Metadicholandreg; a Novel Sialidase Inhibitor

R. Pr, S. Yogisha, S. Anand, Purushotham Gv
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Abstract

Humans face a constant threat from pathogens like influenza varieties H1N1, H5N1, and others and there is a need to prevent these from epidemics. The pathogens depend on successful colonization of the host in order to reproduce and multiply. Sialidases are known as neuraminidases are a group of enzymes, the most abundant of these being the exo-sialidases that can catalyze the cleavage of sialic acids from carbohydrates, glycoproteins or glycolipids. Sialidases have been thoroughly studied since their discovery 75 years ago and their occurrence in bacteria and viruses is widespread. They are found in diverse virus families and bacteria and other microbes. Moreover, sialic acids serve as a receptor for various pathogens. This allows bacteria like H1N1 or other influenza viruses, to enter the host cell. There is a need to block sialidases as they release sialic acid that serves as nutrition for the microbes and as well allows them to bind and invade the host cell where they can proliferate. This makes sialidases an interesting target to control pathogenic activity. Metadichol® is nanoemulsion of long-chain lipid alcohols derived from food ingredients. In rats, it has an LD50 of 5000 mg/kilo and its ingredients are present in many foods we consume on a daily basis. It has antiviral and antibacterial and anti-parasitic properties. We studied inhibition of Sialidases by inducing it with Lipopolysaccharide (LPS) using THP1 cells. Metadichol showed inhibition at 1 picogram per ml to 1 nanogram per/ml. Compared to Prednisone. It is 100 times more active. Previous studies on Metadichol® showed that it is toxic to cancer cells at higher concentrations. Since it is safer, it has the potential of being directly tested on humans without side effects and could have a potential role in mitigating the pathogens that a burden on the Public health system.
Metadicholandreg;一种新型唾液酸酯酶抑制剂
人类面临着来自流感变种H1N1、H5N1和其他病原体的持续威胁,有必要防止这些病原体流行。病原体依靠宿主的成功定植来繁殖和繁殖。唾液酸酶被称为神经氨酸酶,是一组酶,其中最丰富的是外源性唾液酸酶,它可以催化从碳水化合物、糖蛋白或糖脂中裂解唾液酸。自75年前发现唾液酸酶以来,人们对其进行了深入的研究,它们在细菌和病毒中广泛存在。它们存在于不同的病毒科、细菌和其他微生物中。此外,唾液酸可作为多种病原体的受体。这使得像H1N1或其他流感病毒这样的细菌能够进入宿主细胞。有必要阻断唾液酸酶,因为它们释放唾液酸,为微生物提供营养,也允许它们结合并侵入宿主细胞,在那里它们可以增殖。这使得唾液酸酶成为控制致病活性的一个有趣的靶点。Metadichol®是从食品原料中提取的长链脂质醇纳米乳液。在大鼠中,它的LD50为5000毫克/公斤,我们每天食用的许多食物中都含有它的成分。它具有抗病毒、抗菌和抗寄生虫的特性。我们研究了脂多糖(LPS)诱导THP1细胞抑制唾液酸酶的作用。元二醇表现出1微克/毫升至1纳克/毫升的抑制作用。与强的松相比。它的活性是原来的100倍。先前对Metadichol®的研究表明,高浓度的Metadichol对癌细胞是有毒的。由于它更安全,它有可能在没有副作用的情况下直接在人体上进行测试,并可能在减轻对公共卫生系统造成负担的病原体方面发挥潜在作用。
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