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As a traditional Chinese medicine, Eupatorium lindleyanum DC. has an effect on resolving phlegm, relieving cough, and relieving asthma. In this study, an ultra high performance liquid chromatography with quadrupole time-of-flight mass spectrometry method was established for qualitative analysis of Eupatorium lindleyanum. Besides, we developed an ultra high performance liquid chromatography with triple quadrupole tandem mass spectrometry method in positive and negative multiple reaction monitor modes for the quantitative analysis of 27 chemical constituents from 19 different batches of Eupatorium lindleyanum. The methodology validated linearity, intraday and interday precision, stability, repeatability, and recovery. The results showed that there were some differences in different batches of Eupatorium lindleyanum, which might be attributed to the influence of different growth environments and climatic conditions on the accumulation of compounds. The variable importance of projection value of orthogonal partial least square discriminant analysis and anti-inflammatory activity test showed that eupalinolide A, B, C, and K have high content and strong activity, which could provide a reference for the follow-up study of the quality markers of Eupatorium lindleyanum. Collectively, we developed a rapid and efficient method for the qualitative analysis and simultaneous quantification of Eupatorium lindleyanum, which was beneficial for the comprehensive utilization and development of resources.

Danqi tablet composed of the dried roots of Salvia miltiorrhiza and Panax notoginseng is a well-known Chinese patent medicine commonly used for the treatment of cardio-cerebrovascular diseases such as coronary heart disease and myocardial ischemia. Numerous chemical constituents belonging to S. miltiorrhiza and P. notoginseng were detectable in Danqi tablet. Here, we established and validated a rapid and sensitive ultra-performance liquid chromatography coupled with triple quadrupole mass spectrometry method for simultaneous quantification of 23 components in Danqi tablet and then successfully applied to assay 12 batches of samples from ten manufacturers. Our results demonstrated that the contents of 23 components in 12 batches of Danqi tablets varied significantly and their quality indeed existed different based on principal component analysis. According to the quantitative data and the loading plot of principal component analysis, five abundant compounds in Danqi tablet were selected as characteristic chemical markers possibly responsible for the quality assessment. Among them, salvianolic acid B and ginsenoside Rg1 were further chosen to be combined at 2:5 ratio to evaluate the anti-thrombotic activity on phenylhydrazine-induced zebrafish heart thrombosis model. Expectedly, this component combination increased the heart red blood cells intensity compared with the model group and the median effective concentration was 123.4 μg/mL, suggestive of its well anti-thrombotic effect. This study contributed to quantitative evaluation of Danqi tablet and indicated the combination of salvianolic acid B and ginsenoside Rg1 may be capable of reflecting the effect of Danqi tablet, thereby providing reference for further investigations on the improvement of quality control and clinical application of Danqi tablet. This article is protected by copyright. All rights reserved.

Safflower has both medicinal and edible values but research on its nutrient composition is still lacking. This study was established for the quantitative determination of 28 nucleosides, nucleobases, and amino acids based on the ultra-performance liquid chromatography coupled with triple-quadrupole linear ion-trap tandem mass spectrometry. Analysis of 30 batches of safflower from different producing areas indicated that the contents of l-proline, l-asparagine, l(+)-arginine, l-serine, l-histidine, uracil, guanosine, and uridine was high in safflower. Principle component analysis and cluster analysis found that samples from different regions could be distinguished well, and samples from the same area could be clustered into one class, different geographical environments may cause the differences of nucleosides, nucleobases, and amino acids in safflower. The analysis of principal component analysis, cluster analysis, and counter propagation artificial neural network show similar results. Then the content of nucleosides, nucleobases, and essential amino acids were compared, and found that the content in safflower from Gansu was higher than those from other regions, and there was a little difference between the samples from Xinjiang, Sichuan, and Yunnan. This research revealed the composition of nucleosides, nucleobases, and amino acids in safflower, and provided a theoretical basis for utilization of safflower.

A metal-free and efficient visible-light-induced spirocyclization of indolyl-ynones with diselenides at room temperature under air atmosphere to prepare 3-selenospiroindolenines in moderate to good yields has been developed. The resulting products were tested for in vitro anticancer activity by MTT assay, and compounds 3 c and 3 e showed potent cancer cell-growth inhibition activities.

A visible-light mediated multicomponent cascade reaction of diselenides, alkynes, and sulfur dioxide was developed, in which multiple C-Se and C-S bonds were constructed, and unexpected β-sulfonylvinylselane compounds were generated with high selectivity for E configuration. β-Sulfonylvinylselane transformation into 1,4-oxathiine-4,4-dioxide and sulfonylethyne derivates was then investigated. A plausible mechanism involving a selenium radical-initiated cascade reaction and sulfur dioxide insertion was proposed.

Leonurus japonicus Houtt., a traditional Chinese herbal medicine, is often used as a gynecological medicine with the effect of promoting blood circulation, regulating menstruation, clearing heat, and detoxificating. As the most important alkaloid in L. japonicus, leonurine has a wide range of biological activities, such as antioxidation, anti‐inflammation, and anti‐apoptosis. Cardiovascular system and central nervous system diseases are arrogant killers that threaten human lives and health around the world, but many drugs for treating them have certain side effects. This paper reviews the potential therapeutic effects of leonurine on cardiovascular system and central nervous system diseases, summarizes the previous research progress, and focuses on its therapeutic effect in various diseases. Although leonurine plays a prominent role in the treatment of cardiovascular system and central nervous system diseases, there are still some shortages, such as low bioavailability, weak transmembrane ability, and poor fat solubility. Therefore, the structure modification of leonurine may solve these problems and provide reference value for the development of new drugs. At present, leonurine is in clinical trial, and it is hoped that our summary will help to provide guidance for its future research on the basic science and clinical application., This article reviews the pharmacological effects of a hot potential drug leonurine on cardiovascular and brain diseases. Its structure modification may be an effective way to reduce side effects, strengthen efficacy, and improve bioavailability. We believe that in the near future, leonurine is very likely to become one of the new drugs following the results of artemisinin, which will benefit all human beings.

An unexpected domino reaction of β-keto sulfones with acetylene ketones has been developed. The domino reaction of β-keto sulfones with diynones proceeded smoothly in the 30% mol K2CO3 without other additives, and afforded the novel 3(2H)-furanone derivatives. Replaced diynones with terminal alkyne ketones, the reaction regioselectivity was changed and sulfonylbenzenes were obtained via the benzannulation in good yields.

OBJECTIVES Guided by the unified theory of acceptance and use of technology (UTAUT), the study explored information and communications technology (ICT) use and anticipation among middle-aged adults in urban China. METHODS Path analysis was performed on data from 401 participants aged 45-65 to examine the associations between anticipated ICT support and the acceptance and adoption process of ICT. RESULTS For the late middle-aged adults, those who had greater belief in ICT usefulness and received more social support for ICT use were more likely to anticipate greater ICT support in old age. These associations were not found in the early middle-aged group. DISCUSSION The frequency of ICT use may be the key explanation for different ICT predictors and patterns. The constructs of UTAUT are sequential steps. Middle-aged adults may believe in ICT usefulness even though they have not witnessed it in person.

A method for the intramolecular addition of triarylmethanes to alkynes has been developed. The reaction was efficiently promoted by KOtBu/DMF without any transition-metal catalyst. A variety of indene derivatives were prepared in moderate to good yields. A cascade cyclization of 2-alkyl-substituted substrates at elevated reaction temperature gave bicyclic indene derivatives. The reaction is proposed to proceed through the generation of a triphenylmethyl radical.

In most cases, the title reaction yields the expected products under the mild conditions A).

Odoroside A (OA) is an active ingredient extracted from the leaves of Nerium oleander Linn. (Apocynaceae). This study aims to examine the anticancer bioactivity of OA against CRC cells and to investigate the action mechanisms involved. As a result, OA can significantly inhibit cellular ability and induce apoptosis of CRC cells in a concentration-dependent manner without any obvious cytotoxicity in normal colorectal epithelial cells. Then, quantitative proteomics combined with bioinformatics is adopted to investigate the alterations of proteins and signaling pathways in response to OA treatment. As suggested by the proteomic analysis, flow cytometry and Western blotting analyses validate that exposure of CRC cells to OA causes cell cycle arrest and apoptosis, accompanied with the activation of the ROS/p53 signaling pathway. This observation demonstrates that OA, as a natural product, can induce oxidative stress to suppress tumor cell growth, implicating a novel therapeutic agent against CRC without obvious side effects.

A method for the intramolecular addition of triarylmethanes to alkynes has been developed. The reaction was efficiently promoted by KOtBu/DMF without any transition-metal catalyst. A variety of indene derivatives were prepared in moderate to good yields. A cascade cyclization of 2-alkyl-substituted substrates at elevated reaction temperature gave bicyclic indene derivatives. The reaction is proposed to proceed through the generation of a triphenylmethyl radical.

In most cases, the title reaction yields the expected products under the mild conditions A).

Carboxylesterase and UDP-glucuronosyltransferase-mediated metabolism of irinotecan (CPT-11) has long been proposed to be responsible for its anti-tumor activity and toxicity, like delayed-onset diarrhea. However, recent studies failed to gain more comprehensive in vivo and in vitro pharmacokinetic profiles of irinotecan. Herein, we use rat plasma, human liver microsomes and immortalized HepG2 cell as experimental subjects to describe a sensitive and versatile UHPLC-MS/MS method for simultaneously quantifying CPT-11 and its metabolites, including SN-38 and SN-38G. The method was applied to investigate the pharmacokinetic and metabolic behavior of CPT-11 in the biological samples. Calibration curves for all bio-matrices showed acceptable linearity (r2 > 0.99). The intra- and inter-day precisions (RSD, %) were within 15% and the excellent accuracy (RE) was between 2.96 and 14.12%. In addition, the specificity, matrix effect and extraction recovery all met the requirements of biological sample analysis. We successfully applied this method to investigate the pharmacokinetics of irinotecan in various biological samples, mediated by carboxylesterase and UDP-glucuronosyltransferase. This method could be employed in monitoring the metabolic status and clinical efficacy of irinotecan in the future.

Iridium-catalyzed acceptorless dehydrogenative coupling of tertiary amines and arylamines has been developed. A number of benzimidazoles were prepared in good yields. An iridium-mediated C–H activation mechanism is suggested. This finding represents a novel strategy for the synthesis of benzimidazoles.

A new synthesis of phenanthrene derivatives has been achieved through intramolecular cyclization of 1,1′-biphenyl aldehydes and ketones promoted by KOt-Bu/DMF. A free radical reaction pathway is proposed.

It is suggested, that a DMSO radical generated in tBuOK/DMSO systems works as the crucial initiator for the title cyclization process.

A new synthesis of indole derivatives has been achieved through intramolecular dehydrative coupling of tertiary amines and ketones promoted by KO-t-Bu/DMF. The reaction probably proceeds via an α-amino alkyl radical pathway.

The 6-endo-cyclization of substrates (VI) and (VIII) gives rise to corresponding tetrahydroquinoline derivatives, whilst the reaction of substrate (XI) leads to indoline (XII) as a result of a 5-exo-cyclization.