Journal of Pharmacy Research最新文献

Beta-thalassemia is a genetic disease caused by either reduced production or complete absence of beta-globin chains. It is characterized by dyserythropoiesis which leads to the development of early erythroid precursor cells into immature erythroblasts. Patients with high level of fetal hemoglobin (HbF) develop less severe symptoms and survive normally. Therefore, augmentation of the level of HbF has been an effective therapeutic approach for patients of beta-thalassemia. Iron overload is the leading cause of mortality in beta-thalassemia. Natural pharmacological agents have been used to stimulate the HbF level and reduce iron overload in patients suffering from this deleterious disease. This is an efficient way to treat beta-thalassemia as it also provides better correlation between in vivo and in vitro synthesis of beta-globin chains in patients. Being economic, it is also affordable for the patients in developing countries. This article reports some natural compounds of plant origin having a therapeutic role in inducing HbF level and possessing chelation therapy in beta-thalassemia patients.

Aim

Acetyl-CoA carboxylase (ACC) is a biotin-dependent enzyme which plays a key role in fatty acid biosynthesis via production of melonyl-CoA as an essential substrate. It is involved in homeostasis of fatty acids inside the system using both up and down regulating mechanisms. Apart from this In silico analysis of its catalytic site and regulatory sites make it a potential target for herbicidal and insecticidal drug targeting. Currently the 3D structure of Acetyl-CoA carboxylase (ACC) from Jatropha curcas has not been solved in Protein Data Bank (PDB). Hence the aim of the present study is to build the 3D structure of Acetyl-CoA carboxylase (ACC) from J. curcas also to perform a virtual screening for the identification of the effective inhibitors using molecular docking studies.

Methods

Homology modeling has been used to determine the 3D structure of Acetyl-CoA carboxylase (ACC) from J. curcas. Structure validation and molecular docking studies has been carried out using Procheck and Molegro Virtual Docker respectively.

Results

Ramachandran Plot confirmed quality of modeled structures along with main chain and side chain parameters. Out of 309 residues in SPDBV model, 244 were in core region 19 residues were in additional allowed region, 2 residues were in generous allowed region and no residues were in disallowed region.

Conclusion

Energy minimization for SPDBV model thermodynamically proved accepted structure with energy of −12,063.024 kJ/mol. The model further can be subjected to pharmacodynamic and pharmacokinetic studies. Molecular docking studies identified few established herbicides which could be promising inhibitors of Acetyl-CoA carboxylase (ACC). Efforts to screen and identify ACC inhibitors using flexible molecular docking resulted in Pinoxaden from Phenylpyrazole class as the most effective inhibitor with rerank = −81.436 and RMSD = 0.31.

Aim

The present study was carried out to evaluate the hepatoprotective activity of different extracts of Gynandropsis gynandra.

Methods

The different extracts of G. gynandra at doses 100, 200 and 400 mg/kg b.w. were tested for their hepatoprotection against carbon tetrachloride (CCl₄) induced liver intoxication in rats.

Results

The extracts of G. gynandra showed a dose dependent hepatoprotection activity. Among all the extracts, methanolic extract produced maximum hepatoprotection (71.45%) at a dose of 400 mg/kg.

Conclusion

The results of the present investigation indicate that all the extracts of G. gynandra possess hepatoprotective activity and this effect was may be due to the presence of various chemical constituents.

Objective

Brahmi (Bacopa monnieri Linn) is an important herb in Ayurved, reported to have a wide range of medicinal properties. In clinical practice it is usually prescribed in its various dosage forms. The most common of those are Brahmi Ghrita (BG) and Saraswatarishta (SW). Use of Brahmi as anti-convulsion drug is well documented in scientific literature however; no data is available on the effect of its commonly practiced dosage forms. Hence, the study was carried out to evaluate anti-convulsion potential of BG and SW.

Method

The anticonvulsant activity of BG and SW was studied against seizures induced by Maximal Electroshock (MES) in rats and phenytoin (25 mg/kg Intra Peritoneal) was used as standard. Different phases of convulsions (Hind limb extension, jerking, grooming, tail straub and recovery) were recorded as index of convulsion. The brain tissue was dissected out for biochemical analysis.

Result

Treatment of rats with SW and BG in Maximal Electroshock (MES) induced convulsions showed statistically significant potential as compared to control groups (P ≤ 0.01 or P ≤ 0.001). SW or BG showed significant improvement in all the phases of convulsion except grooming response. Brain tissues of test animals evaluated for malondialdehyde (MDA) levels showed the higher levels in phenytoin group than in BG and SW treated group suggesting protection of brain tissue from oxidative damage.

Conclusion

The results indicated SW and BG to be effective in promoting restorative and neuroprotective action in convulsions thus suggesting a further scope of evaluation of these formulations as an adjuvant treatment for convulsions.

Objective

To establish the pharmacognostic parameters using pharmacopoeial standards for correct identity of Patala (Stereospermum chelonoides (L.f.) DC.) and to compare original species with recommended substitutes (Stereospermum tetragonum DC. and Radermachera xylocarpa (Roxb.) K. Schum.).

Methodology

The pharmacognostic parameters include morphology, etymology, physicochemical properties, phytochemical analysis, HPTLC fingerprint and quantification of standard marker compound.

Results

The etymological characters mentioned are tree, mature leaflets being rough, and inflorescences with black peduncles, flowers picture-like, copper colour and eye ball-seed leads to relate the identity as S. chelonoides. The physicochemical properties match to S. tetragonum with respect to pharmacognostic limits prescribed for S. chelonoides. Phytochemical screening of all three species viz., S. chelonoides, S. tetragonum and R. xylocarpa collected from different biogeographic regions of India showed presence of carbohydrates, saponins, proteins, flavonoids, gums and resins. The standard marker p-coumaric acid is detected with Rf 0.37 in methanolic root extracts of all three species with different concentrations.

Conclusion

The developed HPTLC profile for the roots of Patala serves as an inexpensive qualitative tool in quality control for differentiating substitutes and adulterants from the authentic species of Patala and rapid approach to detect and quantify p-coumaric acid; similar studies concluded that the roots of S. chelonoides is the authentic Patala.

Background and aim

The stem bark of Alstonia boonei is used in traditional medicine to treat or reduce inflammation and pain in Nigeria. In view of these, the effect of the ethanol extract of its stem bark on agar-induced leucocyte migration in rats as a mechanism of anti-inflammation was investigated.

Methods

The effect of the ethanol extract of the stem bark of A. boonei on agar-induced leucocyte migration in rats was evaluated using standard analytical method.

Results

The results showed significant (p < 0.05) inhibitions of leucocyte migrations in the rats administered 400, 800 and 1200 mg/kg body weight (b. w) compared to the leucocyte migration of the rats in the control group (5 ml/kg b. w of normal saline). The inhibitory effect of the extract was dose-dependent and comparable to that of the reference anti-inflammatory drug, indomethacin (0.3 mg/kg b. w).

Conclusion

The data indicate that the ethanol extract of the stem bark of A. boonei possesses remarkable inhibitory effect on leucocyte migration and therefore, justifies the traditional use of the stem bark of A. boonei as an anti-inflammatory agent.

Background

An increasing demand for natural additives has shifted the attention from synthetic to natural antioxidants. As leafy vegetables are found to be good source of antioxidants and the present study is to examine the antioxidant potential and antimicrobial activity of leaf extracts of Pimpinella tirupatiensis.

Methods

Antioxidant potential of leaves of P. tirupatiensis was studied using different methods like DPPH, nitric oxide, hydrogen peroxide scavenging activity. Reducing power and antimicrobial activity was estimated by using both gram positive and gram negative microorganisms by using DMF as solvent.

Results

The aqueous extracts showed maximum scavenging activity of DPPH followed by nitric oxide, hydrogen peroxide and reducing power respectively. Benzene and alcoholic extract showed maximum antimicrobial activity.

Conclusion

Substantial amounts of antioxidants including vitamins C and E, carotenoids, flavonoids, phenols and tannins etc. can be utilized to scavenge the excess free radicals from the body.

Aim

This study was designed to assess the antioxidant property of crude methanolic extract of Tetracera potatoria roots (MeTp); a bioactive constituent isolated from it, betulinic acid (BA) and a combination of BA with ascorbic acid.

Methods

The crude extract was obtained by cold extraction. Phytochemical screening of the crude extract was carried out using standard methods. Isolation of betulinic acid (BA) was effected by Accelerated Gradient Chromatography (AGC) fractionation of MeTp. Structural elucidation of the isolated BA was done with ¹H and ¹³C NMR spectroscopic technique. MeTp, isolated BA and BA plus ascorbic acid mixture (1:1) were evaluated for their antioxidant activity by 1,1-diphenyl-2-picrylhydrazyl, (DPPH) method.

Results

The phytochemical analysis showed the presence of alkaloids, flavonoids, cardiac glycosides, saponins and tannins. Anthraquinones were absent. The ¹H and ¹³C NMR data obtained for the isolated BA were in accordance with published data. Antioxidant activity (IC₅₀) of tested materials ranged from 18 to 148 μg/ml, with MeTp having the highest value relative to ascorbic acid, the reference standard. The radical scavenging activities of MeTp and that of BA plus ascorbic acid mixture were greater than that of ascorbic acid alone, indicating synergism between ascorbic acid and betulinic acid.

Conclusion

The findings established the antioxidant property of methanolic root extract of T. potatoria. The combination of betulinic acid and ascorbic acid could be useful for the development of new antioxidant drug.

Aim

The present study was aimed to synthesis series of quinazolinone derivatives against mammary carcinoma.

Methods

The compounds were synthesized by reaction of nucleophilic attack, Wohler's classical synthesis followed by condensation reaction. The synthesized quinazolinone derivatives were characterized by physico chemical analysis like melting point, TLC, IR, UV and NMR. Compounds have been evaluated for their in-vitro antioxidant methods like DPPH method, H₂O₂ method, nitrous oxide scavenging method, super oxide scavenging method, ABTS radical scavenging, lipid peroxidation and also in-vitro cytotoxicity study against MCF-7, BT-549, ZR-75 (human breast cancer) cell lines by MTT assay method.

Results

From physico chemical data the structure of synthesized compounds was confirmed. Antioxidant activity was found from the IC₅₀ value. Qc showed lowest IC₅₀ value in DPPH radical scavenging assay and nitric oxide scavenging assay and was observed to be 27.20 μg/ml and 26.3 μg/ml respectively. In super oxide scavenging activity and lipid peroxidation and H₂O₂ assays showed a good activity it was observed 26.3 μg/ml, 18.10 μg/ml and 21.4 μg/ml respectively. Qb showed lowest IC₅₀ value in ABTS radical scavenging assay and was observed to be 26.9 μg/ml. Qe showed lowest IC₅₀ value in lipid peroxidation method and was observed to be 149 μg/ml. QN-D showed a moderate antioxidant. In cytotoxic activity, Qc showed lowest IC₅₀ value, i.e. 21.77, 23.03 and 21.14 μg/ml and Qb showed moderate values like 23.25 μg/ml, 27.39 μg/ml and 27.86 μg/ml in MCF-7, BT-549 and ZT-75 respectively.

Conclusion

All the synthesized compounds showed moderate to good antioxidant and potent cytotoxic activity.

Objective

To evaluate the antimalarial activity of ethanolic extract of Neopetrosia exigua in ICR mice. The safety of the extracts was also ICR mice by the acute oral toxicity test.

Methods

The crude ethanol extract of Neopetrosia exigua (50, 100, 200 and 400 mg/kg) was investigated for its antimalarial activity against Plasmodium berghei during early infection. The acute toxicity of the extract was also investigated. At the end of 14 days, mice were sacrificed for histopathology study.

Results

The extract of Neopetrosia exigua demonstrated significant (p < 0.05) schizonticidal activity. The acute toxicity test showed that the extract of Neopetrosia exigua is toxicological safe by oral administration. Histopathological study revealed normal architecture of kidney and liver of mice.

Conclusion

The extract of sponge Neopetrosia exigua has anti-malarial activity in vivo.