Atherosclerosis, a cardiovascular disease, is at the top of the list among the diseases leading to death. Although the biochemical and pathophysiological cascades involved within the development of atherosclerosis have been identified clearly, its nature is quite complex to be treated with a single agent targeting a pathway. Therefore, many natural and synthetic compounds have been suggested for the treatment of the disease. The majority of the drugs employed target one of the single components of the pathological outcomes, resulting in many times less effective and longterm treatments. In most cases, treatment options prevent further worsening of the symptoms rather than a radical treatment. Consequently, the current review has been prepared to focus on the validated and non-validated targets of atherosclerosis as well as the alternative treatment options such as hydroxymethyl glutaryl coenzyme A (HMG-CoA) reductase inhibitors, acyl-CoA cholesterol acyl transferase (ACAT) inhibitors, lipoprotein lipase stimulants, bile acid sequestrants, and some antioxidants. Related to the topic, both synthetic compounds designed employing medicinal chemistry skills and natural molecules becoming more popular in drug development are scrutinized in this mini review.

动脉粥样硬化是一种心血管疾病，在导致死亡的各种疾病中名列前茅。尽管已经清楚地确定了动脉粥样硬化发展过程中涉及的生化和病理生理学级联，但是其性质相当复杂，要用靶向该途径的单一药物进行治疗。因此，已经提出了许多天然和合成的化合物来治疗该疾病。所用的大多数药物针对的是病理结果的单一组成部分之一，导致长期有效的治疗效果降低了很多倍。在大多数情况下，治疗选择可以防止症状进一步恶化，而不是进行彻底治疗。最后，当前的审查已经准备好集中于动脉粥样硬化的有效靶标和非有效靶标以及其他治疗选择，例如羟甲基戊二酰辅酶A（HMG-CoA）还原酶抑制剂，酰基-CoA胆固醇酰基转移酶（ACAT）抑制剂，脂蛋白脂肪酶刺激剂，胆汁酸螯合剂和一些抗氧化剂。与此主题相关的是，在本微型评论中对使用药物化学技能设计的合成化合物和在药物开发中变得越来越流行的天然分子进行了详细审查。