and flavonoids released after digestion is responsible, in part, for the bioaccessible ACE inhibitory activity of buckwheat biscuits.


2020 ◽  
Vol 15 (8) ◽  
pp. 1934578X2094466
Author(s):  
Shi-Ying Huang ◽  
Hui-Min David Wang ◽  
Jianhua Ke ◽  
Jian Li ◽  
Lili Chen ◽  
...  

Previous studies have focused on the role of a cultured red macroalga Bangia fuscopurpurea as a functional food; however, except for antioxidant activity, there are no reports directly regarding the potential cosmetic properties of this alga. Our present study explored the moisturizing effect of its ethanol extract (BFH1) and used the tyrosinase activity inhibition assay to evaluate its in vitro whitening effect. The in vitro moisture-retention ability of BFH1 was similar to that of glycerol (positive control), but its moisture-absorption ability was significantly higher. The overall in vivo moisturizing effect of topical application of BFH1 in mice was similar to that of glycerol, but BFH1 did not cause significant changes in the oil content of the skin, and there were no obvious side effects regarding skin appearance and external behavior during treatment. BFH1 exerted in vitro tyrosinase inhibitory activity with a half-maximal inhibitory concentration (IC50) of 48.3 μg/mL (IC50 of positive control, vitamin C: 19.6 μg/mL). The total phenolic content of BFH1 was determined as 10.8 % ± 0.07 %. Thus, BFH1 has high potential to be turned into a cosmetic ingredient with moisturizing and whitening effects.


Blood ◽  
1982 ◽  
Vol 59 (3) ◽  
pp. 625-627
Author(s):  
JG Kelton ◽  
CJ Carter ◽  
A Santos ◽  
J Hirsh

There is evidence from clinical studies and animal experiments that aspirin has a greater antithrombotic activity in males compared to females. We investigated platelet function in vitro and in vivo in rabbits before and after the administration of a dose of aspirin (5 mg/kg) which inhibited collagen stimulated thromboxane B2 generation. Infusion of collagen into untreated animals resulted in a 38 +/- 4% (m +/- SE, n = 13) decrease in platelet count (assessed by whole blood radioactivity) in the male animals, and a 27 +/- 3% (m +/- SE, n = 13) in the female animals. Pretreatment with aspirin resulted in a significant inhibitory effect in the male but not the female animals (p less than 0.05). The male animals had significantly greater thromboxane B2 generation in vivo than did the female animals following an equal dose of collagen (males, 2.64 +/- 0.7 ng/ml thromboxane B2, n = 14; females, 1.67 +/- 0.4 ng/ml thromboxane B2, n = 15, p less than 0.05). In contrast no sex related difference in the inhibitory effect of aspirin on maximal collagen induced aggregation was found when platelets were studied in vitro. The greater reactivity of male patients in vivo may be accounted for by the observed increase in thromboxane B2 generation. This might also explain the greater thrombotic tendency of males, and the observed difference in the antithrombotic effect of aspirin in males and females.


2021 ◽  
Author(s):  
Luiz Henrique Corrêa Portari ◽  
Silvia Regina Correa-Silva ◽  
Julio Abucham

Introduction: Cabergoline is the treatment of choice for prolactinomas. However, 10-20% of prolactinomas are resistant to cabergoline. Metformin, a biguanide widely used in the treatment of diabetes mellitus, has been shown to reduce prolactin secretion in various pituitary tumor cell lineages both in vitro and in vivo and in human pituitary adenomas in vitro. The aim of this study is to test the effects of metformin addition to cabergoline treatment on prolactin levels in patients with resistant prolactinomas. Subjects and Methods: This is a prospective study performed in an outpatient clinic in a reference center. Ten adult patients (26-61 y) with prolactinomas (7M), persistent hyperprolactinemia (38-386 ng/mL) under cabergoline treatment (2-7 mg/week) for at least six months (6-108 mo), features of metabolic syndrome and not taking metformin were included. Metformin (1.0-2.5 g v.o./d) was given according to patients´ tolerance. Cabergoline doses were kept unchanged. Serum prolactin levels were measured before and after short- (30-60 d) and long- term (120-180 d) metformin treatment. Results: Mean prolactin levels did not show any significant changes (148 ± 39 ng/ml vs 138 ± 42 ng/ml vs 133 ± 39 ng/ml, before, at 30-60 days, and at 120-180 days, respectively, P=0.196) after metformin (mean dose: 1.25 g/day; range: 1.0-2.0 g/day). No patient reached a normal prolactin level during metformin treatment. Two patients were considered partial responders for exhibiting prolactin decreases ≥50% at a single time point during metformin. Conclusion: Metformin addition to ongoing high dose cabergoline treatment in patients with cabergoline-resistant prolactinomas failed to show a consistent inhibitory effect in serum prolactin levels.


2016 ◽  
Vol 2016 ◽  
pp. 1-7 ◽  
Author(s):  
Gyo-Nam Kim ◽  
Mi-Rae Shin ◽  
Sung Ho Shin ◽  
Ah Reum Lee ◽  
Joo Young Lee ◽  
...  

Pancreatic lipase is the enzyme responsible for digestion and absorption of triglycerides, being its inhibition one of the widest studied methods used to determine the potential activity of natural products to inhibit dietary fat absorption. Decrease of energy intake from dietary fat through inhibition of this enzyme may be an excellent strategy to prevent and treat obesity. The inhibitory activity on pancreatic lipase enzyme ofDiospyros kakifruit andCitrus unshiupeel mixture extract (PCM) was evaluatedin vitroand its antiobesity effects were studied based on the serum lipid parameters analysis from high-fat diet- (HFD-) fed micein vivo. PCM was orally administered at a dose of 50 and 200 mg/kg body weight for 6 weeks. In addition, the activity of pancreatic lipase was assessed using orlistat (positive control). PCM exhibited inhibitory effect on lipase activity with IC50value of 507.01 μg/mL. Moreover, serum triacylglycerol, total cholesterol levels, and visceral fat weight were significantly reduced compared to HFD control mice in PCM 200 mg/kg-treated mice (p<0.05). These results suggest that PCM administration may be a novel potential antiobesity agent for reduction of fat absorption via inhibition of pancreatic lipase.


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