Neochlorogenic acid: an anti-HIV active compound identified by screening of Cortex Mori [Morus Alba L. (Moraceae)]

Abstract

Context

Chinese herbs such as Cortex Mori [Morus alba L. (Moraceae)] may inhibit human immunodeficiency virus (HIV), but active compounds are unknown.

Objective

Screening of Cortex Mori and other herbs for anti-HIV active compounds.

Materials and methods

HIV-1 virus (multiplicity of infection: 20), and herbs (dissolved in dimethyl sulfoxide, working concentrations: 10, 1, and 0.1 mg/mL) such as Cortex Mori, etc., were added to 786-O cells (10⁵ cell/well). Zidovudine was used as a positive control. Cell survival and viral inhibition rates were measured. The herb that was the closest inactivity to zidovudine was screened. Mass spectrometry identified the active compounds in herbs (mobile phase: 0.05% formic acid aqueous solution and acetonitrile, gradient elution, detection wavelength: 210 nm). The effect of the compounds on reverse transcriptase (RT) products were evaluated by real-time PCR. Gene enrichment was used to analyse underlying mechanisms.

Results

With a dose of 1 mg/mL of Cortex Mori, the cell survival rate (57.94%) and viral inhibition rate (74.95%) were closest to the effect of zidovudine (87.87%, 79.81%, respectively). Neochlorogenic acid, one of the active ingredients, was identified by mass spectrometry in Cortex Mori. PCR discovery total RT products of neochlorogenic acid group (mean relative gene expression: 6.01) significantly inhibited (control: 35.42, p < 0.0001). Enrichment analysis showed that neochlorogenic acid may act on haemopoietic cell kinase, epidermal growth factor receptor, sarcoma, etc., thus inhibiting HIV-1 infection.

Conclusions

For people of low socioeconomic status affected by HIV, Chinese medicine (such as Cortex Mori) has many advantages: it is inexpensive and does not easily produce resistance. Drugs based on active ingredients may be developed and could have important value.

Keywords:

• Traditional Chinese medicine
• reverse transcriptase
• enrichment analysis

Acknowledgments

We thank International Science Editing (http://www.internationalscienceediting.com) for editing this manuscript.

Disclosure statement

No potential conflict of interest was reported by the author(s).

Data availability statement

The relevant data have been uploaded as supplementary and can also be obtained from the corresponding author.

Additional information

Funding

This work was supported by the National Science and Technology Program during the Twelfth Five-year Plan Period (grant number: 2012ZX10005001-005), the Chongqing Postdoctoral Science Foundation (grant number: Xm2017089), and the Natural Science Foundation Project of Chongqing, Chongqing Science and Technology Commission (grant numbers: Cstc2018jcyjAX0723 and Cstc2018jcyjAX0732).