Evaluation Of Plasma Concentrations Of Boswellic Acids In Fasting Healthy Human Subjects Supplemented With A Test Product AquaLOX (Standardized To 78% AKBA) In Comparison With A Reference Product 5-LoxinÂ® (Standardized To 30% AKBA)

开始日期2017-12-26

申办/合作机构

Laila Nutraceuticals Pvt Ltd.

100 项与 AKBA (Shanghai Jiaotong University) 相关的临床结果

登录后查看更多信息

100 项与 AKBA (Shanghai Jiaotong University) 相关的转化医学

登录后查看更多信息

100 项与 AKBA (Shanghai Jiaotong University) 相关的专利（医药）

登录后查看更多信息

274

项与 AKBA (Shanghai Jiaotong University) 相关的文献（医药）

2024-10-01·Journal of Ethnopharmacology

Protection effect of Dioscoreae Rhizoma against ethanol-induced gastric injury in vitro and in vivo: A phytochemical and pharmacological study

Article

作者: Fan, Xinxin ; Ma, Yajie ; An, Luyao ; Li, Renshi ; Xie, Yujun ; Bayoude, Alamusi ; Wang, Xiaoyan ; Yu, Boyang

ETHNOPHARMACOLOGICAL RELEVANCEDioscoreae Rhizoma, a kind of Chinese yam, is a medicinal and edible plant used in China for strengthening the spleen and stomach. However, there is a lack of modern pharmacology studies regarding its anti-gastric injury activity.AIM OF THE STUDYThis study aimed to investigate the phytochemical composition of Chinese yam aqueous extract (CYW) and evaluate its gastroprotective effects against ethanol-induced gastric injury in vitro and in vivo.MATERIALS AND METHODSThe active components of CYW were identified using HPLC-QTOF-MS/MS in combination with the GNPS molecular networking and network pharmacology. In vitro studies were performed in the RAW264.7/GES-1 cell coculture system. In vivo study, mice were treated with CYW (0.31, 0.63, and 3.14 g/kg BW, orally) for 14 days, followed by a single oral dose of ethanol (10 mL/kg BW) to induce gastric injury. The biochemical, inflammation and oxidative stress markers were analyzed using commercial kits. Histopathology was used to assess the degree of gastric injury. Gene and protein expressions were studied using RT-qPCR and western blotting, respectively.RESULTSCYW significantly restored the levels of SOD, GPx and CAT, and reduced the MDA content. Further analyses showed that CYW significantly alleviated the gastric oxidative stress by inhibiting the inflammation via decreasing p-NF-κB and p-IκB-α expression levels and inhibiting the generation of IL-6, TNF-α, and IL-1β. At the same time, the fraction remarkably upregulated Bcl-2, downregulated Bax and increased growth factor secretion, thereby prevented gastric mucous cell. Besides, The combination of HPLC-QTOF-MS/MS, GNPS molecular networking analysis, and network pharmacology demonstrated that linoleic acid, 3-acetyl-11-keto-beta-boswellic acid, adenosine, aminocaproic acid, tyramine, DL-tryptophan, cycloleucine, lactulose, melibiose, alpha-beta-trehalose, and sucrose would be the main active compounds of CYW against ethanol-induced gastric injury.CONCLUSIONThis study showed that CYW is potentially rich source of anti-oxidant and anti-inflammatory bioactive compounds. It showed efficacy against ethanol-induced gastric injury by inhibiting inflammation, oxidative stress, and apoptosis in the stomach. The results of the current work indicate that Dioscoreae Rhizoma could be utilized as a type of natural resource for production of new medicine and functional foods to prevent and/or ameliorate ethanol-induced gastric injury.

2024-09-01·Phytomedicine

Single-dose comparative pharmacokinetic/pharmacodynamic study of a micellar formulation versus a native Boswellia serrata dry extract in healthy volunteers

Article

作者: Ulrich, Judith ; Zolk, Oliver ; Abdel-Kahaar, Emaad ; Duweb, Amira ; Pfeiffer, Maximilian ; Schmiech, Michael ; Syrovets, Tatiana ; Simmet, Thomas

BACKGROUNDExtracts of oleogum resins of Boswellia trees possess anti-inflammatory activities. Micellar formulations have been developed to increase the oral bioavailability of bioactive boswellic and lupeolic acids.PURPOSEThe current single-dose crossover clinical trial compares for the first time pharmacokinetics/pharmacodynamics of two Boswellia serrata nutraceuticals, native Biotikon® BS-85 and micellar Boswellia-Loges®.METHODSAfter oral administration of the study preparations (800 mg) to 20 healthy volunteers, plasma concentrations of 8 boswellic and lupeolic acids were measured by using HPLC-MS/MS for up to 48 h Blood samples collected 2 and 5 h after drug administration were stimulated for 24 h with endotoxic lipopolysaccharide. The release of proinflammatory cytokines analyzed by flow cytometry was used as readout of the pharmacodynamic properties of the preparations.REGISTRATIONGerman Clinical Trials Register (DRKS) No. DRKS00027369.RESULTSAdministration of the micellar extract significantly increased C_max, AUC_0-48, and shortened T_max for all boswellic and lupeolic acids compared to native extract. Accordingly, their relative bioavailability increased to 1,720-4,291 % with the highest difference for acetyl-11-keto-β-boswellic acid (AKBA). Both preparations reduced the release of TNF-α and the native formulation diminished also IL-1β and IL-6. However, no significant differences were observed between the preparations, except for a higher decrease in IL-1β by the native formulation Biotikon® BS-85. In a lymphocytic gene reporter cell line, both nutraceuticals similarly inhibited the NF-κB transcription factor activity as well as the TNF-α release, yet the native formulation Biotikon®BS-85 was more efficient in inhibiting TNF-α.CONCLUSIONAdministration of the micellar Boswellia serrata nutraceutical increased the oral bioavailability of boswellic and lupeolic acids. Yet, the increase in plasma concentration did not enhance the anti-inflammatory efficacy of the micellar extract compared to the native extract in this ex vivo model.

2024-08-31·Cureus

Interactions of Acetyl-11-Keto-Beta-Boswellic Acid on Catechol-O-Methyltransferase in the Management of Masticatory Myofascial Pain Syndrome

Article

作者: Yadalam, Pradeep Kumar ; Ramalingam, Karthikeyan ; Ramadoss, Ramya ; Suresh, Ramya ; Muthukrishnan, Arvind

BACKGROUNDMasticatory myofascial pain syndrome (MMPS) is a soft tissue inflammatory disorder that leads to acute or chronic localized pain and stiffness in the muscles. Catechol-O-methyltransferase (COMT) plays a crucial role in mediating pain perceptions in humans by transferring methyl groups to catecholamines. This process requires adequate S-adenosyl methionine (SAMe). A reduction in SAMe leads to COMT inhibition. Boswellia serrata possesses multiple therapeutic benefits and is used for treating chronic pain.AIMThe study aimed to evaluate the therapeutic potential of acetyl-11-keto-beta-boswellic acid (AKBA) by targeting COMT. Methodology: Molecular docking and dynamic simulations were conducted using Desmond software from Schrödinger LLC, USA, to evaluate the interaction between COMT protein and AKBA ligands. The COMT protein structure was sourced from the Protein Data Bank and preprocessed using optimized potentials for liquid simulations. Molecular docking identified potential binding sites between COMT and AKBA through hydrogen bonding, resulting in a docking score of -6.0 kcal/mol.RESULTSThe molecular docking revealed a docking score of -6.0 kcal/mol for the interaction between COMT and AKBA. The dynamic simulation demonstrated that the COMT-AKBA complex remained stable within a 3.0 Angstrom range over 60 nanoseconds. These findings indicate stable natural small molecular interactions between COMT and AKBA.CONCLUSIONAKBA exhibits potential as a therapeutic agent for MMPS, demonstrating stable interactions with COMT. These findings warrant further in vitro and in vivo analyses to confirm efficacy.

100 项与 AKBA (Shanghai Jiaotong University) 相关的药物交易

登录后查看更多信息

研发状态

10 条进展最快的记录,

后查看更多信息

适应症	最高研发状态	国家/地区	公司	日期
学习障碍	临床前	伊朗	Mashhad University of Medical Sciences	2024-01-01
记忆障碍	临床前	伊朗	Mashhad University of Medical Sciences	2024-01-01
银屑病	临床前	中国	上海交通大学	-