Exploration in the Mechanism of Ginsenoside Rg5 for the Treatment of Osteosarcoma by Network Pharmacology and Molecular Docking.

OBJECTIVE: Osteosarcoma is a primary malignancy originating from mesenchymal tissue characterized by rapid growth, early metastasis and poor prognosis. Ginsenoside Rg5 (G-Rg5) is a minor ginsenoside extracted from Panax ginseng C.A. Meyer which has been discovered to possess anti-tumor properties. The objective of current study was to explore the mechanism of G-Rg5 in the treatment of osteosarcoma by network pharmacology and molecular docking technology. METHODS: Pharmmapper, SwissTargetPrediction and similarity ensemble approach databases were used to obtain the pharmacological targets of G-Rg5. Related genes of osteosarcoma were searched for in the GeneCards, OMIM and DrugBank databases. The targets of G-Rg5 and the related genes of osteosarcoma were intersected to obtain the potential target genes of G-Rg5 in the treatment of osteosarccoma. The STRING database and Cytoscape 3.8.2 software were used to construct the protein-protein interaction (PPI) network, and the Database for Annotation, Visualization and Integrated Discovery (DAVID) platform was used to perform gene ontology (GO) and Kyoto Encyclopedia of Genes and Genomes (KEGG) pathway enrichment analyses. AutoDock vina software was used to perform molecular docking between G-Rg5 and hub targets. The hub genes were imported into the Kaplan-Meier Plotter online database for survival analysis. RESULTS: A total of 61 overlapping targets were obtained. The related signaling pathways mainly included PI3K-Akt signaling pathway, Proteoglycans in cancer, Lipid and atherosclerosis and Kaposi sarcoma-associated herpesvirus infection. Six hub targets including PIK3CA, SRC, TP53, MAPK1, EGFR, and VEGFA were obtained through PPI network and targets-pathways network analyses. The results of molecular docking showed that the binding energies were all less than -7 kcal/mol. And the results of survival analysis showed TP53 and VEGFA affect the prognosis of sarcoma patients. CONCLUSION: This study explored the possible mechanism of G-Rg5 in the treatment of osteosarcoma using network pharmacology method, suggesting that G-Rg5 has the characteristics of multi-targets and multi-pathways in the treatment of osteosarcoma, which lays a foundation for the follow-up experimental and clinical researches on the therapeutic effects of G-Rg5 on osteosarcoma.

Insight into the pharmacological effects of andrographolide in musculoskeletal disorders.

Andrographis paniculata (A. paniculata) is a traditional herbal medicine that has been widely used in Asian countries for hundreds of years. Andrographolide (AG) is a diterpene lactone extracted from A. paniculata. Owing to the in-depth study of pharmacological mechanisms, the therapeutic potential of AG, including its anti-inflammatory, anti-tumor, and immunoregulatory attributes, has attracted the attention of many researchers. Studies testing the therapeutic effects of AG have demonstrated desirable results in the treatment of a variety of clinical diseases. With high safety and various biological functions, AG might be a promising candidate for the treatment of musculoskeletal disorders. Here, we review all available literatures to summarize the pharmacological effects of AG and facilitate further researches on musculoskeletal diseases.

[Quality analysis of Citri Trifoliatae Fructus in different harvest time by HPLC combined with electronic eye technology].

As a local variety of medicinal material, Citri Trifoliatae Fructus is widely used in many places, whereas its harvest time remains unclear. Therefore, studying its harvest time can make more reasonable use of this medicinal material. In this study, we determined the flavonoids content and compared the color of Citri Trifoliatae Fructus harvested in different time, aiming to guide the harvest of this medicinal material. The fresh fruits of Citrus trifoliata were collected from Xinxiang city, Henan province, graded according to the diameter range, and then dried. The contents of isonaringin, naringen, and poncirin in Citri Trifoliatae Fructus were determined by HPLC, and the color values of the samples were detected by electronic eye. The correlation analysis of the obtained data was carried out to explore the relationships of color and diameter with quality. The results showed that the contents of isonaringin, naringen, and poncirin varied significantly in different harvest time, within the ranges of 0.21-1.20, 2.21-11.59, and 3.73-23.16 mg·g~(-1), respectively. With the delay of harvest time, Citri Trifoliatae Fructus showed the color changing from green to yellow, gradually increased diameter, and gradually decreased contents of isonaringin, naringen, and poncirin. The contents of isonaringin, naringen, and poncirin were negatively correlated with the degree of red and green(a~*) and positively correlated with the degree of yellow and blue(b~*). The contents of naringen and poncirin had significantly negative correlations with the diameter. This study indicates that the quality of Citri Trifoliatae Fructus can be judged by its diameter and skin color, which provides a theoretical basis for the rational harvest of this medicinal material.

Anticancer Phenolics from Dryopteris fragrans (L.) Schott.

Cancer is one of the most major diseases that threatens human health and life. The aim of this work was to obtain novel anticancer molecules from D. fragrans, a kind of medicinal plant. The structure of the new compound was identified using spectroscopic data (¹H-NMR, 13C-NMR and two dimensions NMR). Its anticancer properties were evaluated using the 3-(4,5-dimethyl-2-thiazolyl)-2,5-diphenyl-2-H-tetrazolium bromide (MTT) assay against four human cells including lung cancer cells (A549), breast cancer cells (MCF-7), gastric cancer cells (SGC7901) and noncancerous human umbilical vein endothelial cells (HUVEC). A new phenylpropanoid-(E)-caffeic acid-9-O-ß-d-xylpyranosyl-(1→2)-ß-d-glucopyranosyl ester (1), with seven known compounds (2-8)-was isolated. The IC50 value of compound 1 against MCF-7 cells was 2.65 ± 0.14 µM, and the IC50 values of compound 8 against three cancer cells were below 20 µM.

A New Human Cancer Cell Proliferation Inhibition Sesquiterpene, Dryofraterpene A, from Medicinal Plant Dryopteris fragrans (L.) Schott.

The global burden of cancer continues to increase largely with the aging and growth of the world population. The purpose of the present work was to find new anticancer molecules from a natural source. We utilized chromatographic methods to isolate compounds from medicinal plant Dryopteris fragrans (L.) Schott. The structure of the new compounds was determined by spectroscopic and spectrometric data (1D NMR, 2D NMR, and EMI-MS). Their anti-proliferation effects against five human cancer cell lines including A549, MCF7, HepG2, HeLa, and PC-3 were evaluated by CCK-8 andlactate dehydrogenase (LDH) assay. A new sesquiterpene, (7S, 10S)-2,3-dihydroxy-calamenene-15-carboxylic acid methyl ester (1), and two known compounds (2 and 3) were isolated. The new sesquiterpene was named dryofraterpene A and significantly inhibited cancer cell proliferation without any obvious necrosis below a 10 µM concentration. In conclusion, a novel anticancer sesquiterpene together with two known compounds was isolated, which might be a promising lead compound for the treatment of cancer.

The chemical composition of human milk from Inner Mongolia of China.

In Inner Mongolia, China, the chemical composition of 66 breast milk samples at three lactation stages was analysed. Except for total nitrogen content, the contents of total solid, fat, NPN, lactose and ash were not significantly different between colostral, transitional and mature milk. Fatty acids did not vary over the three lactation stages, while unsaturated fatty acids accounted for 59.95-63.22% of the total fatty acids. Relatively low contents of vitamins were in the milk because the volunteer mothers did not take any vitamin supplementation over the entire lactation period. Besides sodium and phosphate, the concentrations of most minerals in the breast milk remained fairly constant across the three lactation stages.