Germacrane Sesquiterpene Dilactones from Mikania micrantha and Their Antibacterial and Cytotoxic Activity.

Four new germacrane sesquiterpene dilactones, 2ß-hydroxyl-11ß,13-dihydrodeoxymikanolide (1), 3ß-hydroxyl-11ß,13-dihydrodeoxymikanolide (2), 1α,3ß-dihydroxy-4,9-germacradiene-12,8:15,6-diolide (3), and (11ß,13-dihydrodeoxymikanolide-13-yl)-adenine (4), together with five known ones (5-9) were isolated from the aerial parts of Mikania micrantha. Their structures were elucidated on the basis of extensive spectroscopic analysis. Compound 4 is featured with an adenine moiety in the molecule, which is the first nitrogen-containing sesquiterpenoid so far isolated from this plant species. These compounds were evaluated for their in vitro antibacterial activity against four Gram-(+) bacteria of Staphyloccocus aureus (SA), methicillin-resistant Staphylococcus aureus (MRSA), Bacillus cereus (BC) and Curtobacterium. flaccumfaciens (CF), and three Gram-(-) bacteria of Escherichia coli (EC), Salmonella. typhimurium (SA), and Pseudomonas Solanacearum (PS). Compounds 4 and 7-9 were found to show strong in vitro antibacterial activity toward all the tested bacteria with the MIC values ranging from 1.56 to 12.5 µg/mL. Notably, compounds 4 and 9 showed significant antibacterial activity against the drug-resistant bacterium of MRSA with MIC value 6.25 µg/mL, which was close to reference compound vancomycin (MIC 3.125 µg/mL). Compounds 4 and 7-9 were further revealed to show in vitro cytotoxic activity toward human tumor A549, HepG2, MCF-7, and HeLa cell lines, with IC50 values ranging from 8.97 to 27.39 µM. No antibacterial and cytotoxic activity were displayed for the other compounds. The present research provided new data to support that M. micrantha is rich in structurally diverse bioactive compounds worthy of further development for pharmaceutical applications and for crop protection in agricultural fields.

Efficacy and Safety of Xue-Fu-Zhu-Yu Decoction for Patients with Coronary Heart Disease: A Systematic Review and Meta-Analysis.

OBJECTIVE: To systematically evaluate the efficacy and safety of XFZYD for coronary heart disease (CHD). METHODS: A comprehensive literature search of randomized controlled trials using XFZYD for CHD was conducted in 10 electronic databases from their establishment to December 20, 2020. The researchers screened the relevant trials in NoteExpress, extracted the data in duplicate independently, assessed the risk of bias in the trials using the Cochrane collaboration tool, and then used Rev Man 5.3 for data analysis. RESULTS: 30 trials with 3126 participants were included for meta-analysis. The results showed that the clinical effects of XFZYD and its combination with chemical drugs (CD) were 1.13 (RR; 1.13; 95% CI, 1.03 to 1.24) and 1.26 (RR; 1.26; 95% CI, 1.20 to 1.32) times those of CD, respectively. And, it could also improve electrocardiogram effect, which was 1.63 (RR; 1.63; 95% CI, 1.04 to 2.53) times that of CD. XFZYD could not only decrease duration of angina pectoris and improve vascular endothelial function but also obviously reduce the TCM syndrome score. When used in combination with CD, it could also lower AF, correct the dyslipidemia, and reduce the blood viscosity. CONCLUSION: These results demonstrated that XFZYD had great advantages in treating CHD with no obvious adverse reactions. Therefore, it is believed that XFZYD is more suitable for CHD patients with clinical indicators of dyslipidemia, high blood viscosity, or vascular endothelial dysfunction. This study is the first systematic review and meta-analysis with some unique ways, including its comprehensiveness, large-scale search, the novelty of findings, and transparent approach.

Application of Computer-Aided Tongue Inspection for Preliminary Screening of Esophageal Cancer.

OBJECTIVE: To differentiate patients with esophageal cancer or premalignant lesions from the high-risk population for preliminary screening of esophageal cancer using a feature index determined by a computer-aided tongue information acquisition and processing system (DS01-B). METHODS: Totally, 213 patients diagnosed with esophageal cancer or premalignant lesions and 2,840 normal subjects were collected including primarily screened and reexamined, all of them were confirmed with histological examinations. Their tongue color space values and manifestation features were extracted by DS01-B and analyzed. Firstly, the analysis of variance was performed to differentiate normal subjects from patients with esophageal cancer and premalignant lesions. Secondly, the logistic regression was conducted using 10 features and gender, age to get a predictive equation of the possibility of esophageal cancer or premalignant lesions. Lastly, the equation was tested by subjects undergoing primary screening. RESULTS: Saturation (S) values in the HSV color space showed significant differences between patients with esophageal cancer and normal subjects or those with mild atypical hyperplasia (P<0.05); blue-to-yellow (b) values in the Lab color space showed significant differences between patients with esophageal cancer or premalignant lesions and normal subjects (P<0.05). Logistic regression analysis showed that the computer-aided tongue inspection approach had an accuracy of 72.3% (2008/2776) in identifying patients with esophageal cancer or premalignant lesions for preliminary screening in high-risk population. CONCLUSION: Computer-aided tongue inspection, with descriptive and quantitative profile as described in this study, could be applied as a cost- and timeefficient, non-invasive approach for preliminary screening of esophageal cancer in high-risk population.

[Pharmacological mechanism analysis of oligopeptide from Pinctada fucata based on in silico proteolysis and protein interaction network].

Thoracic obstruction is mainly attributed to the scope of coronary heart disease in modern medicine, and traditional Chinese medicine(TCM) shows a significant effect in the treatment of thoracic obstruction. In this research, a network pharmacology method was carried out to systemically study the underlying mechanism of the core herbal compatibility in TCM on the thoracic obstruction. First, we collected the literature about TCM prescriptions for treating thoracic obstruction from CNKI. Then, a prescription database was establish by TCM inheritance support platform system(V2.5) to determine the medication rules and core herbal compatibility in TCM. Finally, to obtain the potential signaling pathways, KEGG pathway analysis was performed by BATMAN-TCM online analysis tool. Results showed that the potential signal pathway of core herbal compatibility in TCM for the clinical treatment of thoracic obstruction was calcium ion and cGMP-PKG signaling pathway. This study provided a new research strategy for the study of the medication rules and mechanism of traditional Chinese medicine in the treatment of thoracic obstruction.

[Correlative analysis of the diversity patterns of regional surface water, NDVI and thermal environment].

Taking Zhengzhou City, the capital of Henan Province in Central China, as the study area, and by using the theories and methodologies of diversity, a discreteness evaluation on the regional surface water, normalized difference vegetation index (NDVI), and land surface temperature (LST) distribution was conducted in a 2 km x 2 km grid scale. Both the NDVI and the LST were divided into 4 levels, their spatial distribution diversity indices were calculated, and their connections were explored. The results showed that it was of operability and practical significance to use the theories and methodologies of diversity in the discreteness evaluation of the spatial distribution of regional thermal environment. There was a higher overlap of location between the distributions of surface water and the lowest temperature region, and the high vegetation coverage was often accompanied by low land surface temperature. In 1988-2009, the discreteness of the surface water distribution in the City had an obvious decreasing trend. The discreteness of the surface water distribution had a close correlation with the discreteness of the temperature region distribution, while the discreteness of the NDVI classification distribution had a more complicated correlation with the discreteness of the temperature region distribution. Therefore, more environmental factors were needed to be included for a better evaluation.

[Spatiotemporal variation of urban heat island in Zhengzhou City based on RS].

By using two Landsat remote sensing images (May 14, 1988 by TM sensor and May 10, 2001 by ETM+ sensor) and local meteorological data, this paper analyzed the causes and harms of urban heat island (UHI) in Zhengzhou City. The brightness temperatures of the images were calculated by mono-window algorithm, and related thematic maps were figured out. The results showed that with the expanding urban area of Zhengzhou City, the UHI effect was growing. Comparing with that in 1988, the high-temperature region of the City in 2001 had a clear shift and expansion towards northeast and southwest, being similar to the change trends of the low vegetation coverage area and urban land area. In order to alleviate the growing UHI effect, attentions should be paid on the urban greening work and the choice of reasonable greening patterns in the process of urbanization.