酸性溶剂在体外改善了西斯的作用
1Department of Computational Biology, St. Jude Children's Research Hospital, Memphis, TN, 38105, USA.
Biochemical and biophysical research communications
|April 19, 2024
概括
硫酸二甲基-盐酸 (DMSO-HCl) 提供了一个稳定的替代方案,用于溶解晶在体外,保持药物的疗效不同于传统的方法. 这一进步有助于癌症研究,改善了西斯的处理和组合疗法.
科学领域:
- 在瘤学瘤学.
- 药理学 药理学是指药理学的学科.
- 生物化学 生物化学
背景情况:
- 西斯是一种重要的化疗剂,在体外和体内进行了广泛的研究.
- 目前用于准备用于体外测试的西斯溶液的方法,例如使用二甲基硫氧化物 (DMSO) 或正常盐水 (NS),存在重大缺点,包括药物活性降低,不稳定性和溶解性问题.
- 这些局限性使研究工作复杂化,旨在了解西斯的作用机制,减轻其毒性,并开发新的药物组合.
研究的目的:
- 引入和验证一种新的溶剂系统,用于在体外制备西斯.
- 为了解决与当前西斯胺溶解方法相关的局限性,特别是不稳定性和有效性降低.
- 提供一种更可靠,更稳定的方法,用于在体外癌症研究,涉及西斯.
主要方法:
- 一种新的溶剂混合物,二甲基硫氧化-盐酸 (DMSO-HCl) 被制备并用于溶解西斯.
- 在DMSO-HCl中溶解的西斯的稳定性和药物活性被评估并与在正常盐水中溶解的西斯相比较.
- 评估了cisplatin在DMSO-HCl中与其他DMSO溶解化合物的兼容性.
主要成果:
- 在DMSO-HCl中溶解的西斯丁显示出与在NS中溶解的西斯丁相似的药物活性.
- 与NS相比,DMSO-HCl中的西斯在延长的储存期内表现出更好的稳定性.
- 该DMSO-HCl溶剂系统缓解了与西斯普拉丁不稳定性,有限溶解度和组合药物配方并发症相关的问题.
结论:
- DMSO-HCl混合物代表了一种优质的替代溶剂,用于制备用于体外癌症研究的西斯普拉丁溶液.
- 这种新方法增强了西斯的稳定性,并保持了药物的疗效,克服了现有协议的关键局限性.
- 这些发现为优化基于的体外研究提供了宝贵的见解,并促进了结合癌症疗法的开发.
相关概念视频
02:11Leveling Effect and Non-Aqueous Acid-Base Solutions
8.2K
This lesson defines the leveling effect in acidic and basic solutions and its role in aqueous and non-aqueous solutions. It is essential to understand the competing nature of various species in a chemical system.
The Leveling Effect of a Solvent
A generic acid (HA) reacts with the generic base (B-) to yield the corresponding conjugate base (A-) and conjugate acid (HB):
The Leveling Effect of a Solvent
A generic acid (HA) reacts with the generic base (B-) to yield the corresponding conjugate base (A-) and conjugate acid (HB):
8.2K
01:22Electrophilic Aromatic Substitution: Sulfonation of Benzene
6.5K
Sulfonation of benzene is a reaction wherein benzene is treated with fuming sulfuric acid at room temperature to produce benzenesulfonic acid. Fuming sulfuric acid is a mixture of sulfur trioxide and concentrated sulfuric acid.
6.5K
00:53Extraction: Effects of pH
1.4K
Consider a neutral form of an amine, B, with a partition coefficient, K, in a liquid mixture containing organic and aqueous phases. The pH of the aqueous phase affects the charge on acidic and basic solutes, and the charged form is usually more soluble in the aqueous phase. Suppose the conjugate acid form of the amine is soluble only in the aqueous phase while the base form is soluble in both phases. Then the distribution coefficient, D, can be given as the ratio of amine concentration in the...
1.4K
01:26Enhanced Elimination of Poison
1.1K
Poison can be effectively removed from the gastrointestinal (GI) tract through various decontamination procedures.
Antidotes serve a crucial role in counteracting the effects of poison by inhibiting enzymes responsible for producing harmful drug metabolites. In some cases, these toxic metabolites can be neutralized by endogenous cosubstrates, which are maintained at specific concentrations to prevent interaction with cellular macromolecules and subsequent cell death.
Renal excretion is the...
Antidotes serve a crucial role in counteracting the effects of poison by inhibiting enzymes responsible for producing harmful drug metabolites. In some cases, these toxic metabolites can be neutralized by endogenous cosubstrates, which are maintained at specific concentrations to prevent interaction with cellular macromolecules and subsequent cell death.
Renal excretion is the...
1.1K
01:25Acid-Base Balance
2.5K
The human body maintains a narrow pH range regulated through acid-base balance. This balance is crucial as changes in the hydrogen ion concentration can disrupt cell membrane stability, alter protein structures, and change enzyme activities. The normal pH of arterial blood is 7.4, venous blood and interstitial fluid is 7.35, and intracellular fluid averages 7.0.
When the pH of arterial blood rises above 7.45, it results in a condition called alkalosis. Conversely, a drop below 7.35 leads to...
When the pH of arterial blood rises above 7.45, it results in a condition called alkalosis. Conversely, a drop below 7.35 leads to...
2.5K
01:29Leveling Effect
1.6K
In acid-base chemistry, the leveling effect refers to the limitation imposed by the solvent on the strength of acids and bases in solution. When a base stronger than the solvent's conjugate base is used, it deprotonates the solvent until the base is entirely consumed, making it ineffective against weaker acids. Conversely, an acid stronger than the solvent's conjugate acid protonates the solvent until the acid is depleted, rendering it ineffective against weaker bases. Essentially, the...
1.6K