Transport of glycinin, the major soybean allergen, across intestinal epithelial IPEC ‐J2 cell monolayers
The objective of this study was to elucidate the pathway and mechanism of glycinin hydrolysate transport through the intestinal epithelial barrier using IPEC-J2 cell model. Purified glycinin was digested by in vitro static digestion model. The pathway and mechanism of glycinin hydrolysates transport through intestinal epithelial cells were investigated by cellular transcytosis assay, cellul ar uptake assay, immunoelectron microscopy and endocytosis inhibition assay. The glycinin hydrolysates were transported across IPEC-J2 cell monolayers in a time/dose-dependent manner following the Michaelis equation. Immunoelectron mi...
Source: Journal of Animal Physiology and Animal Nutrition - May 1, 2024 Category: Zoology Authors: Ziang Zheng,
Yintong Zhao,
Shugui Zheng,
Yajin Liu,
Simiao Liu,
Junfeng Han Tags: ORIGINAL ARTICLE Source Type: research
Design, synthesis, and biological evaluation of novel 2,3-Di-O-Aryl/Alkyl sulfonate derivatives of l-ascorbic acid: Efficient access to novel anticancer agents via in vitro screening, tubulin polymerization inhibition, molecular docking study and ADME predictions
Bioorg Chem. 2024 Apr 26;147:107402. doi: 10.1016/j.bioorg.2024.107402. Online ahead of print.ABSTRACTA series of novel l-ascorbic acid derivatives bearing aryl and alkyl sulfonate substituents were synthesized and characterized. In vitro anticancer evaluation against MCF-7 (breast) and A-549 (lung) cancer cell lines revealed potent activity for most of the compounds, with 2b being equipotent to the standard drug colchicine against MCF-7 (IC50 = 0.04 μM). Notably, compound 2b displayed 89-fold selectivity for MCF-7 breast cancer over MCF-10A normal breast cells. Derivatives with two sulfonate groups (2a-g, 3a-g) exhibited...
Source: Bioorganic Chemistry - April 30, 2024 Category: Chemistry Authors: Santosh R Deshmukh Archana S Nalkar Aniket P Sarkate Shailee V Tiwari Deepak K Lokwani Shankar R Thopate Source Type: research
Design, synthesis, and biological evaluation of novel 2,3-Di-O-Aryl/Alkyl sulfonate derivatives of l-ascorbic acid: Efficient access to novel anticancer agents via in vitro screening, tubulin polymerization inhibition, molecular docking study and ADME predictions
Bioorg Chem. 2024 Apr 26;147:107402. doi: 10.1016/j.bioorg.2024.107402. Online ahead of print.ABSTRACTA series of novel l-ascorbic acid derivatives bearing aryl and alkyl sulfonate substituents were synthesized and characterized. In vitro anticancer evaluation against MCF-7 (breast) and A-549 (lung) cancer cell lines revealed potent activity for most of the compounds, with 2b being equipotent to the standard drug colchicine against MCF-7 (IC50 = 0.04 μM). Notably, compound 2b displayed 89-fold selectivity for MCF-7 breast cancer over MCF-10A normal breast cells. Derivatives with two sulfonate groups (2a-g, 3a-g) exhibited...
Source: Bioorganic Chemistry - April 30, 2024 Category: Chemistry Authors: Santosh R Deshmukh Archana S Nalkar Aniket P Sarkate Shailee V Tiwari Deepak K Lokwani Shankar R Thopate Source Type: research
Efficacy and safety of colchicine for the treatment of myopericarditis
Conclusion
In patients with first attack of pericarditis associated with myocardial involvement, colchicine was safe and efficacious for the reduction of recurrences. (Source: Heart)
Source: Heart - April 25, 2024 Category: Cardiology Authors: Collini, V., De Martino, M., Andreis, A., De Biasio, M., Gaspard, F., Paneva, E., Tomat, M., Deferrari, G. M., Isola, M., Imazio, M. Tags: Open access, Editor's choice Special populations Source Type: research
The effect of colchicine on cancer risk in patients with immune-mediated inflammatory diseases: a time-dependent study based on the Taiwan ’s National Health Insurance Research Database
ConclusionColchicine was associated with the lower aHR of the all cancer and colorectal cancer formation in patients with the IMIDs. (Source: European Journal of Medical Research)
Source: European Journal of Medical Research - April 22, 2024 Category: Research Source Type: research
Efficacy and safety of colchicine for atrial fibrillation prevention: An updated meta-analysis of randomized controlled trials
Atrial fibrillation (AF), the most common arrhythmia, is closely related to inflammation. Colchicine has the potent anti-inflammatory effects. Several randomized clinical trials (RCTs) have evaluated the efficacy and safety of colchicine in the prevention of AF but the results are inconsistent. (Source: International Journal of Cardiology)
Source: International Journal of Cardiology - April 20, 2024 Category: Cardiology Authors: Xu Tian, Nan Zhang, Panagiotis Korantzopoulos, George Bazoukis, Konstantinos P. Letsas, Gary Tse, Tong Liu Source Type: research
The role of colchicine in the management of COVID-19: a Meta-analysis
The Coronavirus disease 2019 (COVID-19) pandemic has robustly affected the global healthcare and economic systems and it was caused by coronavirus-2 (SARS-CoV-2). The clinical presentation of the disease range... (Source: BMC Pulmonary Medicine)
Source: BMC Pulmonary Medicine - April 20, 2024 Category: Respiratory Medicine Authors: Kholoud Elshiwy, Ghada Essam El-Din Amin, Mohamed Nazmy Farres, Rasha Samir and Mohamed Farouk Allam Tags: Research Source Type: research
Colchicine for the treatment of patients with COVID-19: an updated systematic review and meta-analysis of randomised controlled trials
Conclusions
The results of this meta-analysis do not support the use of colchicine as a treatment for reducing the risk of mortality or improving other relevant clinical outcomes in patients with COVID-19. However, RCTs investigating early treatment with colchicine (within 5 days of symptom onset or in patients with early-stage disease) are needed to fully elucidate the potential benefits of colchicine in this patient population.
PROSPERO registration number
CRD42022369850. (Source: BMJ Open)
Source: BMJ Open - April 17, 2024 Category: General Medicine Authors: Cheema, H. A., Jafar, U., Shahid, A., Masood, W., Usman, M., Hermis, A. H., Naseem, M. A., Sahra, S., Sah, R., Lee, K. Y. Tags: Open access, Infectious diseases, COVID-19 Source Type: research
Colchicine in atherosclerotic cardiovascular disease
In conclusion, while colchicine shows promise in reducing MACE, its net risk–benefit profile requires further elucidation before its widespread adoption into clinical practice for the secondary prevention of atherosclerotic cardiovascular disease. Much more large-scale, long-term trial data are still needed in this space. (Source: Heart)
Source: Heart - April 15, 2024 Category: Cardiology Authors: Tucker, B., Goonetilleke, N., Patel, S., Keech, A. Tags: Review articles Reviews Source Type: research
Modification of the phenyl ring B of phenyl 4-(2-oxoimidazolidin-1-yl)benzenesulfonates by pyridinyl moiety leads to novel antimitotics targeting the colchicine-binding site
Bioorg Med Chem Lett. 2024 Apr 11:129745. doi: 10.1016/j.bmcl.2024.129745. Online ahead of print.ABSTRACTA series of 8 novel pyridinyl 4-(2-oxoimidazolidin-1-yl)benzenesulfonates (PYRIB-SOs) were designed, prepared and evaluated for their mechanism of action. PYRIB-SOs were found to have antiproliferative activity in the nanomolar to submicromolar range on several breast cancer cell lines. Moreover, subsequent biofunctional assays indicated that the most potent PYRIB-SOs 1-3 act as antimitotics binding to the colchicine-binding site (C-BS) of α, β-tubulin and that they arrest the cell cycle progression in the G2/M phase....
Source: Bioorganic and Medicinal Chemistry Letters - April 13, 2024 Category: Chemistry Authors: Vincent Ouellette Chahrazed Bouzriba Atziri Corin Chavez Alvarez Genevi ève Hamel-Côté S ébastien Fortin Source Type: research
Low-dose colchicine for atherosclerosis: long-term safety
Eur Heart J. 2024 Apr 10:ehae208. doi: 10.1093/eurheartj/ehae208. Online ahead of print.ABSTRACTLow-dose colchicine (0.5 mg daily) is now FDA-approved for secondary prevention in patients with coronary disease and will be increasingly prescribed in clinical practice. In this State-of-the-Art Review, data were collated from contemporary systemic reviews of case reports, drug registries, and placebo-controlled trials that assessed specific issues of safety related to the continuous use of colchicine in a range of clinical settings to inform physicians, pharmacists, and patients of the absolute risks of continuous use of low-...
Source: Atherosclerosis - April 10, 2024 Category: Cardiology Authors: Stefan Mark Nidorf Eldad Ben-Chetrit Paul M Ridker Source Type: research
Low-dose colchicine for atherosclerosis: long-term safety
Eur Heart J. 2024 Apr 10:ehae208. doi: 10.1093/eurheartj/ehae208. Online ahead of print.ABSTRACTLow-dose colchicine (0.5 mg daily) is now FDA-approved for secondary prevention in patients with coronary disease and will be increasingly prescribed in clinical practice. In this State-of-the-Art Review, data were collated from contemporary systemic reviews of case reports, drug registries, and placebo-controlled trials that assessed specific issues of safety related to the continuous use of colchicine in a range of clinical settings to inform physicians, pharmacists, and patients of the absolute risks of continuous use of low-...
Source: Atherosclerosis - April 10, 2024 Category: Cardiology Authors: Stefan Mark Nidorf Eldad Ben-Chetrit Paul M Ridker Source Type: research
Design and synthesis of novel imidazole-chalcone derivatives as microtubule protein polymerization inhibitors to treat cervical cancer and reverse cisplatin resistance
Bioorg Chem. 2024 Apr 4;147:107310. doi: 10.1016/j.bioorg.2024.107310. Online ahead of print.ABSTRACTUsing the licochalcone moiety as a lead compound scaffold, 16 novel imidazole-chalcone derivatives were designed and synthesized as microtubule protein polymerization inhibitors. The proliferation inhibitory activities of the derivatives against SiHa (human cervical squamous cell carcinoma), C-33A (human cervical cancer), HeLa (human cervical cancer), HeLa/DDP (cisplatin-resistant human cervical cancer), and H8 (human cervical epithelial immortalized) cells were evaluated. Compound 5a exhibited significant anticancer activi...
Source: Bioorganic Chemistry - April 7, 2024 Category: Chemistry Authors: Zhengye Liu Zheng Yang Mourboul Ablise Source Type: research
Design and synthesis of novel imidazole-chalcone derivatives as microtubule protein polymerization inhibitors to treat cervical cancer and reverse cisplatin resistance
Bioorg Chem. 2024 Apr 4;147:107310. doi: 10.1016/j.bioorg.2024.107310. Online ahead of print.ABSTRACTUsing the licochalcone moiety as a lead compound scaffold, 16 novel imidazole-chalcone derivatives were designed and synthesized as microtubule protein polymerization inhibitors. The proliferation inhibitory activities of the derivatives against SiHa (human cervical squamous cell carcinoma), C-33A (human cervical cancer), HeLa (human cervical cancer), HeLa/DDP (cisplatin-resistant human cervical cancer), and H8 (human cervical epithelial immortalized) cells were evaluated. Compound 5a exhibited significant anticancer activi...
Source: Bioorganic Chemistry - April 7, 2024 Category: Chemistry Authors: Zhengye Liu Zheng Yang Mourboul Ablise Source Type: research
Colchicine for the Prevention of Cardiovascular Disease: Potential Global Implementation
Curr Cardiol Rep. 2024 Apr 4. doi: 10.1007/s11886-024-02049-y. Online ahead of print.ABSTRACTPURPOSE OF REVIEW: Targeting traditional cardiovascular risk factors is effective in reducing recurrent cardiovascular events, yet the presence of residual cardiovascular risk due to underlying systemic inflammation is a largely unaddressed opportunity. This review aims to comprehensively assess the evolving role of colchicine as a therapeutic approach targeting residual inflammatory risk in the context of those with coronary artery disease (CAD).RECENT FINDINGS: Inflammation plays a significant role in promoting atherosclerosis, a...
Source: Atherosclerosis - April 4, 2024 Category: Cardiology Authors: Robert S Zhang Brittany N Weber Diego Araiza-Garaygordobil Michael S Garshick Source Type: research
