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Jafri, Asif
- Antiproliferative and Antibacterial Activity of Some Para-Substituted Benzylideneacetophenones and Establishing their Structure Activity Relationship
Abstract Views :270 |
PDF Views:75
Authors
Deepak Chowrasia
1,
Nisha Sharma
1,
Ajay Kumar
1,
Vinod Dohrey
1,
Md. Arshad
2,
Asif Jafri
2,
Juhi Rais
2,
Madhu Gupta
2,
Sahabjada
2
Affiliations
1 University Institute of Pharmacy, Chhatrapati Shahu Ji Maharaj University, Kanpur 208 024, IN
2 Department of Zoology, Lucknow University, Lucknow 226 007, IN
1 University Institute of Pharmacy, Chhatrapati Shahu Ji Maharaj University, Kanpur 208 024, IN
2 Department of Zoology, Lucknow University, Lucknow 226 007, IN
Source
Current Science, Vol 114, No 02 (2018), Pagination: 391-396Abstract
We report here in-vitro antiproliferative and antibacterial activity of para-substituted benzylideneacetophenones and established their structure activity relationship to optimize para position as a biologically-oriented-synthetic target for design of small moleculebased future anticancer/antibacterial agents. Among synthesized compounds, 1c exhibits excellent antiproliferative activity against human osteosarcoma cell line (MG-63) compared to 1b and 1a suggesting dimethylamino (–N(CH3)2) functionality as a better para-substituted analogue for in-future anticancer agents. Similarly antibacterial screening of the aforesaid compounds against different strains of Gramnegative and Gram-positive bacteria reveals methoxy (–OCH3) rather than dimethylamino (–N(CH3)2) as a better para-substituted functionality on ring B comparatively. From our results, we justify our theory ‘lipophilicity affects antibacterial activity’.Keywords
Antiproliferative, Antibacterial Assay, Benzylideneacetophenone, MTT Assay.References
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- Ahmad, M. S., Sahabjada, Jafri, A., Ahmad, S., Afzal, M. and Arshad, M., Induction of apoptosis and antiproliferative activity of naringenin in human epidermoid carcinoma cell through ROS generation and cell cyle arrest. PLoS ONE, 2014, 9(10), e110003; doi:10.1371/journal.pone.0098409.
- Kaleem, S., Siddiqui, S., Hussain, A., Arshad, M., Akhtar, J., Rizvi, A. and Siddiqui, H. H., Eupalitin induces apoptosis in prostate carcinoma cells through ROS generation and increase of caspase3 activity. Cell Biol. Intern., 2016, 40(2), 196–203.
- Role of Interleukin-I Super Family in Progression of Osteoarthritis
Abstract Views :224 |
PDF Views:129
Authors
Amit Kumar
1,
Md Arshad
2,
Ajai Singh
3,
Asif Jafri
4,
Sabir Ali
5,
Manish Yadav
5,
Suchit Swaroop
1
Affiliations
1 Experimental and Public Health Laboratory, Department of Zoology, University of Lucknow, Lucknow – 226007, IN
2 Molecular Endocrinology Lab, Department of Zoology, University of Lucknow, Lucknow-226007, IN
3 Department of Orthopaedics, King George Medical University, Lucknow – 226003, IN
4 Molecular Endocrinology Lab, Department of Zoology, University of Lucknow, Lucknow – 226007, IN
5 Department of Orthopedics, King George Medical University, Lucknow – 226003, IN
1 Experimental and Public Health Laboratory, Department of Zoology, University of Lucknow, Lucknow – 226007, IN
2 Molecular Endocrinology Lab, Department of Zoology, University of Lucknow, Lucknow-226007, IN
3 Department of Orthopaedics, King George Medical University, Lucknow – 226003, IN
4 Molecular Endocrinology Lab, Department of Zoology, University of Lucknow, Lucknow – 226007, IN
5 Department of Orthopedics, King George Medical University, Lucknow – 226003, IN
Source
Journal of Ecophysiology and Occupational Health, Vol 17, No 1-2 (2017), Pagination: 9-16Abstract
Osteoarthritis (OA) is considered as multifactorial disorder characterized by erosion of articular cartilage, tightening of joint space, subchondral bone remodelling and internal synovial inflammation. OA reduces joint function progressively as a person gets older. The most important group of the cytokines or chemokines are pre-dominantly involving in the early progression of the disease includes IL-1, IL-6, IL-18 and TNF-a, etc. IL-1 family of cytokines are known to be strongest stimulus for progressive synthesis of Matrix Metallo Proteinases (MMPs). Large number of immune cells, chondrocytes and endothelial cells potentially secrete IL-1 with diverse effect on number of diseases. This review highlights the association of IL-1 family cytokine in OA.Keywords
Cytokine, IL-1 Family, Mode of Action, Osteoarthritis.- Antioxidant and Anti-Apoptotic Activities of Phytochemically Validated Fruit Extract of Solanum xanthocarpum in Primary Chondrocytes
Abstract Views :331 |
PDF Views:120
Authors
Neelam Shivnath
1,
Vineeta Rawat
1,
Sahabjada
1,
Asif Jafri
1,
Juhi Rais
1,
Habiba Khan
1,
Md. Arshad
1
Affiliations
1 Molecular Endocrinology Lab, Department of Zoology, University of Lucknow, Lucknow – 226007, Uttar Pradesh, IN
1 Molecular Endocrinology Lab, Department of Zoology, University of Lucknow, Lucknow – 226007, Uttar Pradesh, IN
Source
Journal of Ecophysiology and Occupational Health, Vol 18, No 3-4 (2018), Pagination: 106-116Abstract
The chondrocyte death may contribute in progression of osteoarthritis (OA). Solanum xanthocarpum (Family: Solanaceae) fruits were known for antioxidant activity. This study demonstrates that the phytochemically validated Solanum xanthocarpum fruits (SXF) extract has inhibitory activities on nitric oxide (NO) induced cell death and ROS formation in primary cultured chondrocytes. Chondrocyte death was induced by 1.5 mM of Sodium Nitroprusside (SNP). The Cell viability was measured by MTT assay and nuclear changes were observed by DAPI and Hoechst-PI. Antioxidant activity of SXF was demonstrated in H2O2 induced ROS generation in chondrocytes. Indomethacin (IM) (25μM), a NSAID was taken as positive control. Phytochemical analysis revealed the presence of flavonoids, anthraquinone glycosides, steroids, alkaloids, terpenoids and tannins. SXF significantly reduces the cell death induced by SNP in a dose dependent manner. The fluorescent photomicrograph of DAPI, Hoechst-PI and ROS also revealed the decreased rate of apoptosis in a dose-dependent manner. This study suggests that SXF shows anti-apoptotic and antioxidant activity in chondrocytesKeywords
Apoptosis, Chondrocytes, Non-Steroidal Anti-Inflammatory Drugs (NSAIDs), Osteoarthritis, Phytochemicals.References
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- Synthetic Modulation Including Structure Establishment, Antiproliferative Activity of Some p-Aryl Substituted (Z)-2-Cyanoethylideneacetohydrazides, and their Structure Activity Relationship
Abstract Views :229 |
PDF Views:81
Authors
Deepak Chowrasia
1,
Nisha Sharma
1,
Ajay Kumar
1,
Md Arshad
2,
Sahabjada Siddiqui
2,
Asif Jafri
2,
Juhi Rahis
2
Affiliations
1 University Institute of Pharmacy, Chhatrapati Shahu ji Maharaj (CSJM) University, Kalyanpur, Kanpur 208 024, IN
2 Department of Zoology, Lucknow University, Lucknow 226 007, IN
1 University Institute of Pharmacy, Chhatrapati Shahu ji Maharaj (CSJM) University, Kalyanpur, Kanpur 208 024, IN
2 Department of Zoology, Lucknow University, Lucknow 226 007, IN
Source
Current Science, Vol 115, No 12 (2018), Pagination: 2287-2290Abstract
A series of p-substituted aryl-2-cyanoethylideneacetohydrazides derivatives (2a-j) were successfully synthesized in the laboratory (yield 60–80%). The synthesized compounds were screened for their antiproliferative activity against MCF-7 (estrogen dependent human breast cancer cell line), SaOS-2 (osteosarcoma cell line), and K562 (myeloid leukemia cell line) by MTT (3-(4,5-dimethylthiazol-2-yl)-2,5- diphenyltetrazolium bromide) reduction assay. They showed moderate to mild antiproliferative activity, (2j) being the most potent in the series with an IC50 55, 64 and 35 μM against MCF-7, SaOS-2 and K562 cell lines, depict p-nitro as a better antiproliferative substituent comparatively. We have also tested the hypothesis – ‘Electron withdrawing phenomenon affects antiproliferative activity’.Keywords
Cancer, Cyanoacetohydrazide, Electron Withdrawing Ring Substituent, MTT Assay.References
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