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

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.

The endocrine disruptor hexachlorobenzene can cause oxidative damage in the testis of mice.

Hexachlorobenzene is a widespread endocrine disruptor. However, the effect of hexachlorobenzene on the reproductive toxicity of male animals is not described in detail. To investigate the toxic effects of hexachlorobenzene in mouse testes, hexachlorobenzene (100, 400 and 1,600 mg/kg) is fed to mice. The morphology of the testes was analysed by haematoxylin and eosin staining. We also investigated the expression of biomarkers for oxidative stress. Database screening identified proteins that interact with hexachlorobenzene and the aryl hydrocarbon receptor, a weak ligand of hexachlorobenzene. Gene enrichment analysis and protein-protein interaction analyses were also performed. Real-time PCR detected the expression levels of the aryl hydrocarbon receptor in four different stages of testicular cells. We identified significantly increased activity levels of superoxide dismutase (p < 0.05) and catalase (p < 0.05) in mouse testes that had been subjected to oxidative damage. The cell thickness and the number of cell layers in the seminiferous tubules had decreased by varying degrees after the hexachlorobenzene treatment. Particularly, cytokines and proteins involved in transcriptional regulation showed enrichment. The highest levels of aryl hydrocarbon receptor expression were detected in the spermatocytic cell line. Hexachlorobenzene exposure caused testicular damage in mice. The toxicity characteristics of hexachlorobenzene were not dose-dependent.

Therapeutic effects of Sheng Xue Fang in a cyclophosphamide-induced anaemia mouse model.

CONTEXT: Sheng Xue Fang (SXF) has been used to treat anaemia for decades with good efficacy. OBJECTIVE: To study the effect and possible mechanism of SXF to restore haematopoietic function. MATERIALS AND METHODS: Balb/c mice (10 per/group, half male, half female) were treated with SXF (three dose groups, 8.5, 17, and 22.1 g/kg) by gavage for 14 days, and cyclophosphamide (80 mg/kg) was injected on days 10-12. Only injection of cyclophosphamide (negative control) or physiological saline (blank control) were included as controls. The spleen and femur were processed for histopathology. Active components and the target of SXF were screened. The target was used for gene enrichment and protein-protein interaction (PPI) analysis. RESULTS: Red blood cell relative changes in the SXF group (low: -5.50 ± 1.58%; medium: -11.11 ± 4.15%; high: -8.81 ± 2.67%) and relative negative control (26.21 ± 2.51%) significantly increased (all p < 0.01) in female mice. Haemoglobin and red blood cell-specific volume showed the same trend. However, SXF did not have significant effects on male mice. Splenic index in the medium group (4.44 ± 0.46%) relative negative control (3.38 ± 0.10%) significantly improved (p < 0.01) in female mice. Using network pharmacology, 77 active components and 337 targets were screened from SXF. These targets are closely related to the mitogen-activated protein kinase pathway. CONCLUSIONS: SXF has good clinical application potential. However, the mechanism requires in-depth research. Our findings are of great significance in anaemia treatment and provide a new perspective for Chinese medicine research.