scholarly journals IN VITRO ANTIUROLITHIATIC ACTIVITY OF MACERATED AQUEOUS EXTRACT OF TERMINALIA BELERICA BY USING TURBIDITY METHOD

Author(s):  
ANU V. ◽  
AKHILA S. ◽  
SNEHA ANTONY

Objective: To evaluate the anti-urolithiatic activity of macerated aqueous extract of Terminalia belerica by using turbidity method Method: The present study was used to study the inhibitory effect of the Terminalia belerica on urinary stone formation. The aim of study was to examine the In vitro antiurolithiatic activity of macerated aqueous extract of T.belerica was to estimate inhibitory activity of aqueous extract on the formation of urinary stone. Cystone was used as a positive control. Anti urolithiatic study was performed by turbidity method. Result: The percentage inhibition shown by aqueous extract at 20μg/ml was 60% and with almost constant inhibition at 100μg/ml and 200μg/ml ranging between 72% and 80%. The percentage inhibition showed by aqueous extract of Terminalia belerica has significant compared to standard drug. Conclusion: In future this drug can be performed in vitro and clinical study beneficial for people with avoiding adverse effect of modern medicinal drugs

2017 ◽  
Vol 243 (4) ◽  
pp. 375-385 ◽  
Author(s):  
Siti Rosmani Md Zin ◽  
Zahurin Mohamed ◽  
Mohammed A Alshawsh ◽  
Won F Wong ◽  
Normadiah M Kassim

Anastatica hierochuntica L. ( A. hierochuntica), a folk medicinal plant, was evaluated for mutagenic potential via in vitro and in vivo assays. The in vitro assay was conducted according to modified Ames test, while the in vivo study was performed according to Organisation for Economic Co-operation and Development guideline for mammalian erythrocyte micronucleus assay. Four groups ( n= 5 males and 5 females per group) Sprague Dawley rats were randomly chosen as the negative control, positive control (received a single intramuscular injection of cyclophosphamide 50 mg/kg), 1000 and, 2000 mg/kg A. hierochuntica aqueous extracts. All groups except the positive control were treated orally for three days. Findings of the in vitro assay showed mutagenic potential of AHAE at 0.04 and 0.2 mg/ml. However, no mutagenic effect was demonstrated in the in vivo study up to 2000 mg/kg. No significant reduction in the polychromatic and normochromatic erythrocytes ratio was noted in any of the groups. Meanwhile, high micronucleated polychromatic erythrocytes frequency was seen in cyclophosphamide-treated group only. These findings could perhaps be due to insufficient dosage of A. hierochuntica aqueous extracts to cause genetic damage on the bone marrow target cells. Further acute and chronic in vivo toxicity studies may be required to draw pertinent conclusion on the safety aspect of A. hierochuntica aqueous extracts consumption. Impact statement In this paper, we report on the mutagenicity evaluation of Anastatica hierochuntica aqueous extract. This is a significant research in view of the popularity of this herb consumption by the people across the globe despite of limited scientific evidence on its toxicity potential. This study is intended to encourage more extensive related research in order to provide sufficient evidence and guidance for determining its safe dosage.


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.


Molecules ◽  
2019 ◽  
Vol 24 (16) ◽  
pp. 2912 ◽  
Author(s):  
Sherif T. S. Hassan ◽  
Miroslava Šudomová ◽  
Kateřina Berchová-Bímová ◽  
Karel Šmejkal ◽  
Javier Echeverría

Psoromic acid (PA), a bioactive lichen-derived compound, was investigated for its inhibitory properties against herpes simplex virus type 1 (HSV-1) and type 2 (HSV-2), along with the inhibitory effect on HSV-1 DNA polymerase, which is a key enzyme that plays an essential role in HSV-1 replication cycle. PA was found to notably inhibit HSV-1 replication (50% inhibitory concentration (IC50): 1.9 μM; selectivity index (SI): 163.2) compared with the standard drug acyclovir (ACV) (IC50: 2.6 μM; SI: 119.2). The combination of PA with ACV has led to potent inhibitory activity against HSV-1 replication (IC50: 1.1 µM; SI: 281.8) compared with that of ACV. Moreover, PA displayed equivalent inhibitory action against HSV-2 replication (50% effective concentration (EC50): 2.7 μM; SI: 114.8) compared with that of ACV (EC50: 2.8 μM; SI: 110.7). The inhibition potency of PA in combination with ACV against HSV-2 replication was also detected (EC50: 1.8 µM; SI: 172.2). Further, PA was observed to effectively inhibit HSV-1 DNA polymerase (as a non-nucleoside inhibitor) with respect to dTTP incorporation in a competitive inhibition mode (half maximal inhibitory concentration (IC50): 0.7 μM; inhibition constant (Ki): 0.3 μM) compared with reference drugs aphidicolin (IC50: 0.8 μM; Ki: 0.4 μM) and ACV triphosphate (ACV-TP) (IC50: 0.9 μM; Ki: 0.5 μM). It is noteworthy that the mechanism by which PA-induced anti-HSV-1 activity was related to its inhibitory action against HSV-1 DNA polymerase. Furthermore, the outcomes of in vitro experiments were authenticated using molecular docking analyses, as the molecular interactions of PA with the active sites of HSV-1 DNA polymerase and HSV-2 protease (an essential enzyme required for HSV-2 replication) were revealed. Since this is a first report on the above-mentioned properties, we can conclude that PA might be a future drug for the treatment of HSV infections as well as a promising lead molecule for further anti-HSV drug design.


2020 ◽  
Vol 32 (4) ◽  
pp. 776-782
Author(s):  
Ravindra S. Sonawane ◽  
Kiran D. Patil ◽  
Avinash V. Patil

A series of novel imidazopyridine derivatives as proton pump inhibitors was designed with compounds of CID data base and explored considering AZD0865 as standard. Many compounds were identified and docked in proton pump ATPase pocket (PDB ID: 4ux2). Molecular docking studies revealed that many compounds showed good proton pump ATPase inhibitory activity. The docking poses revealed the interaction of ligands with amino acid. The standard drug AZD0865 had docking score of -7.112302 and displayed interactions with Asn138 and Asp137. A series of novel imidazopyridine derivatives as proton pump inhibitors were docked, synthesized and characterized by IR, NMR, CHN and MS spectral analysis. The target imidazopyridines were prepared from substituted 2-aminonicotinic acid and 2-bromo-1-substituted ethanone. in vitro Studies explained that few compounds exhibited moderate to good proton pump ATPase inhibitory activity in comparison with the reference drugs i.e. AZD0865. Compounds 11 and 12 shown higher activities with the IC50 4.3. Compounds 1, 4, 6, 7, 8, 10 and 13 showed weak anti-ulcer activity with its IC50 5.2, 5.8, 5.5, 5.1, 4.9, 4.6 and 5.9 and positive control AZD0865 shown IC50 2.0.


2020 ◽  
Vol 23 ◽  
pp. 54-62
Author(s):  
O.O. Amujoyegbe ◽  
M. Idu ◽  
J.M. Agbedahunsi ◽  
G.N. Bazuaye

Sickle cell disorder is a genetic ailment with enormous social and economic burden for patients and caregivers. The most promising management apart from being expensive particularly for poor African people, faces some major incompatibility problems. The patients consequently rely on herbal therapy which could be prepared in single or combination forms to manage the painful episodes and its complications. This present study aimed to formulate polyherbal combination and evaluate three purposively selected plants previously reported for their antisickling activities. The polyherbal products were formulated using both aqueous and 70% ethanol extracts into different combinational ratio with the best in 1:1:1 and evaluated for its antisickling activity. The antisickling activity involved both the inhibitory and reversal effects at varying concentrations from 1.0 mg/ml to 6.0 mg/ml using ciklavit as the positive control. The best inhibitory activity was found in ethanol extract of Piper guineense, Gongronema latifolium and Cymbopogon citratus (PGC) with 70.09 ± 0.67% when compared with the positive control (59.25 ± 0.05%) at 4.0 mg/mg while the reversal ability was 67.87 ± 1.23%. The aqueous extracts of the combinations had activity above 50% with the exception of PGC (2:3:1) which is a little less than 50% (46.67 ± 0.98%) while the highest was 60.02 ± 0.87%. The polyherbal ethanol extract had better effects than the aqueous extract and the standard drug used in this study.


2021 ◽  
Author(s):  
Ramchandra Ranadive Kiran ◽  
J. Neeta Karale ◽  
Jagtap Nilesh Pradnya ◽  
Ivan V. Zmitrovich ◽  
Vladimir V. Perelygin

The aim of this study is to test the effect of aqueous, ethereal and alcoholic extracts of the fruit bodies of the wood-destroying fungus Inonotus rickii on locomotor activity resulting from contraction of both cross-striated and smooth muscles. The pharmacological activity of I. rickii raw materials was determined in vitro using the dose-response curve method (smooth muscles) and in experiments with oral intake of extracts (CNS-mediated effects on cross-lacing muscles). The aqueous extract of fungal material showed an increase in the motor activity of smooth muscles compared to standard caffeine, which indicates the ability of fungal extract to have a stimulating effect on the synapses. It was found that I. rickii extracts have an effect on smooth muscle contraction similar to the acetylcholine. It was shown that the greatest stimulating activity demonstrates an aqueous extract that may be a result of inhibitory effect of diethyl ether and ethanol on synapses. The described effects put on the agenda both the fractionation of active extracts and further experiments on the therapeutic applications of their described properties. As a field of possible application of this kind of substances can be considered the cardiovascular remodeling, the maintenance of smooth muscle tone during a number of surgical interventions, and the palliative cure of disseminated cancers.


2019 ◽  
Vol 51 (2) ◽  
pp. 234-241
Author(s):  
V. A. Kadnor ◽  
S. N. Shelke

A series of carbazole-based 1,4-benzothiazepine and pyrazoline derivatives were synthesized and the structures of the newly synthesized compounds were confirmed by FT-IR, 1H NMR, 13C NMR and mass spectral studies. All new derivatives 4(a-f) and 5(a-e) were screened for their in vitro antimicrobial activity, and also for their antimalarial activity. Compounds 4a, 4b, 4d, 5a, 5b and 5c exhibited promising antimicrobial and antimalarial activities as compared to positive control. Notably, compounds 4a, 4b and 4d showed excellent antifungal activity against Penicillium sp. comparable to that of a standard drug.


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