硫异循环的多目标药理学:抗癌和抗氧化前景
Aliki Drakontaeidi1, Ilias Papanotas1, Eleni Pontiki1
1Department of Pharmaceutical Chemistry, School of Pharmacy, Faculty of Health Sciences, Aristotle University of Thessaloniki, 54124 Thessaloniki, Greece.
Antioxidants (Basel, Switzerland)
|August 29, 2024
概括
氧化应激通过破坏DNA并促进瘤生长来促进癌症. 新型硫异环化合物显示出双重抗氧化和抗癌作用的前景,提供新的治疗策略.
科学领域:
- 生物化学 生物化学
- 在瘤学瘤学.
- 药用化学 医学化学
背景情况:
- 由活性氧物种 (ROS) 驱动的氧化应激与癌症的发展和进展密切相关.
- 虽然ROS可以导致DNA损伤和破坏抗氧化防御,但癌细胞通常利用氧化环境促进生存和增殖.
- 现有的抗氧化剂疗法产生了不同的结果,突出了需要更有效的策略.
研究的目的:
- 探索氧化应激在癌症中的双重作用和新型治疗剂的潜力.
- 研究硫异环衍生物作为具有抗氧化和抗癌活性的多功能化合物.
- 了解结构修改,如基替代,如何影响这些双重性质.
主要方法:
- 关于氧化应激,癌症和抗氧化机制之间的相互作用的文献综述.
- 对瘤学中硫异环化合物的最新研究进行分析.
- 检查结构-活性关系,专注于基和电子吸收替代物在环上.
主要成果:
- 反应性氧物种 (ROS) 在癌症中起着双重作用,有助于瘤发生并使瘤存活.
- 硫异环衍生物正在研究其结合的抗氧化和抗癌作用.
- 基替代在环上增强了抗氧化活性,而电子吸收组,特别是在para位置,提高了抗癌潜力.
结论:
- 针对氧化应激和癌症之间的复杂关系需要创新的治疗方法.
- 多功能药物,如某些硫异环,为改善癌症治疗提供了有希望的途径,潜在的副作用更少.
- 战略性分子设计,包括特定的替代剂,对于优化新药候选药物的双抗氧化和抗癌疗效至关重要.
更多相关视频
相关概念视频
Electron Transport Chain: Complex I and II
12.3K
The mitochondrial electron transport chain (ETC) is the main energy generation system in the eukaryotic cells. However, mitochondria also produce cytotoxic reactive oxygen species (ROS) due to the large electron flow during oxidative phosphorylation. While Complex I is one of the primary sources of superoxide radicals, ROS production by Complex II is uncommon and may only be observed in cancer cells with mutated complexes.
ROS generation is regulated and maintained at moderate levels necessary...
ROS generation is regulated and maintained at moderate levels necessary...
12.3K
Targeted Cancer Therapies
7.5K
The targeted cancer therapies, also known as “molecular targeted therapies,” take advantage of the molecular and genetic differences between the cancer cells and the normal cells. It needs a thorough understanding of the cancer cells to develop drugs that can target specific molecular aspects that drive the growth, progression, and spread of cancer cells without affecting the growth and survival of other normal cells in the body.
There are several types of targeted therapies against...
There are several types of targeted therapies against...
7.5K
Combined Effects of Drugs: Synergism
3.8K
Synergism is a useful mechanism where combining two or more drugs is more effective than each constituent used alone. Such combinations are also called supra-additive interactions. The drugs collectively enhance the final therapeutic effect by acting on different targets. Another advantage is that the low dose of each constituent drug is sufficient to achieve the desired effect. This helps reduce the duration of therapy and lower the adverse effects of these drugs.
Such synergistic combinations...
Such synergistic combinations...
3.8K
Phase II Reactions: Sulfation and Conjugation with α-Amino Acids
190
Sulfation and α-amino acid conjugation are two critical biotransformation reactions in drug metabolism. Sulfation, a phase II biotransformation reaction, involves adding a polar sulfate group to a drug, enhancing its water solubility and promoting excretion. This process can either co-occur with or occur independently of glucuronidation. Nonmicrosomal sulfotransferase enzymes catalyze the process. The reaction involves 3'-phosphoadenosine-5'-phosphosulfate or PAPS coenzyme...
190
Drugs that Stabilize Microtubules
2.0K
Microtubules are dynamic structures that undergo cycles of catastrophe and rescue. The microtubules play a central role in cell division by forming the spindle apparatus for segregating the chromosomes. This makes them ideal targets for regulating dividing cells in tumors and malignant cancer cells. Microtubule stabilizing drugs help stabilize the microtubule formation and promote its polymerization. Paclitaxel was the first microtubule stabilizing agent used as anticancer drug in chemotherapy...
2.0K
Phase II Reactions: Miscellaneous Conjugation Reactions
48
Phase II biotransformations are detoxification mechanisms that conjugate xenobiotics with endogenous substances, neutralizing their toxicity.
A key example involves the conjugation of cyanide ions, which impair cellular respiration and alter hemoglobin into non-oxygen-carrying cyanmethemoglobin. To neutralize this threat, a sulfur atom from thiosulphate is transferred to the cyanide ion, catalyzed by the enzyme rhodanese, resulting in an inactive compound called thiocyanate. The production of...
A key example involves the conjugation of cyanide ions, which impair cellular respiration and alter hemoglobin into non-oxygen-carrying cyanmethemoglobin. To neutralize this threat, a sulfur atom from thiosulphate is transferred to the cyanide ion, catalyzed by the enzyme rhodanese, resulting in an inactive compound called thiocyanate. The production of...
48


![Cercosporin-Photocatalyzed [4+1]- and [4+2]-Annulations of Azoalkenes Under Mild Conditions](/_next/image?url=https%3A%2F%2Fcloudfront.jove.com%2FCDNSource%2Fteasers%2F60786.jpg&w=3840&q=50)