Icariside compound, preparation method thereof, and application thereof

Abstract

An icariside compound as shown in Formula I wherein the compound is a natural chemical component in the traditional Chinese herbal epimedium or a chemically modified or a totally synthetic product based on the natural component. The compound can be used for preparing pharmaceuticals, health care products, cosmetic and skin care products and the like for improvement of immunity in a human body.

Description

REFERENCE TO RELATED APPLICATION[0001]This application claims the priority of Chinese patent application No. 201510264195.5 “ICARISIDe COMPOUND, PREPARATION METHOD THEREOF, AND APPLICATION THEREOF” filed on May 20, 2015, hereby incorporated by reference in its entirety.BACKGROUND[0002]Human immunity refers to the ability of the body to protect against causative factors outside or within host cells from infection or invasion, i.e. the ability of the body to maintain a normal and stable environment within the body. In the environments where people live, air, water, food, and most items we contact in daily life, for example, contains a variety of harmful microorganisms such as bacteria, viruses, mycoplasma, chlamydia, fungi and other pathogens (causative factors outside a host cell). Human body may also be affected by the environmental changes, the emergence of a latent virus or bacteria in the host cell, or infection or invasion of cancer cells produced by gene mutation and the like (...

AI Technical Summary

Benefits of technology

[0021]The present invention proves by toxicology research that icariside I and icariside C have low toxicity and side effects (DC50>2 g / kg body weight) which is safe for use.

[0022]In addition, all the results and achievements of the present invention are based on the very effective screening model established by the present inventors. Therefore, a further objective of the present invention is to provide an experimental model for screening substances having impacts (either enhance or inhibit) on immunity. Small molecular compounds having the effect of improving or inhibiting human immunity were screened out by the model by applying exogenous antigens to stimulate human peripheral blood mononuclear cells (PBMCs) to produce cytokine IFN-γ, adding the pharmaceuticals to be tested to the mixed system of exogenous antigens and PBMCs, and measuring the effect on production level of IFN-γ. Specifically, the method prepared human peripheral blood mononuclear cells (PBMCs) by isolation from fresh blood collected from healthy people. Then the exogenous antigens for example monoclonal stimulatory molecules Anti-CD3, Anti-CD3 / Anti-CD28, PBMCs from different people, or human cells infectively stimulated by other causative factors (e.g. viruses, bacteria and cancer cells) were applied for stimulation. The peripheral blood mononuclear cells, after the above stimulation, produced new cytokine IFN-γ. Then the pharmaceuticals to be tested (compounds to be screened) were added at different concentrations in a gradient and well-mixed. The PBMCs after completion of stimulation were seeded and cultured in a 96-well mini round bottom plates and were incubated in 5% CO2 at 37° C. in an incubator. Finally, by using ELISA techniques, the levels of IFN-γ produced in the culture were measured at different incubation time. Increased level of produced IFN-γ indicates that the tested compound has the effect of improving the immunity. On the other hand, decreased level of produced IFN-γ indicates that the tested compound has the effect of inhibiting human immunity. Thus, the present method can also be used to screen small molecular compounds having an effect of inhibiting human immunity, i.e. immune inhibitor.

Problems solved by technology

When the immunity (antibodies or cytokines etc.) produced by human immune system is not sufficient to fight against the disease causative factors, people get sick.

However, these are specific for certain diseases which greatly limit their applications.

In addition, they are easy to be degraded which have a short half-life and poor bioavailability and which are difficult to be large-scale synthesized, separated and purified.

So far, attempts to find small molecular compounds with good effects on enhancing immunity are not yet successful.

However, systematic studies on the separation of active components therein are rare, in particular that on icariside I and icariside C due to their extremely low content (while its homologue, icariin, has higher content) leading to difficulty in conducting an effective research, let alone industrial application.

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