Bergaptol (5-hydroxypsoralen or 5-hydroxyfuranocoumarin) is a naturally occurring furanocoumarin widely found in citrus fruits, which has multiple health benefits. Nonetheless, no specific review articles on bergaptol have been published. Compiling updated information on bergaptol is crucial in guiding future research direction and application. The present review focuses on the research evidence related to the pharmacological properties and toxicity of bergaptol. Bergaptol has anti-inflammatory, antioxidant, anti-cancer, anti-osteoporosis, anti-microbial, and anti-lipidemic effects. It can inhibit the activities of cytochrome P450s (CYP), especially CYP2C9 and CYP3A4, thereby affecting the metabolism and concentrations of some drugs and toxins. Compared with other coumarins, bergaptol has the least potency to inhibit CYP3A4 in cancer cells. Instead, it can suppress drug efflux transporters, such as P-glycoprotein, thereby overcoming chemotherapeutic drug resistance. Furthermore, bergaptol has antimicrobial effects with a high potential for inhibition of quorum sensing. In vivo, bergaptol can be retained in plasma for longer than other coumarins. Nevertheless, its toxicity has not been clearly reported. In vitro study suggests that, unlike most furocoumarins, bergaptol is not phototoxic or photomutagenic. Existing research on bergaptol has mostly been conducted in vitro. Further in vivo and clinical studies are warranted to identify the safe and effective doses of bergaptol for its multimodal application.

中文翻译：

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佛手柑醇，柑橘中的主要呋喃香豆素：药理特性和毒性

Bergaptol（5-羟基补骨脂素或 5-羟基呋喃香豆素）是一种天然存在的呋喃香豆素，广泛存在于柑橘类水果中，具有多种健康益处。尽管如此，尚未发表有关香柠檬醇的具体评论文章。收集香柠檬醇的最新信息对于指导未来的研究方向和应用至关重要。本综述重点关注与香柠檬醇药理特性和毒性相关的研究证据。 Bergaptol 具有抗炎、抗氧化、抗癌、抗骨质疏松、抗菌和抗血脂作用。它可以抑制细胞色素P450s（CYP），特别是CYP2C9和CYP3A4的活性，从而影响一些药物和毒素的代谢和浓度。与其他香豆素类相比，香柠檬醇抑制癌细胞中 CYP3A4 的效力最小。相反，它可以抑制药物外流转运蛋白，例如 P-糖蛋白，从而克服化疗耐药性。此外，香柠檬醇具有抗菌作用，并且具有很高的抑制群体感应的潜力。在体内，香柠檬醇在血浆中的保留时间比其他香豆素更长。然而，其毒性尚未明确报道。体外研究表明，与大多数呋喃香豆素不同，香柠檬醇不具有光毒性或光致突变性。现有的香柠檬醇研究大多是在体外进行的。需要进一步的体内和临床研究来确定香柠檬醇的多模式应用的安全有效剂量。