در هنگام جستجو کلمه در قسمت عنوان میتوانید کلمات مورد جستجو را با کاراکتر (-) جدا کنید.
کاربرد نوع شرط:
- جایگاه : پژوهشی
- مجله: Iranian Journal of Basic Medical Sciences
- نوع مقاله: Journal Article
- کلمات کلیدی: Molecular docking,Anti-diarrheal,Manilkara zapota,Anti-secretory,Anti-spasmodic,Anti-ulcer
- چکیده:
- چکیده انگلیسی: Objective(s): This study was designed to investigate various gastrointestinal effects of Manilkara zapota (Sapodilla), exploring its anti-diarrheal, anti-secretary, anti-spasmodic, anti-ulcer and anti-motility potential.
Materials and Methods: Antidiarrheal and anti-secretary activities were investigated using castor oil induced diarrhea and castor oil induced fluid accumulation. Isolated rabbit jejunum tissues (antispasmodic) were employed for in vitro experiments. Antiulcer, antimotility and molecular docking were performed using ethanol-HCl induced ulcer assay, charcoal meal transit time and Auto Doc Vina.
Results: Mz.Cr exhibited protection against castor oil-induced diarrhea (P<0.05 vs. saline group) and dose-dependently inhibited intestinal fluid secretions (P<0.001 vs. castor oil group). Mz.Cr caused relaxation of spontaneous and K+ (80 Mm)-induced contractions with EC50 values of 0.11mg/ml (0.08-0.1, n=4) and 0.16 mg/ml (0.09-0.2, n=4) respectively (*P<0.05**P<0.01 ***P<0.001). It showed protective effect against gastric ulcers induced by ethanol-HCl (P<0.001 vs. saline group). Mz.Cr reduced distance travelled by charcoal meal (P<0.001 vs. saline group). Plant constituents: caffeoylquinic acid and methyl 4-O-galloylchlorogenate showed high binding affinities (E-value≥-6.5 Kcal/mol) against histaminergic H2 receptors, H+/K+ ATPase pump and voltage gated L-type calcium channels, while possesses moderate affinities (E-value≥8 Kcal/mol) against histaminergic H1, muscarinic M1, M3 and mu-opioid, whereas lower affinities (E-value≥9.5 Kcal/mol) vs. calmodulin, adrenergic α1, phosphodiesterase enzyme and dopaminergic D2 receptors. Lupeol-3-acetate and β-amyrin-3-(3’-dimethyl) butyrate observed weak affinities.
Conclusion: In present study, M. zapota is reported to exhibits anti-diarrheal, anti-secretory, anti-spasmodic, anti-motility, anti-ulcer effects and computational binding affinities against gastrointestinal targets.- انتشار مقاله: 24-07-1397
- نویسندگان: Muhammad Bilal Riaz,Arif-ullah Khan,Neelam Gul Qazi
- مشاهده
- جایگاه : پژوهشی
- مجله: Iranian Journal of Basic Medical Sciences
- نوع مقاله: Journal Article
- کلمات کلیدی: Molecular docking,Anti-diarrheal,Manilkara zapota,Anti-secretory,Anti-spasmodic,Anti-ulcer
- چکیده:
- چکیده انگلیسی: Objective(s): This study was designed to investigate various gastrointestinal effects of Manilkara zapota (Sapodilla), exploring its anti-diarrheal, anti-secretary, anti-spasmodic, anti-ulcer and anti-motility potential.
Materials and Methods: Antidiarrheal and anti-secretary activities were investigated using castor oil induced diarrhea and castor oil induced fluid accumulation. Isolated rabbit jejunum tissues (antispasmodic) were employed for in vitro experiments. Antiulcer, antimotility and molecular docking were performed using ethanol-HCl induced ulcer assay, charcoal meal transit time and Auto Doc Vina.
Results: Mz.Cr exhibited protection against castor oil-induced diarrhea (P<0.05 vs. saline group) and dose-dependently inhibited intestinal fluid secretions (P<0.001 vs. castor oil group). Mz.Cr caused relaxation of spontaneous and K+ (80 Mm)-induced contractions with EC50 values of 0.11mg/ml (0.08-0.1, n=4) and 0.16 mg/ml (0.09-0.2, n=4) respectively (*P<0.05**P<0.01 ***P<0.001). It showed protective effect against gastric ulcers induced by ethanol-HCl (P<0.001 vs. saline group). Mz.Cr reduced distance travelled by charcoal meal (P<0.001 vs. saline group). Plant constituents: caffeoylquinic acid and methyl 4-O-galloylchlorogenate showed high binding affinities (E-value≥-6.5 Kcal/mol) against histaminergic H2 receptors, H+/K+ ATPase pump and voltage gated L-type calcium channels, while possesses moderate affinities (E-value≥8 Kcal/mol) against histaminergic H1, muscarinic M1, M3 and mu-opioid, whereas lower affinities (E-value≥9.5 Kcal/mol) vs. calmodulin, adrenergic α1, phosphodiesterase enzyme and dopaminergic D2 receptors. Lupeol-3-acetate and β-amyrin-3-(3’-dimethyl) butyrate observed weak affinities.
Conclusion: In present study, M. zapota is reported to exhibits anti-diarrheal, anti-secretory, anti-spasmodic, anti-motility, anti-ulcer effects and computational binding affinities against gastrointestinal targets.- انتشار مقاله: 24-07-1397
- نویسندگان: Muhammad Bilal Riaz,Arif-ullah Khan,Neelam Gul Qazi
- مشاهده
- جایگاه : پژوهشی
- مجله: Asian Pacific Journal of Cancer Prevention
- نوع مقاله: Journal Article
- کلمات کلیدی: Thymoquinone (TQ),FASN,Her-2,Cyclophosphamide (Cyclo)
- چکیده:
- چکیده انگلیسی: Objective: Cancer chemotherapy at the recommended doses is largely associated with toxicity, and also it is not
effective enough to reduce the advancement of the disease at lower doses. Thymoquinone (TQ) is an active compound
derived from black seeds (Nigella sativa) which exhibits anticancer activities. The aim of the present study was to
investigate the synergistic effect of TQ alone and in combination with cyclophosphamide (cyclo), and to unravel the
role of TQ in fatty acid synthase (FASN) mediated molecular signaling in Her2 + and Her2- breast cancer cell lines.
Methods: The effect of TQ on the growth of Her2+ SKBR-3 and Her2- MDA-231 breast cancer lines were evaluated
as percent cell viability by cytotoxicity-based MTT assay. The analysis of cell cycle arrest was done through flowcytometry
followed by Western blot and RT-PCR to detect signaling events in the cells. Results: The data showed
that TQ-cyclo (0.5mM-10μM) combination significantly inhibited the proliferation through the 5.49% and 57.72%
accumulation of cells in sub-G1 and G1 respectively as 12% cells were shifted from G2/M phase in Her2+ breast cancer
cells. Similarly, TQ-cyclo (0.5mM-20μM) combination exhibited that the 16.6% cells were arrested in Sub-G1 and only
3.54% cells were remained in G2/M phase as it was 22.89% in DMSO control in Her-2- breast cancers cells. Though
TQ alone or in combination with cyclo alleviated the PI3K/Akt signaling by downregulating the phosphorylation of Akt
and upregulating the PTEN, no changes was observed in FASN and Her-2 as well in both type of cells. The significant
decreased expression of cyclin D1 was found in TQ-cyclo combinations. Conclusion: The current findings suggested
that TQ can alter the cell cycle progression and induce cell death independent of FASN mediated signaling. In terms of
clinical perspective, the present study clearly showed that TQ can broadly augment the effect of cyclo in breast cancer
cases irrespective of Her-2+ or Her-.- انتشار مقاله: 08-07-1397
- نویسندگان: Arif Khan,Yousef H Aldebasy,Sultan A Alsuhaibani,Masood A Khan
- مشاهده