Chemical Constituents from the Heartwood of Solanum Verbascifolium L. And Their Anti-Inflammatory Activities Combined Network Pharmacology.

Phytochemical studies on 95 % ethanol extract of the heartwood of Solanum verbascifolium L. resulted in the isolation of one new amide derivative (1), and 21 known phenylpropanoids compounds. The structures were characterized by spectral analysis and high-resolution mass spectrometric analysis. The anti-inflammatory activity of amide compounds 1-4 and 6-9 by investigating their impact on the release of nitric oxide (NO) in MH-S cells. Our findings unveiled significant inhibitory effects on NO secretion. Compound 1 exhibited robust dose-dependent suppression, with pronounced inhibition observed at both 20 µM (P<0.01) and 40 µM (P<0.01). Furthermore, compound 9 demonstrated noteworthy inhibitory effects at 40 µM (P<0.01). Similarly, compounds 3 and 4 displayed substantial inhibition of NO secretion at the same concentration, although the significance level was slightly lower (P<0.05). It is expected that there is a substantial association between the anti-inflammatory activities of amides and their targets, specifically PTGS2, by combining network pharmacology and molecular docking techniques. This discovery emphasizes amides' potential as an interesting subject for additional study in the realm of anti-inflammatory medications.

Transcriptional Regulation of the Acer truncatum B. Response to Drought and the Contribution of AtruNAC36 to Drought Tolerance.

Drought stress is one of the major environmental factors severely restricting plant development and productivity. Acer truncatum B, which is an economically important tree species, is highly tolerant to drought conditions, but the underlying molecular regulatory mechanisms remain relatively unknown. In this study, A. truncatum seedlings underwent a drought treatment (water withheld for 0, 3, 7, and 12 days), after which they were re-watered for 5 days. Physiological indices were measured and a transcriptome sequencing analysis was performed to reveal drought response-related regulatory mechanisms. In comparison to the control, the drought treatment caused a significant increase in antioxidant enzyme activities, with levels rising up to seven times, and relative electrical conductivity from 14.5% to 78.4%, but the relative water content decreased from 88.3% to 23.4%; these indices recovered somewhat after the 5-day re-watering period. The RNA sequencing analysis identified 9126 differentially expressed genes (DEGs), which were primarily involved with abscisic acid responses, and mitogen-activated protein kinase signaling. These DEGs included 483 (5.29%) transcription factor genes from 53 families, including ERF, MYB, and NAC. A co-expression network analysis was conducted and three important modules were analyzed to identify hub genes, one of which (AtruNAC36) was examined to clarify its function. The AtruNAC36 protein was localized to the nucleus and had a C-terminal transactivation domain. Moreover, it bounded specifically to the NACRS element. The overexpression of AtruNAC36 in Arabidopsis thaliana resulted in increased drought tolerance by enhancing antioxidant enzyme activities. These findings provide important insights into the transcriptional regulation mediating the A. truncatum response to drought. Furthermore, AtruNAC36 may be relevant for breeding forest trees resistant to drought stress.

PeGSTU58, a Glutathione S-Transferase from Populus euphratica, Enhances Salt and Drought Stress Tolerance in Transgenic Arabidopsis.

Glutathione S-transferases (GSTs) play a crucial role in responding to abiotic stress and are an important target for research on plant stress tolerance mechanisms. Populus euphratica is a promising candidate species for investigating the abiotic tolerance mechanisms in woody plants. In our previous study, PeGSTU58 was identified as being associated with seed salinity tolerance. In the present study, PeGSTU58 was cloned from P. euphratica and functionally characterized. PeGSTU58 encodes a Tau class GST and is located in both the cytoplasm and nucleus. Transgenic Arabidopsis overexpressing PeGSTU58 displayed enhanced tolerance to salt and drought stress. Under salt and drought stress, the transgenic plants exhibited significantly higher activities of antioxidant enzymes, including SOD, POD, CAT, and GST, compared to the wild-type (WT) plants. Additionally, the expression levels of several stress-responsive genes, including DREB2A, COR47, RD22, CYP8D11, and SOD1 were upregulated in PeGSTU58 overexpression lines compared to those in WT Arabidopsis under salt and drought stress conditions. Furthermore, yeast one-hybrid assays and luciferase analysis showed that PebHLH35 can directly bind to the promoter region of PeGSTU58 and activate its expression. These results indicated that PeGSTU58 was involved in salt and drought stress tolerances by maintaining ROS homeostasis, and its expression was positively regulated by PebHLH35.

Seven undescribed compounds from the flower heads of Helianthus annuus L.

Seven undescribed compounds, namely, 4-hydroxy-3-(2'-hydroxy-3'-methyl-1'-butenyl) acetophenone-1'-O-ß-D-glucopyranoside (1), 4-hydroxy-3-((Z)-3'-hydroxy-3'-methyl-1'-butenyl) acetophenone-8-O-ß-D-glucopyranoside (2), 4,6-hydroxy-3-((Z)-3'-hydroxy-3'-methyl-1'-butenyl) acetophenone-8-O-ß-D-glucopyranoside (3), 4-hydroxy-3-((Z)-3'-hydroxy-3'-methyl-1'-butenyl) acetophenone-6-O-ß-D-glucopyranoside (4), 2-hydroxymethylimino-3,4-dimethyl-7-hydroxy-6-methyl ketone-2H-chromon (5), annuolide A-15-O-ß-D-glucopyranoside (6) and heliannuoside A (7), together with eighteen known compounds, were obtained from water extract of the flower heads of Helianthus annuus L. (Asteraceae). The structures of these compounds were elucidated based on spectroscopic analyses. Upon evaluation of the anti-inflammatory activity of compounds 1-9, 15-18, 21 and 24-25 by their effects on the release of NO in MH-S cells, compound 6 showed significant inhibition of NO secretion at 12.5 µM (P < 0.05) and 25 µM (P < 0.01) in a dose-dependent manner, and compound 18 showed inhibition of NO secretion at 25 µM (P < 0.05).

Knockdown of FBI-1 Inhibits the Warburg Effect and Enhances the Sensitivity of Hepatocellular Carcinoma Cells to Molecular Targeted Agents via miR-3692/HIF-1α.

The transcription suppressor factor FBI-1 (the factor that binds to inducer of short transcripts-1) is an important regulator of hepatocellular carcinoma (HCC). In this work, the results showed that FBI-1 promoted the Warburg effect and enhances the resistance of hepatocellular carcinoma cells to molecular targeted agents. Knockdown of FBI-1 via its small-interfering RNA (siRNA) inhibited the ATP level, lactate productions, glucose uptake or lactate dehydrogenase (LDH) activation of HCC cells. Transfection of siFBI-1 also decreased the expression of the Warburg-effect-related factors: hypoxia-inducible factor-1 alpha (HIF-1α), lactate dehydrogenase A (LDHA), or GLUT1, and the epithelial-mesenchymal transition-related factors, Vimentin or N-cadherin. The positive correlation between the expression of FBI-1 with HIF-1α, LDHA, or GLUT1 was confirmed in HCC tissues. Mechanistically, the miR-30c repressed the expression of HIF-1α by binding to the 3'-untranslated region (3'-UTR) of HIF-1α in a sequence-specific manner, and FBI-1 enhanced the expression of HIF-1α and HIF-1α pathway's activation by repressing the expression of miR. By modulating the miR-30c/HIF-1α, FBI-1 promoted the Warburg effect or the epithelial-mesenchymal transition of HCC cells and promoted the resistance of HCC cells to molecular targeted agents.

COC use, ACE/AGT gene polymorphisms, and risk of stroke.

OBJECTIVES: To clarify the effects of the association between combined oral contraceptives (COC) use and ACE/AGT gene on stroke risk, and to undertake a preliminarily study of the molecular mechanism of the association between COC exposure and predisposing genes of hypertension on the increased risk of stroke. METHODS: This study was a multi-center case-control study based on the population of 25 towns in the surveillance regions of Jiangsu province, China. RESULTS: (i) The univariate analysis of the frequency of the DD genotype of ACE insert/delete (I/D) polymorphism between the cases and controls indicated its significant association with the stroke (P<0.01), especially for hemorrhagic stroke (P<0.01). (ii) Women with COC exposure and ACE I/D genotype had an increased risk for all strokes [adjusted odds ratio 5.63; 95% confidence interval (CI), 2.20, 15.68], and an increased risk for hemorrhagic stroke (adjusted odds ratio 31.53; 95% CI, 3.54, 281.14) after adjustment for education and occupation. (iii) Multivariate analyses showed that hypertension was the most important risk factor for hemorrhagic stroke and ischemic stroke. COC use was a significant risk factor for hemorrhagic stroke. The combined effects of COC use, for 15 years and above, and ACE I/D polymorphism increased the risk of all strokes by more than eight times, and the risk of hemorrhagic stroke by more than 15 times. CONCLUSION: Hypertension was a most important risk factor for stroke incidence. The D allele of ACE I/D polymorphism may be a potential risk allele for stroke. COC users carried the ID+DD genotype that may further increase the risk of stroke, especially for hemorrhagic stroke.

Estrogen receptor beta genetic variants and combined oral contraceptive use as relates to the risk of hypertension in Chinese women.

BACKGROUND AND AIMS: Estrogen receptor beta (ESR2) plays an important role in cardiovascular physiology and blood pressure regulation, whereas estrogens may influence gene expression, growth, and cellular differentiation in target tissues by activating estrogen receptors. This study aims to investigate the association between common genetic variants of ESR2 gene and the risk of hypertension and to explore the combined effected of ESR2 variants and combined oral contraceptive (COC) use for hypertension risk. METHODS: A population-based case-control study was conducted in 621 female hypertensive patients and 621 female normotensive controls. RESULTS: ESR2 G1082A heterozygote genotype (GA) was in significant relationship with hypertension (crude odds ratio [OR] = 1.38, 95% CI: 1.09-1.76; adjusted odds ratio [OR] = 1.38, 95% CI: 1.09-1.76). No association was observed for ESR2 G1730A polymorphism. Furthermore, the joint effects of the heterozygote of G1082A polymorphism (heterozygote model: GG/AA vs. GA) and cumulative COC use time ≥15 years significantly increased the risk of hypertension [adjusted odds ratio (OR) = 2.19, 95% CI: 1.49-3.24], and the interaction effects between those two risk factors were significant (p = 0.0001). CONCLUSIONS: The heterozygote GA genotype of ESR2 gene G1082A polymorphism may be a risk genotype for hypertension in Chinese women, and the GA genotype (heterozygote model: GG/AA vs. GA) of G1082A locus together with COC use simultaneously contributed to hypertension development.

Impact of different contraceptive methods on quality of life in rural women of the Jiangsu province in China.

BACKGROUND: The combined oral contraceptives (COCs) and intrauterine devices (IUDs) are the most common contraceptive methods used by women. Women's choices of contraceptive method are largely affected by the safety and efficacy of contraceptive methods as well as by change in women's quality of life. However, there are still scanty data focusing on the impact of COC or IUD on quality of life in women, especially in China. The aim of this study was to evaluate the impact of desogestrel and ethinyl estradiol tablets (Marvelon) and Yuangong-Cu220 IUD (YCu220 IUD) on quality of life in rural women of the Jiangsu province in China. STUDY DESIGN: In this prospective cohort study, 784 COC users and 910 YCu220 IUD users were included. The women filled up quality-of-life questionnaires (Quality of Life Enjoyment and Satisfaction Questionnaire) before and after use of contraceptive methods. RESULTS: Significant score changes in physical health, mood, work/school/labor, living situation, vision, general well-being and overall satisfaction were noted as significant improvements after COC use in women (p<.05), and the largest improvements were in physical health and living situation; all item scores except for work/school/labor, household activities and leisure time activities had improved statistically from baseline in YCu220 IUD users (p<.05). For COC users, the proportions of women with total quality-of-life scores >/=57 before and after COC use were 11.50% and 11.79%, respectively; but the proportion of YCu220 IUD users with total quality-of-life scores >/=57 increased from 4.40% to 12.04%. Compared to women without contraceptive use history, women with past OC and/or IUD use had a significantly higher difference in the total quality-of-life scores. CONCLUSIONS: COC and YCu220 IUD could significantly improve overall quality of life in rural women of the Jiangsu province.