Green chemistry lowers chemical hazards during chemical design, manufacture, and use. By using cleaner solvents, catalysts, and reaction conditions, this technique reduces environmental pollution and boosts atom economy and energy efficiency. Rapid industrialization and urbanization are causing significant harm to our environment by releasing a lot of dangerous and undesired chemicals, gases, or other pollutants. The secrets hidden in nature and its by-products must now be discovered by us in order to enhance the synthesis of physiologically significant moieties and foster its growth. Heterocyclic compounds and its derivatives exhibit various biological potential like anticancer, antimicrobial, anticonvulsant, analgesic, antitubercular, antiinflammatory and cardiovascular activities. This make them good candidates for future medication discovery and give them the potential to be an arsenal for treating diseases. This article provides an overview of the numerous environmentally friendly and green synthetic techniques used to create diverse physiologically significant heterocyclic scaffolds in the period 2002–2022. It is anticipated that this compilation of pertinent information will be of significance and practical value to chemists specializing in organic and pharmaceutical domains, potentially stimulating additional advancements in reaction development within this captivating area of study. 

Green Synthesis of Therapeutically Active Heterocyclic Scaffolds: A Review

Tumor is one of the major diseases that endanger people's health.At present,the treatments used for tumor include surgery,chemotherapy,radiotherapy and so on.Nonetheless,the traditional treatments have some disadvantages,such as insufficient treatment effect,liable to cause multidrug resistance,toxicity and side effect.Further research and exploration of tumor treatment schemes are still necessary.As the energy converter of cells,mitochondria are currently considered to be one of the most important targets for the design of new drugs for tumor,cardiovascular and neurological diseases.Nano-drug delivery carriers have the characteristics of being easily modified with active targeting groups,and it can achieve accurate targeted drug delivery to cells and organelles.This paper reviews the application of mitochondrial targeted nanoparticles in tumor diagnosis and treatment from the aspects of inhibiting tumor cell proliferation,promoting tumor cell apoptosis,inhibiting tumor recurrence and metastasis,and inducing cell autophagy.

Application of Mitochondrial Targeting Strategy of Nano-delivery System in Tumor Diagnosis and Treatment

The tumour necrosis factor-related apoptosis-inducing ligand (TRAIL) triggers the apoptosis of tumour cells. According to recent studies, a number of malignant tumours show resistance to TRAIL due to activation and overexpression of the Yes-associated protein (YAP) signal pathway. Objective:
 To construct a novel type of bacterial outer membrane vesicles (BEVs) based delivery system to inhibit the growth of oral squamous cell carcinoma (OSCC) cells. Methods: BEVs loaded with verteporfin (VPF)/TRAIL (BEVs–TRAIL/VPF) was prepared by ultracentrifugation and filtration.
 The expression of TRAIL was verified by BCA and transmission electron microscopy. High-performance liquid chromatography was used in determining the drug loading of VPF and drawing a release curve in vitro. MTT and Western blot were adopted to reveal the anti-tumour activity of BEVs–TRAIL/VPF
 in vitro. Results: The BEVs–TRAIL/VPF particles appeared round by having a well uniform size distribution of approximately 100 nm in diameter. BEVs–TRAIL and VPF were capable of dose-dependently inhibiting the proliferation of SCC25 cells, and the best inhibitory
 effect appeared at ratios of 5:1–10:1. At 100:5–100:15 ratios, BEVs–TRAIL/VPF had a lower IC50 than free BEVs–TRAIL+VPF group (p<0.05), indicating a more efficacious inhibitory effect. The high inhibitory effect of BEVs–TRAIL/VPF on squamous cell carcinoma
 cells is partially associated with the activation of caspase 3, Bax, BCL2, mTOR, p-mTOR and YAP. Conclusion: the administration of TRAIL/VPF in a fixed ratio by BEVs displays a profound inhibitory effect on OSCC cells, providing a novel approach for the treatment of multidrug-resistant
 OSCC.

The Inhibitory Effects of Tumour Necrosis Factor-Related Apoptosis-Inducing Ligand/Vitipofen-Loaded Bacterial Outer Vesicles on Oral Squamous Cell Carcinoma Cells



Multidrug resistance (MDR) is one of the primary causes of tumor chemotherapy
failure. Therefore, it is essential to uncover new drug treatment protocols. In the current study, employing
chitosan (CS) and sodium tripolyphosphate (TPP) as carriers and cross-linking agents, the proanthocyanidins (PHL)/poly (lactic-co-glycolic acid) (PLGA) were encapsulated by emulsion solvent evaporation,
through which the cationic CS-PLGA-PHL nanosystem was obtained. The effectiveness of CS-PLGAPHL on the invasion and migration of human oral squamous cell carcinoma cells was discussed, as were
their potential mechanisms.



A CS-PLGA-PHL nanosystem was constructed by emulsion-solvent evaporation. The size
distribution, dispersion, and morphology were characterised by the laser particle size analyser and transmission electron microscope. Human oral squamous cell carcinoma drug-resistant cell lines SCC131/R
and SCC-15/DDP were cultured in vitro. The two cell types were induced at different concentrations by
CS-PLGA-PHL, after which a CCK⁃8 experiment was performed to determine the effect of CS-PLGAPHL on the proliferation of the two cell lines. The 50% inhibitory concentration (IC50) of CS-PLGAPHL was calculated at different time points. The transwell chamber experiment was performed to identify
the effects of CS-PLGA-PHL on the migration and invasion of OSCC cells. The expression levels of
MMP-2 and MMP-9 were detected by Western blot and q-PCR.



The preparation of nano system to reduce the proliferative activity of OSCC cells together with inhibit the migration, invasion and tumor growth of OSCC cells



CS-PLGA-PHL is well dispersed. The PDI appeared to be lowest when the mass ratio of chitosan
to PLGA equaled 1:15. CS-PLGA-PHL exhibited a marked effect in inhibiting the proliferation of SCC131/R and SCC-15/DDP as well as the invasion and migration. CS-PLGA-PHL was able to downregulate
the expression of MMP-2 and MMP-9 genes and proteins significantly in drug-resistant cell lines.



CS-PLGA-PHL for oral squamous cell carcinoma has been successfully prepared to exert
significant inhibition on the proliferation, invasion, and migration of OSCC cells. The mechanism involved
was possibly related to the down-regulation of MMP-2 and MMP-9 expression by CS-PLGA-PHL.



CS-PLGA-PHL is well dispersed. The PDI appeared to be lowest when the mass ratio of chitosan to PLGA equaled 1 ∶ 15. CS-PLGA-PHL exhibited a marked effect in inhibiting the proliferation of SCC-131/R and SCC-15/DDP as well as the invasion and migration. CS-PLGA-PHL of was able to downregulate the expression of MMP-2 and MMP-9 genes and proteins significantly in drug-resistant cell lines



None


Inhibiting effect of cationic procyanidin nanoparticles on drug-resistant oral squamous cell carcinoma cell lines

Patients with oral squamous cell carcinoma (OSCC) have a poor prognosis. The molecular mechanism of OSCC progression remains unclear. The aim of this study was to explore specific prognostic biomarkers of OSCC at the transcriptome-wide level. A total of 158 differentially expressed long non-coding RNAs (lncRNAs), including 85 cis-acting and 10 trans-acting differentially expressed lncRNAs, were screened in OSCC tissues compared with adjacent normal tissues. Both cisand trans-target genes of differentially expressed lncRNAs were enriched in pathways associated with cancer progression. Additionally, 25 differentially expressed mRNAs were screened. Overlapping analysis of differential protein-coding genes with the cisand trans-target genes of differentially expressed lncRNAs indicated that KIF19 was the only trans-acting gene of differentially expressed lncRNA ‘ENST00000626052’ (named ENSTa). ENSTa was down-regulated in OSCC tissues and cells, and its low expression corresponded to a poor prognosis in OSCC. KIF19 was highly expressed in OSCC tissues and cells. Patients with high expression of KIF19 had a poor prognosis. Cellular experiments showed that KIF19 expression and cell proliferation were inhibited in cells overexpressing ENSTa. However, KIF19 overexpression counteracted the effect of ENSTa overexpression on cell proliferation. In conclusion, ENSTa regulated the trans-acting KIF19 gene in the inhibition of the progression of OSCC, thus they could be suggested as novel biomarkers for OSCC.

https://doi.org/10.2306/scienceasia1513-1874.2022.047

Analysis of novel prognostic markers of oral squamous cell carcinoma at the transcriptome-wide level

Oral squamous cell carcinoma (OSCC) is the main type of oral cancer. Disturbing DNA repair is an invaluable way to improve the effectiveness of tumor treatment. Here, we aimed to explore the key enhancer drivers associated with DNA damage repair in OSCC cells.Gene Set Enrichment Analysis (GSEA), Gene Set Variation Analysis (GSVA) and Kaplan-Meier analysis were applied to explore the relationship among DNA repair-related genes expression and clinical phenotypes based on The Cancer Genome Atlas (TCGA) database. HOMER software and Integrative Genomics Viewer were applied to identify and visualize enhancers using GSE120634. Toolkit for Cistrome Data Browser was applied to predict transcription factors. Human Protein Atlas Database was used to analyze the protein levels of transcription factors in OSCC and control tissues. Seventy-two OSCC patients were included in this study. qRT-PCR was used to detect transcription factor expression in OSCC and adjacent control tissues collected in this study. qRT-PCR and ChIP-qPCR were used to verify the binding of transcription factors to enhancers, and regulation of target genes transcription. Transcription factor knockdown and control cells were treated with cisplatin. CCK8 was used to detect cell viability and proliferation. Western blotting was implemented to detect the levels of DNA repair-related proteins. Transwell assay was used to detect cell invasion.DNA repair was positively associated with the OSCC metastatic phenotype. Patients in the cluster with high expression of DNA repair-related genes had a worse prognosis and a higher proportion of advanced stage, low-differentiation, alcohol consumption and smoking compared to the cluster with low DNA repair-related gene expression. Seventeen metastasis-specific enhancer-controlled upregulated DNA repair-related genes, with the top two upregulated genes being ADRM1 26 S proteasome ubiquitin receptor (ADRM1) and solute carrier family 12 member 7 (SLC12A7) were screened. High mobility group 20 A (HMG20A) was the key prognostic enhancer driver regulating metastasis-specific DNA repair-related genes, with higher expression in OSCC tissues than normal control tissues, and higher expression in metastatic OSCC tissues than non-metastatic OSCC tissues. HMG20A bound to the metastasis-specific enhancers of ADRM1 and SLC12A7, thereby promoting ADRM1 and SLC12A7 expression. Knockdown of HMG20A enhanced cisplatin sensitivity of cells, and inhibited OSCC cells from repairing DNA damage caused by cisplatin, as well as proliferation and invasion of OSCC cells.HMG20A was identified as the key prognostic enhancer driver regulating DNA repair in OSCC cells, providing a new therapeutic target for OSCC. 

/pdf/hmg20a-was-identified-as-a-key-enhancer-driver-associated-3b45uqn7.pdf

HMG20A was identified as a key enhancer driver associated with DNA damage repair in oral squamous cell carcinomas

The present study aims at the preparation of a chitosan-PLGA-based proanthocyanidin from hawthorn fruit loaded nano-system (CS-PLGA-PHL) and investigate its inhibitory effect on SCC-25 cells and the related mechanisms. Methods: CS-PLGA-PHL nanocomposites were constructed by emulsion-solvent
 evaporation. The effect of CS-PLGA-PHL on the proliferation of human normal squamous epithelial hNOK cells were detected. The antitumor activity of CS-PLGA-PHL on SCC-25 cells were studied by cytotoxicity test, cell cycle and apoptosis analysis. The apoptotic protein and gene expression in
 SCC-25 cells was detected by western blotting and q-PCR. Results: The particle size distribution of CS-PLGA-PHL was narrow with an average of 177.60±41.00 nm. CS-PLGA-PHL did not show significant cytotoxicity to hNOK cells (IC50 > 50 μg/mL), with strong cytotoxicity
 to SCC-25 cells (IC50 = 1.21 μg/mL), which could block the G0/G1 phase of SCC-25 cells and increase the distribution of G2/M phase. Meanwhile, the apoptosis induction of CS-PLGA-PHL was higher than that of free PHL and PLGA-PHL group (P <0.05). The cell cycle inhibition
 and apoptosis induction may be due to the up regulation of apoptosis-associated proteins and genes. Conclusion: CS-PLGA-PHL nanocomposites can inhibit the cell cycle and promote apoptosis of SCC-25 cells by up regulating the expression of apoptosis-associated proteins and genes, suggesting
 that it has potential as a chemotherapeutic drug for the treatment of oral squamous cell carcinoma.

Preparation of chitosan modified poly(lactic-co-glycolic acid) nanoparticles containing hawthorn proanthocyanidins: SCC25 cell cycle arrest, antiproliferation, and apoptosis studies

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