相关实验视频
Updated: Jun 15, 2025

08:36
Scaled-Up Preparation of an Intermediate of Upatinib, ACT051-3
Published on: April 7, 2023
1.0K
利用UPO的多功能性,将鲁丁转化为更容易溶解和生物活性产品
Abel Muñiz-Mouro1, Beatriz Gullón2, Gemma Eibes1
1CRETUS, Department of Chemical Engineering, Universidade de Santiago de Compostela, 15782 Santiago de Compostela, Galicia, Spain.
New biotechnology
|August 24, 2024
概括
非特异性过氧酶 (UPO) 修改了天然的抗氧化剂 rutin,产生了更可溶和生物活性的产品. 研究了酶的可重复使用性,在恢复过程中面临稳定性挑战.
科学领域:
- 生物催化剂是一种生物催化剂.
- 酶学 是一种酶学.
- 自然产品的修改自然产品的修改
背景情况:
- 非特异性过氧激酶 (UPO) 提供了基于酶的多功能氧功能化.
- UPOs可以修改天然抗氧化剂,生产高价值产品.
- 鲁丁是一种天然的黄类抗氧化剂,是UPO修饰的潜在基质.
研究的目的:
- 为了研究由Agrocybe aegerita UPO.Agrocybe aegerita UPO.Agrocybe aegerita UPO.Agrocybe aegerita UPO.Agrocybe UPO.Agrocybe aegerita UPO.Agrocybe aegerita UPO.Agrocybe aegerita UPO.Agrocybe UPO.Agrocybe UPO.Agrocybe aegerita UPO.Agrocybe aegerita UPO.Agrocybe aegerita UPO.Agrocybe UPO.Agrocybe UPO.Agrocybe aegerita UPO.Agrocybe aegerita UPO.Agrocybe aegerita UPO.Agrocybe aegerita UPO.Agrocybe aegerita UPO.Agrocybe UPO.Agrocybe UPO.Agrocybe UPO.Agrocybe
- 优化基于UPO的鲁丁修饰以提高溶解度和生物活性.
- 评估UPO在酶膜反应器中的可重复使用性和稳定性.
主要方法:
- 使用来自Agrocybe aegerita的UPO对鲁丁的酶修饰.
- 反应条件的多变量优化.
- 酶膜反应器用于酶回收和可重复使用性评估.
- 调查 Askorbic 酸对产品形状的影响.
主要成果:
- 通过过氧化和/或过氧化,然后通过寡合化,UPO成功修改了鲁丁.
- 优化旨在最大限度地提高可溶性抗氧化剂的生产,同时保持酶活性.
- 在膜反应器的过阶段发现了酶稳定性问题.
- 亚酸促进了氧化鲁丁衍生物的形成,增加了溶解性和生物活性.
结论:
- 通过UPO介导的鲁丁修饰产生更容易溶解和潜在的更多生物活性化合物.
- 酶的可重复使用性在恢复过程中提出了与酶稳定性相关的挑战.
- 需要进一步的研究来克服工业应用的酶稳定性限制.
相关概念视频
Drug Biotransformation: Overview
2.4K
Pharmaceutical substances known as xenobiotics are predominantly lipophilic and nonionized. This enables them to permeate lipid bilayers, such as cell membranes, and interact with intracellular target receptors. Lipophilic drugs have an advantage in crossing biological barriers and reaching their intended sites of action. However, lipophilic drugs often have a restricted capacity for renal expulsion or elimination from the body. When these drugs enter the kidneys and undergo glomerular...
2.4K
Phase II Reactions: Glucuronidation
326
Glucuronidation, a pivotal phase II biotransformation process, involves the coupling of glucuronic acid to a drug or xenobiotic. Given its widespread occurrence and critical role in drug metabolism, it's considered the most crucial phase II reaction. It enhances the water solubility of substances, aiding their expulsion from the body. The driving force behind these reactions is a group of enzymes known as UDP-glucuronosyltransferases (UGTs). UGTs facilitate the transfer of a glucuronic acid...
326
Phase I Oxidative Reactions: Overview
251
Phase I biotransformation, or functionalization, is a crucial chemical process that converts drugs and other xenobiotics into more water-soluble forms, facilitating expulsion from the body. It involves oxidative, reductive, and hydrolytic reactions that add or unveil polar functional groups on lipophilic substrates. Key players in phase I reactions are the mixed-function oxidases. Situated in liver cell microsomes, these enzymes predominantly carry out drug metabolism. They require molecular...
251
Prodrugs
2.6K
Prodrugs are a class of pharmaceutical compounds that undergo a biotransformation process within the body to be converted into a pharmacologically active drug. Prodrugs are designed to improve the therapeutic properties of the parent drug, such as enhancing bioavailability, increasing stability, or reducing toxicity. The concept of prodrugs revolves around modifying the chemical structure of the original drug to make it more effective or convenient for administration.
Prodrugs help overcome...
Prodrugs help overcome...
2.6K
Drug Metabolism: Phase II Reactions
3.7K
Phase II reactions are essential for the detoxification and elimination of drugs from the body. These reactions involve the conjugation of parent drugs or their phase I metabolites with endogenous molecules, resulting in more hydrophilic drug conjugates. The primary conjugation reactions in this phase are sulfation and glucuronidation. Both sulfation and glucuronidation typically produce biologically inactive metabolites. However, in some cases involving prodrugs, active metabolites may be...
3.7K
Factors Affecting Dissolution: Drug Permeability, Stability and Stereochemistry
179
Orally administered drugs primarily enter the systemic circulation via passive diffusion through the intestinal membranes. The drug's absorption is influenced by drug stability in the gastrointestinal GI tract, membrane permeability, the surface area available for absorption, luminal drug concentration, and residence time in the lumen. Drug permeability can be enhanced by adjusting the lipophilicity, polarity, or molecular size of the drug, promoting its passive transport across intestinal...
179

