IL-17A inhibitors(Interleukin 17A inhibitors), NF-κB inhibitors(Nuclear factor NF-kappa-B complex inhibitors), TNF-α inhibitors(Tumor necrosis factor α inhibitors)

Therapeutic Areas

Digestive System Disorders

Active Indication

Colitis, Ulcerative

Inactive Indication-

Originator Organization

Guangzhou Magpie Pharmaceuticals Co., Ltd.

Active Organization

Guangzhou Magpie Pharmaceuticals Co., Ltd.

Inactive Organization-

Drug Highest PhaseIND Application

First Approval Date-

Regulation-

Structure

Molecular FormulaC19H22O5

InChIKeyIZOBIZVXEKNCNN-ZNQIEUMMSA-N

CAS Registry126455-04-7

100 Clinical Results associated with AL-1

100 Translational Medicine associated with AL-1

100 Patents (Medical) associated with AL-1

Literatures (Medical) associated with AL-1

01 Sep 2024·Asian Journal of Neurosurgery

Comparative Efficacy of Intracuff 1% and 2% Alkalinized Lignocaine with Saline on Endotracheal Tube-Induced Hemodynamic Changes and Emergence Phenomena in Neurosurgical Patients

Article

Author: Mudgal, Pratibha ; Talwar, Vandana ; Mounisha, Elugoti

Abstract Introduction Extubation is associated with hemodynamic changes and emergence phenomena leading to cough, sore throat, dysphonia, and dysphagia in the postoperative period. The aim of our study was to compare intracuff 2% alkalinized lignocaine with 1% alkalinized lignocaine and saline in reducing endotracheal tube induced emergence phenomena and haemodynamic changes at extubation in neurosurgical patients. Materials and Methods In this randomized controlled study, 90 adult patients of either sex, scheduled to undergo neurosurgical procedures were randomly divided into three groups of 30 each to receive either 1% alkalinized lignocaine (AL1), 2% alkalinized lignocaine (AL2), or saline as cuff inflation media. Intracuff pressures and haemodynamic variables were noted intraoperatively and during emergence. The presence of postextubation cough, sore throat, dysphonia, and dysphagia were monitored until 24 hours postoperatively. Data were analyzed using Chi-square test and ANOVA. A p-value of less than 0.05 was considered significant. Results The intracuff pressures were significantly less with alkalinized lignocaine as compared to saline, after 3 hours of induction. Post extubation, hemodynamic parameters and incidence of coughing and bucking at extubation were significantly less in Groups AL1 (p = 0.024) and AL2 (p = 0.02) as compared to saline. On assessment of laryngotracheal morbidity, the incidence of coughing was found to be significantly less with 2% alkalinized lignocaine as compared to saline (p = 0.021) at 1 hour after extubation. Sore throat was significantly less in Groups AL1 and AL2 as compared with saline at 1 hour (p = 0.008, 0.002 respectively) and 8 hours (p = 0.01 in both groups), and in Group AL2 versus saline at 24 hours (p = 0.044) after extubation. The incidence of dysphonia was significantly less in Groups AL1 and AL2 as compared with saline at 1 hour (p = 0.016, p = 0.002) and 24 hours (p = 0.012 in both groups) and in Group AL2 versus saline at 8 hours (p = 0.03) postoperatively. No significant differences were noted between 1% alkalinized lignocaine and 2% alkalinized lignocaine. Conclusion Intracuff alkalinized lignocaine 1% and 2% were significantly better than saline in reducing coughing and bucking at extubation, post extubation haemodynamic changes and incidence of postoperative cough, sore throat, and dysphonia.

21 May 2024·Applied and Environmental Microbiology

Polysaccharide intercellular adhesin and proper phospholipid composition are important for aggregation in Tetragenococcus halophilus SL10

Article

Author: Mogi, Yoshinobu ; Wakinaka, Takura ; Watanabe, Jun ; Kobayashi, Kurumi ; Matsue, Kouta ; Yanagihara, Airi

ABSTRACT Aggregating strains of Tetragenococcus halophilus tend to be trapped during soy sauce mash-pressing process and are, therefore, critical for clear soy sauce production. However, the precise molecular mechanism involved in T. halophilus aggregation remains elusive. In previous studies, we isolated a number of aggregating strains, including T. halophilus AB4 and AL1, and showed that a cell surface proteinaceous aggregation factor is responsible for their aggregation phenotype. In the present study, we explored the role of polysaccharide intercellular adhesin (PIA) in aggregate formation in T. halophilus SL10, isolated from soy sauce. SL10 exhibited similar aggregation to AB4 and AL1 but formed a non-uniform precipitate with distinctive wrinkles at the bottom of the test tube, unlike AB4 and AL1. Insertion sequence mutations in each gene of the ica operon diminished aggregation and PIA production, highlighting the critical role of IcaADBC-mediated PIA production in T. halophilus aggregation. Furthermore, two non-aggregating cardiolipin synthase ( cls ) gene mutants with intact ica operon did not produce detectable PIA. Phospholipid composition analysis in cls mutants revealed a decrease in cardiolipin and an increase in phosphatidylglycerol levels, highlighting the association between phospholipid composition and PIA production. These findings provide evidence for the pivotal role of cls in PIA-mediated aggregation and lay the foundation for future studies to understand the intricate networks of the multiple aggregation factors governing microbial aggregation. IMPORTANCE Aggregation, commonly observed in various microbes, triggers biofilm formation in pathogenic variants and plays a beneficial role in efficient food production in those used for food production. Here, we showed that Tetragenococcus halophilus , a microorganism used in soy sauce fermentation, forms aggregates in a polysaccharide intercellular adhesin (PIA)-mediated manner. Additionally, we unveiled the relationship between phospholipid composition and PIA production. This study provides evidence for the presence of aggregation factors in T. halophilus other than the proteinaceous aggregation factor and suggests that further understanding of the coordinated action of these factors may improve clarified soy sauce production.

01 Aug 2022·Current Pharmaceutical Design

Andrographolide Derivative AL-1 Ameliorates LPS-induced Acute Lung Injury by Inhibiting NLRP3 Inflammasome and Lung Permeability

Article

Author: Yu, Pei ; Zhang, Chu ; Wei, Yuke ; Wang, Yuqiang ; Li, Tangjia ; Xu, Lipeng ; Shan, Luchen ; Zhong, Haijing

Background:Acute lung injury (ALI) is a serious respiratory disease with a high mortality rate, and there is an urgent need for a more effective treatment strategy. Andrographolide derivative AL-1 has been identified to possess anti-inflammatory activity. However, whether it could reduce LPS-induced lung injury in mice through inhibiting NLRP3 inflammasome activation and protecting lung permeability has not yet been elucidated. In the present research, we investigated the protective effect of AL-1 on ALI mice and demonstrated the potential mechanisms.Methods:Male Balb/c mice were anesthetized with isoflurane, and ALI mice were induced by intratracheal instillation of LPS. The mice were euthanized after LPS administration for 12 h, then bronchoalveolar lavage fluid (BALF) and lung tissues were collected. The levels of inflammatory factors were measured by ELISA assay, and HE staining and lung injury scoring were used to evaluate the pathological changes in the pulmonary tissues. Immunohistochemistry and immunofluorescence examination were conducted to detect the expression levels of related proteins. Western blot was performed to measure the levels of NLRP3 inflammasome and tight junction proteins.Results:The study indicated that AL-1 effectively alleviated lung injury by reduction of proinflammatory cytokine levels, MPO activity, lung W/D ratio, and total protein levels. Furthermore, AL-1 improved pathological changes in lung tissue and significantly reduced the infiltration of inflammatory cells. Administration with AL-1 markedly inhibited the expression of NLRP3, ASC, Caspase-1, IL-1β, gasdermin D (GSDMD), and VCAM-1 but increased the expression of ZO-1, Occludin, JAM-A, and Claudin-1.Conclusion:Taken together, these results demonstrated that AL-1 ameliorated pulmonary damage by inhibiting the activation of the NLRP3 inflammasome pathway and restoring TJ protein expression.

100 Deals associated with AL-1

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Indication	Highest Phase	Country/Location	Organization	Date
Colitis, Ulcerative	IND Application	CN	Guangzhou Magpie Pharmaceuticals Co., Ltd.	19 Feb 2024

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