Sesquiterpene from Artemisia argyi seed extracts: A new anti-acute peritonitis agent that suppresses the MAPK pathway and promotes autophagy.

To find novel anti-inflammatory drugs, we screened anti-inflammatory compounds from 18 different types of Artemisia argyi seed extracts. The in vitro and in vivo anti-inflammatory activities of the screened compounds and their mechanisms were characterized. We first detected the cytotoxic effect of the compounds on RAW264.7 cells and the inhibitory effect on LPS-induced NO release. It was found that sesquiterpenoids CA-2 and CA-4 had low cytotoxic and strong NO inhibitory activity with an IC50 of 4.22 ± 0.61 µM and 2.98 ± 0.23 µM for NO inhibition, respectively. Therefore, compound CA-4 was studied in depth. We found that compound CA-4 inhibited LPS-induced pro-inflammatory factor production and M1 macrophage differentiation in RAW264.7 cells. Additionally, CA-4 inhibited the expression of p-ERK1/2, p-JNK, iNOS, and COX-2 by blocking the MAPK signaling pathway. CA-4 also promoted the expression of autophagy-related proteins such as LC3 II and Beclin-1 by inhibiting activation of the PI3K/AKT/mTOR signaling pathway, and promoted the generation of autophagosomes. Finally, CA-4 significantly inhibited the degree of inflammation in mice with acute peritonitis, showing good anti-inflammatory activity in vivo. Consequently, compound CA-4 may be a promising drug for the treatment of acute inflammatory diseases and provide new ideas for the synthesis of novel anti-inflammatory compounds.

Corylin inhibits the progression of Non-small cell lung cancer cells by regulating NF-κB signaling pathway via targeting p65.

BACKGROUND: Lung cancer is characterized by high-risk and high mortality, among which non-small cell lung cancer (NSCLC) conquers a dominant position. Previous studies have reported that corylin has anti-inflammatory, anti-oxidant, and anti-tumor effects; however, its role in NSCLC cells remains unclear. HYPOTHESIS: Corylin inhibits the progression of NSCLC cells. METHODS: A lentivector NF-κB luciferase reporter was constructed by molecular cloning. Corylin was screened and identified as an NF-κB pathway inhibitor by luciferase reporter assay. Corylin inhibited the expression of NF-κB downstream genes, which was detected by qRT-PCR. The effect of corylin on NSCLC cells was detected by colony formation assay, cell apoptosis, cell proliferation, in vitro invasion, and cell scratch assay. Corylin inhibited p65 nuclear translocation and was detected by molecular docking, immunofluorescence assay, and Western blot analysis. RESULTS: We constructed a lentiviral expression vector, containing an NF-κB luciferase reporter and established a stable A549 cell line for its expression. Using this cell line, corylin was screened and identified as an NF-κB pathway inhibitor. It was found that corylin inhibited the expression of NF-κB downstream genes and inhibited the proliferation and migration of NSCLC cells. Meanwhile, it was also found that corylin significantly reversed the increased proliferation of NSCLC cell lines induced by p65 overexpression. Molecular docking analysis showed that corylin could bind to p65 by hydrogen bonding. Further study showed that corylin inhibited the NF-κB signaling pathway by blocking p65 nuclear translocation. CONCLUSIONS: Our study screened and identified corylin as an NF-κB inhibitor and elucidated the molecular mechanism by which corylin inhibits the growth of NSCLC cells. The present study provides a novel strategy for improving the prognosis and treatment of NSCLC patients.

Pharmacological Activity of Quercetin: An Updated Review.

Quercetin, a natural flavonoid compound with a widespread occurrence throughout the plant kingdom, exhibits a variety of pharmacological activities. Because of the wide spectrum of health-promoting effects, quercetin has attracted much attention of dietitians and medicinal chemists. An updated review of the literature on quercetin was performed using PubMed, Embase, and Science Direct databases. This article presents an overview of recent developments in pharmacological activities of quercetin including anti-SARS-CoV-2, antioxidant, anticancer, antiaging, antiviral, and anti-inflammatory activities as well as the mechanism of actions involved. The biological activities of quercetin were evaluated both in vitro and in vivo, involving a number of cell lines and animal models, but metabolic mechanisms of quercetin in the human body are not clear. Therefore, further large sample clinical studies are needed to determine the appropriate dosage and form of quercetin for the treatment of the disease.

Variations in compositions and antioxidant activities of essential oils from leaves of Luodian Blumea balsamifera from different harvest times in China.

Xanthoxylin was the main compound (content 44.92% of total volatiles) in the leaves of Luodian B. balsamifera, which might be the key cause of failure in collecting essential oil (EO) of the leaves using general hydrodistillation in Clevenger apparatus. A modified hydrodistillation equipped with Clevenger apparatus was designed for isolating EO from the leaves. Six EOs of Luodian B. balsamifera harvested once a month from September to next February were collected successfully. The main components of EOs were δ-elemene, α-cubenene, caryophyllene, caryophyllene epoxide, γ-eudesmol, xanthoxylin, and α-eudesmol. The EOs of Luodian B. balsamifera collected from October to December had higher antioxidant activities (ACs). Combining the principal component analysis of chemical components with the results of ACs and the yields of six EOs, the leaves of Luodian B. balsamifera were suitable to be harvested in November and December to obtain EO with high quality.

Traditional Chinese Medicine comprehensive therapy for the improvement of motor function in spinal cord injury patients.

OBJECTIVE: To study the effect of early comprehensive therapy of Traditional Chinese Medicine (TCM) on motor function of in patients with spinal cord injury. METHODS: Fifty-one standard spinal cord injury patients with paraplegia were randomly assigned to an experimental or control group. The experimental group received TCM comprehensive therapy, and the control group received modern Western Medicine (WM) treatment for 4 weeks. The motor score (MS), Barthel Index (BI) and American Spinal Injury Association (ASIA) grading were measured in both groups before and after treatment. RESULTS: After treatment, the MS and BI scores of the TCM comprehensive therapy group improved significantly (P < 0.01), and there was no significant difference in ASIA grading (P > 0.05). The differences between the experimental and control groups after treatment were not significant (P > 0.05). CONCLUSION: Early TCM comprehensive therapy is an effective method for improving motor function in patients with spinal cord injury.