Screening the components of Saussurea involucrata for novel targets for the treatment of NSCLC using network pharmacology.

BACKGROUND: Saussurea involucrata (SAIN), also known as Snow lotus (SI), is mainly distributed in high-altitude areas such as Tibet and Xinjiang in China. To identify novel targets for the prevention or treatment of lung adenocarcinoma and lung squamous cell carcinoma (LUAD&LUSC), and to facilitate better alternative new drug discovery as well as clinical application services, the therapeutic effects of SAIN on LUAD&LUSC were evaluated by gene differential analysis of clinical samples, compound target molecular docking, and GROMACS molecular dynamics simulation. RESULTS: Through data screening, alignment, analysis, and validation it was confirmed that three of the major active ingredients in SAIN, namely quercetin (Q), luteolin (L), and kaempferol (K), mainly act on six protein targets, which mainly regulate signaling pathways in cancer, transcriptional misregulation in cancer, EGFR tyrosine kinase inhibitor resistance, adherens junction, IL-17 signaling pathway, melanoma, and non-small cell lung cancer. In addition, microRNAs in cancer exert preventive or therapeutic effects on LUAD&LUSC. Molecular dynamics (MD) simulations of Q, L, or K in complex with EGFR, MET, MMP1, or MMP3 revealed the presence of Q in a very stable tertiary structure in the human body. CONCLUSION: There are three active compounds of Q, L, and K in SAIN, which play a role in the treatment and prevention of non-small cell lung cancer (NSCLC) by directly or indirectly regulating the expression of genes such as MMP1, MMP3, and EGFR.

Precise engineering of Gemcitabine prodrug cocktails into single polymeric nanoparticles delivery for metastatic thyroid cancer cells.

GLOBOCAN estimates 36 types of cancers in 185 countries based on the incidence, mortality, and prevalence in the year 2019. Nowadays, chemotherapy is the most widely used cancer treatment among immune, radio, hormone, and gene therapies. Here, we describe a very simple yet cost-effective approach that synergistically combines drug reconstitution, supramolecular nano-assembly, and tumor-specific targeting to address the multiple challenges posed by the delivery of the chemotherapeutic Gemcitabine (GEM) drug. The GEM prodrugs were gifted to impulsively self-assemble into excellent steady nanoparticles size on covalent conjugation of linoleic acid hydrophobic through amide group with ∼100 nm. Newly synthesized GEM-NPs morphology was confirmed by various electron microscopic techniques. After successful synthesis, we have evaluated the anticancer property of GEM and GEM-NPs against B-CPAP (papillary thyroid carcinoma) and FTC-133 (human follicular thyroid carcinoma) cancer cell lines. Further studies such as AO-EB (acridine orange-ethidium bromide), nuclear staining and flow cytometry analyses on cell death mechanism signified that the cytotoxicity was associated with apoptosis in thyroid cancer cells. GEM-NPs show excellent biocompatibility compared to GEM. The present study explained that GEM-NPs as a safe and hopeful strategy for chemotherapeutics of thyroid cancer therapy and deserve for further clinical evaluations.

[An ecological stoichiometry model based on the size of Nitraria tangutorum]. / 基于白刺个体大小的生态化学计量模型.

Ecological stoichiometry provides a new method for understanding the characteristics, driving forces and mechanisms of C, N and P coupled cycles. However, there are few reports on the variation in ecological stoichiometry of plants during their growth. In this study, we fitted the total elemental mass of different module based on the size of Nitraria tangutorum, and derived the ecological stoichiometry models of different module and whole ramet by measuring the biomass and nutrient concentrations of the current-year stems in 2017, 2-year-old stems, more than 2-year-old stems, leaves, roots and layerings of N. tangutorum ramet. Our results showed that the derivation model could well reflect the changes in ecological stoichiometry during plant growth. The old stems and the layering had higher N:P and C:P, while leaves,current-year stems, and roots had lower N:P and C:P. The whole plant nutrient elements cumulative rate was P:N:C during the growth process. These results were consistent with the growth rate hypothesis and allometric theory, and provide evidence for nutrient reabsorption. This model could be used as an effective way to analyze the dynamic characteristics of elements in plant growth.