Arockiya Anita Margret, R Mareeswari, K Arun Kumar, Arockiya Avila Jerley
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引用次数: 0
摘要
抑郁症是一种精神疾病,被认为是全球性的威胁。它被指定为疾病负担。因此,迫切需要改善抗抑郁药的治疗效果。印度有很大一部分(双孢蘑菇和平菇)是非致幻剂吲哚化合物的重要来源。氨基酸l -色氨酸和5-羟色氨酸(5-HTP)是血清素的前体。5-羟色胺是一种潜在的抗抑郁药,它可以高速率穿过血脑屏障(BBB),并更有效地转化为血清素。由于被称为渗透性糖蛋白(P-gp)的外排泵受体的刺激,通过这一封锁的药物递送仍然是一个挑战。本研究报道了一种比较植物化学分析方法,并利用高效液相色谱法分析了两种食用菌有机提取物的非致幻色氨酸代谢物。通过体外和计算机研究,洗脱的化合物的功效被证实为P-gp抑制剂。从香菇的甲醇和乙醇提取物中得到4种衍生物:5-羟基- l -色氨酸(5HTR)、5-羟基色胺(5-HT)、l -色氨酸(L-Trp)和色胺(TA)。针对P-gp(最低能量分别为-64.38 kcal/mol和-83.93 kcal/mol)的体外和分子对接研究证实了蘑菇衍生代谢物促进药物在大脑中的传递的能力。本研究证实,含有非致幻代谢物的蘑菇可以作为精神活性营养品,对促进精神健康有重要意义。这些蘑菇具有很高的治疗效果,可以作为理想的神经系统药物,导致精神疾病的强化治疗。
Relative profiling of L-tryptophan derivatives from selected edible mushrooms as psychoactive nutraceuticals to inhibit P-glycoprotein: a paradigm to contest blood-brain barrier.
Depression is a mental illness and is considered to be a global threat. It is designated as burden of disease. There is therefore an intense need to improve the therapeutic response of antidepressants. India beholds a wide fraction (Agaricus bisporus and Pleurotus ostreatus ) as a vital source of non-hallucinogenic indole compounds. The amino acids L-tryptophan and 5-hydroxytryptophan (5-HTP) are precursors of serotonin. 5-HTP is a potential antidepressant that can cross the blood-brain barrier (BBB) at a high rate and is converted into serotonin more efficiently. Drug delivery across this blockade remains a challenge due to the stimulation of efflux pump receptors called permeability glycoprotein (P-gp). This work reports a comparative phytochemical assay and profiling of non-hallucinogenic tryptophan metabolites using HPLC from two organic extracts of edible mushrooms. The efficacy of the eluted compounds was authenticated as P-gp inhibitors with in vitro and in silico studies. The following four derivatives were obtained from the methanol and ethanol extracts of the mushrooms: 5-hydroxy-L-tryptophan (5HTR), 5-hydroxy tryptamine (5-HT), L-tryptophan (L-Trp), and tryptamine (TA). In vitro and molecular docking studies targeting P-gp (minimum energy: -64.38 and -83.93 kcal/mol, respectively) substantiated the ability of mushroom-derived metabolites to facilitate drug delivery in the brain. This study verified that mushrooms containing non-hallucinogenic metabolites can act as psychoactive nutraceuticals that are significant for enhancing mental health. The high therapeutic efficacy, these mushrooms can serve as ideal neurological drug leads to fortify treatment for mental illness.
BioTechnologiaAgricultural and Biological Sciences-Plant Science
CiteScore
1.60
自引率
0.00%
发文量
8
审稿时长
8 weeks
期刊介绍:
BIOTECHNOLOGIA – a high standard, peer-reviewed, quarterly magazine, providing a medium for the rapid publication of research reports and review articles on novel and innovative aspects of biotechnology, computational biology and bionanotechnology.