Extracts of Knoxia roxburghii (Spreng.) M. A. Rau Induce Apoptosis in Human MCF-7 Breast Cancer Cells via Mitochondrial Pathways.

Knoxia roxburghii (Spreng.) M. A. Rau (KR) is a plant clinically used in traditional Chinese medicine (TCM) for the treatment of cancer. The study objectives were to examine the effects of KR extracts, petroleum ether (PET), ethyl acetate (EtoAc), butanol (n-BuOH), and H2O-soluble fractions (HSF) of the 75% EtOH extraction on A549 (non-small cell lung cancer), HepG2 (liver cancer), HeLa (cervical cancer), MCF-7 (breast cancer), and L02 (normal hepatocyte) cells. It was found that HSF exhibited the strongest cytotoxic activity against MCF-7 cells, and was accompanied by reduced mitochondrial transmembrane potential, increased levels of intra-cellular reactive oxygen species (ROS) and activated caspases, and upregulated pro-apoptotic and downregulated anti-apoptotic proteins. LC-MS analysis further showed that HSF primarily consisted of calycosin, aloe emodin, rein, maackiain, asperuloside, orientin, vicenin-2, and kaempferide, which have been mostly reported for anti-tumor activity in previous studies. In summary, the current study illustrated the effect, mechanism, and the potential major active components of KR against breast cancer.

[Overview and prospect of research and development cooperation in traditional medicine between China and Thailand].

Under the background of the Belt and Road Initiative, the exchange of traditional medicine has become inevitable. China and Thailand are amicable neighbors, and the cooperation between the two countries in the field of traditional medicine has become increasingly close in recent years. Nevertheless, on account of the differences in culture, region, politics, economy and so on, the two countries have common features and unique characteristics in the theoretical system of traditional medicine, quality standard control of medicinal materials, research and development and use of medicinal materials. This paper summarizes the similarities and differences as well as the development opportunities of traditional medicine between China and Thailand. The specific content involves the development history, resources, and use of medicinal resources in Thailand, the main achievements and existing problems of modern research of Thai medicine, the spread and development of Chinese medicine in Thailand, and the spread and development of Thai medicine in China. Furthermore, the paper outlines the recent situation of traditional medicine interflow and cooperation between the two countries, and predicts the prospects for cooperation and development of traditional medicine between China and Thailand in the context of the Belt and Road Initiative, especially in the joint research and development and the improvement of quality standards of important medicinal plant varieties commonly used by the two countries and circulated across the border. Through the exchange and mutual learning, we can step up the traditional medicine cooperation between China and Thailand, which will provide advantageous conditions for the safety of medicine use as well as political and social stability between the two countries.

Synthetic Regulation of 1,4-Dihydropyridines for the AIE or AIEE Effect: From Rational Design to Mechanistic Views.

Aggregation-induced emission/aggregation-induced emission enhancement (AIE/AIEE) has recently attracted intense research, and a large number of AIE/AIEE luminogens (AIE/AIEEgens) have been constructed for application in diverse scientific fields. The AIE and AIEE effects have similar, but not identical, photophysical behaviors, which are closely related to molecular architectures. However, the current understanding of the inherent differences between AIE and AIEE is still obscure. Herein, a rational design strategy is reported for achieving AIE and AIEE effects by simply incorporating different substituents at the periphery of the same core skeleton. Experimental and theoretical studies on the series of compounds indicated that the restriction of intramolecular twisting motions or/and rotations plays an important role in regard to the corresponding AIE or AIEE behaviors. Moreover, compound 1 a (FW=203, ΦF =80.9 %) was discovered as the lowest molecular weight AIEEgen with a high quantum yield in the solid state despite having no rotatable units. Compound 2 a also exhibited an AIEE effect with the minimum necessary structure (a single ring).

Potential Indicators of Mitochondrial Structure and Function.

Mitochondria regulate a range of important physiological and biochemical cellular processes including apoptotic cell death, energy production, calcium homeostasis, oxidative stress, and lipid metabolism. Given their role as the 'engines' of cells, their dysfunction is associated with a variety of disease states. Exploring the relationship between mitochondrial function and disease can reveal the mechanism(s) of drug activity and disease pathology. In this review, we summarized the methods of evaluating the structure and function of mitochondria, including the morphology, membrane fluidity, membrane potential, opening of the membrane permeability transition pore, inner membrane permeabilization, mitochondrial dynamics, mitophagy, oxidative stress, energy metabolism-related enzymes, apoptotic pathway related proteins, calcium concentration, DNA copy number, oxygen consumption, ß-oxidation-related genes and proteins, cardiolipin content, and adenosine triphosphate content. We believe that the information presented in this review will help explore the pathological processes of mitochondria in the occurrence and development of diseases, as well as the activity and mechanism of drugs, and the discovery of new drugs.

1,4-Dihydropyridines: discovery of minimal AIEEgens and their mitochondrial imaging applications.

Typical aggregation-induced emission enhancement fluorogens (AIEEgens) generally are designed as propeller-shaped molecules with multiple aromatic rotors. Described herein are 1,4-dihydropyridines, which have the minimum size necessary for AIEE, containing only a single ring, synthesized through a facile biocatalysis procedure. Owing to the AIEE property, intramolecular motion can be restrained by the surrounding environment, causing the radiative channel to open up. Both the fluorescence intensities and the lifetimes of the 1,4-dihydropyridine representatives increased with increasing viscosity, and high sensitivities were observed. On the basis of the single crystal X-ray structures, density functional theory (DFT) calculations were performed to explain the mechanism of the single-ring AIEE behaviour. Moreover, a few of the neutral AIEEgens were found to possess a high specificity towards mitochondria. As an example, one of the AIEEgens exhibited superior photostability and excellent storage tolerance, allowing for real-time imaging, viscosity mapping, and long-term tracking of the dynamics of the mitochondrial morphology.