Open Access Original Research Article

Evaluation of Methanolic Extract Induced Antinociceptive, Anti-pyretic and Anti-inflammatory Activity of Ficus hispida Leaves

S. M. Mushiur Rahman, Md. Rubel Haque, Md. Ashraful Zaman, Sohel Rana, Samiron Sana, Md. Tanjir Imam Hasan

Journal of Pharmaceutical Research International, Page 1-12
DOI: 10.9734/JPRI/2018/41664

Objective: Traditionally Ficus hispida is used as a palliative for pain, inflammation, diabetes, fever and neurological disorders. The present study set out to evaluate the antinociceptive, anti-pyretic and anti-inflammatory activity of the methanolic extract of Ficus hispida leaves (MFHL).

Methods: Pithy dried leaves of Ficus hispida were extracted with sufficient amount of pure methanol. The antinociceptive activity of MFHL was evaluated by using formalin induced paw licking, acetic acid-induced writhing, tail immersion and hot plate methods in Swiss albino mice. Its anti-pyretic activity was evaluated by Brewer’s yeast-induced pyrexia test. And anti-inflammatory activity was assessed by using xylene-induced ear edema test.

Results: The crude extract was found to have significant (p<0.05, vs. control) analgesic activity at the oral dose of 200 & 400 mg/kg b. wt., in the tested animals. Extract at dose of 200 mg/kg and 400 mg/kg significantly (p<0.05, vs. control) reduced paw licking and abdominal writhing of mice, and revealed significant increase in latency (p<0.05, vs. control) in tail immersion and hot plate test at 30 and 60 min after their administration. In Brewer’s yeast- induced pyrexia test, the methanolic extract at the dose of 200 mg/kg and 400 mg/kg significantly (p<0.05, vs. control) reduced hyperthermia in mice in 1 hour observation and also lowering of temperature from 2 hours to 4 hours observation period respectively. In anti-inflammatory test, 200 mg/kg and 400 mg/kg of extract exhibited significant (p<0.05, vs. control) ear weight differences and inhibition of ear edema.

Conclusion: Results of above study indicate that Ficus hispida leaves can be a potential source of analgesic, antipyretic and anti-inflammatory medication.

Open Access Original Research Article

The Synergistic Effect of Curcumin and Ziziphora Extract Due to Their Anti-inflammatory and Antioxidant Properties on Ovarian Tissue Follicles

Amir Raoofi, Abdollah Amini, Reza Masteri Farahani

Journal of Pharmaceutical Research International, Page 1-11
DOI: 10.9734/JPRI/2018/45124

Background: The aim of this study was to evaluate the synergistic effect of curcumin and Ziziphora extract due to their anti-inflammatory and antioxidant properties on ovarian tissue follicles in the rat model of the polycystic ovary syndrome (PCOS).

Methods: This experimental study was conducted on 60 female Wistar rats randomly divided into 6 groups of 10. The sham group (receiving curcumin and Ziziphora solvents), the control group (without injection), the PCOS group (injection of 2 mg of estradiol valerate to each rat) and the experimental groups that received intraperitoneal injection of curcumin (600 mg/kg), Ziziphora extract (300 mg/kg) and the combined curcumin and Ziziphora extract after syndrome induction. After 14 days of treatment, the animals were sacrificed by chloroform to collect blood and ovary specimens for histological and serological studies.

Results: The PCOS caused a significant decrease in body weight and ovaries (p<0.001), follicular and granulosa sheath thickness, number of corpus luteum (p <0.001) compared to control group. However, there was no significant difference in tissue changes in experimental ovaries compared to the control. A decrease in LH, estradiol and testosterone, and an increase in FSH and progesterone were significant in the experimental groups compared to the PCOS group (p<0.001). Also, in the PCOS group, the LH, estradiol and testosterone levels were increased significantly, while the FSH and progesterone levels were decreased. In addition, the serum lipid profiles in the experimental group were significantly higher than the PCOS group (p<0.001).

Conclusion: Curcumin and Ziziphora extract due to their antioxidant and anti-inflammatory properties were effective in reducing cysts and modifying the hormonal levels in the polycystic ovary syndrome.

Open Access Original Research Article

Impact of Various Solvents on Yield and Activity of Phenolics and Flavonoides of Ulva lactuca (Chlorophyta) Algae

Abdulrahman L. Al-Malki, Elie K. Barbour, Maryam H. Al-Zahrani, Said S. Moselhy

Journal of Pharmaceutical Research International, Page 1-7
DOI: 10.9734/JPRI/2018/44875

Context: The degenerative diseases, due to generation of reactive oxygen species are one of the main human health hazards in the densly populated cities.

Objective: This study aims at providinga scientific support related to richness of antioxidants in the marine Ulva lactuca (Chlorophyta) algae and their high scavenging activity against various free radicals.

Materials and Methods: Three different solvents were applied on Ulva lactuca (Chlorophyta) algae to compare the recovery of phenolics and flavonoids. The reducing power and scavenging activity of the extracts, against hydroxyl and nitrate radicals, were assessed.

Results: The ethyl acetate extract (EAE) was superior to that of the ethanol and chloroform in obtaining the highest significant recovery of phenolics and flavonoids from Ulva lactuca (Chlorophyta) algae (P ˂ 0.05). In addition, the EAE had the highest significant reducing power and scavenging activity against three radicals (P ˂ 0.05) compared to other two solvents.

Conclusion: The EAE helped in uncovering the richness in antioxidants of Ulva lactuca (Chlorophyta) algae, associated with significant scavenging activity against various radicals. This scientific evidence could be as a prophylactic against degenerative diseases, pending the proof of its safety and efficacy in experimental in vivo trials.

Open Access Original Research Article

Identifying Potential Dual Inhibitory Candidates for Non-Small Cell Lung Cancer through Molecular Docking, 3D-QSAR Pharmacophore-based Virtual Screening, Comparative Molecular Field and Similarity Indices Analysis Modeling

Xiao X. Zhu, Yan Li, Xuan R. Zhang, Lun Yuan, Pei H. Luo, X. Gao, Zhong S. Tan

Journal of Pharmaceutical Research International, Page 1-17
DOI: 10.9734/JPRI/2018/44771

Aim: This work aims to understand potential inhibitory structural requirements and identify lead compounds for non-small cell lung cancer through 3D-QSAR pharmacophore-based virtual screening, molecular docking, CoMSIA and CoMFA QSAR modelling.

Materials and Methods: QSAR pharmacophore models were developed by HypoGen Module and validated by test data set, Fischer’s randomization and Guner-Henry equation. The well-validated pharmacophore model was employed to perform virtual screening to identify potent hits from ZINC database. The retrieved hits were subsequently subjected to filtering using ADMET descriptors and Lipinski’s Rule of Five. CoMSIA and CoMFA were then utilized to produce QSAR models on phenylpyrimidine derivatives also.

Results: Validations on 3D-QSAR pharmacophore model indicate that the enrichment factor is 6.34, GH is 0.517 and a correlation coefficient is 0.83, implying its highly predictive ability. Top three hits: ZINC29356266, ZINC06589615, and ZINC03375633 were identified as promising potent inhibitory candidates with IC50 value of about 0.54 µM and fitness value of about 59.4. Interestingly, the top three hits indicate dual inhibitory activity targeting EGFR and PD-L1 from structure-based docking. Two developed QSAR models from CoMSIA and CoMFA modelling indicate a potential predictive ability (q2=0.67, and 0.71 respectively). The designed compound C indicates a more potential (dual) inhibitory activity (pIC50=7.39) targeting EGFR (fitness=59.78) and CTLA-4 (fitness =47.90).

Conclusion: Validations indicate that the developed 3D-QSAR pharmacophore model is highly predictive. Top three hits were identified as promising potent inhibitory candidates and indicated dual inhibitory activity targeting EGFR and PD-L1. The designed compound C indicates a more potential (dual) inhibitory activity targeting EGFR and CTLA‐4. These important 3D-QSAR and molecular docking bioinformatics results achieved from this work should be valuable in designing more promising potent inhibitory candidates and developing novel lead compounds against advanced NSCLC in future.

Open Access Review Article

The Protective Role of Thymoquinone against Drugs Toxicity: A Review

Mohsen G. Alrashedi

Journal of Pharmaceutical Research International, Page 1-11
DOI: 10.9734/JPRI/2018/44944

Any drug can have side effect at a certain dose which limits its use. On the other hand, evidence support the role of herbal medicines in the prevention and cure of several diseases. Thymoquinone (TQ) is a bioactive component found in the volatile oil of Nigella sativa "black seed". Studies have demonstrated the therapeutic and protective activity of TQ against drug toxicities on various body systems which have been attempted to be reviewed in this article.