Latest ArticlesCardiovascular diseases (CVDs) and malignant tumors are the main causes of death worldwide. The etiology study of CVDs and malignant tumors has found a series of widely recognized risk factors. Medical practice and medical theory usually focus on one of the diseases, but more and more evidence reveals that malignant tumors usually involve the cardiovascular system, thus leading to thromboembolism, heart failure, etc. Anti-cancer treatment proves to induce CVDs, while CVDs seem to increase the risk of malignant tumors. This situation requires researchers to conduct further combined crossover study on both CVDs and malignant tumors. In this review, we discuss the potential common risk factors of cardiovascular diseases and malignant tumors, the pathological and physical mechanism of the two kinds of diseases, the cardiac toxicity induced by tumor therapy and the impact of cardiovascular drugs on cancer from the perspective of cardio-oncology, and in the endput forward the prospect of prevention and treatment.
The resistance and dose limitation of tumors is a serious obstacle to cytotoxic drug therapy in the field of medical oncology. Nitric oxide (NO) is a powerful adjuvant for tumor hypersensitivity for traditional chemotherapy and radiation therapy. The concentration of NO plays an important role in affecting its anti-tumor effect. This review summarizes the mechanism of concentration-dependent effects of NO on tumor cells and the mechanism of chemotherapy sensitization. It provides evidence for rational use of NO to exert anti-tumor effects, and overcoming multidrug resistance and anti-tumor drug development.
Physiologically based pharmacokinetic (PBPK) modeling is an important tool to predict pharmacokinetic or pharmacodynamic profiles in special populations, especially in children and infants where designing and conducting clinical studies is difficult. The application of PBPK modeling can effectively promote the development of pediatric drugs and their clinical use. At present, PBPK modeling of pediatric populations is mainly applied in clinical trial design, drug-drug interaction (DDI) risk assessment, and dose selection in children. This review discusses the advantages of PBPK modeling in pediatric drug research and summarizes how to extrapolate a PBPK model from adults to children. The theoretical basis for pediatric PBPK models, the modelling process and important physiological parameters during the modeling process are introduced. Some successful applications of PBPK modeling in pediatric drug research and development are also presented. This review also analyzes the current limitations and future directions of pediatric PBPK modeling.
The senescence-associated secretory phenotype (SASP) is a generic term for the secretion of a series of cytokines such as pro-inflammatory factors, chemokines and proteases, and is a key feature of senescent cells. SASP is a double-edged sword that can resist a harmful environment in normal cells, but with the decline of body function, the massive secretion of cytokines, chemokines and proteases accelerates aging while inducing inflammation, leading to the development of various aging-related diseases. This article reviews the composition and physiological functions of SASP, the changes in SASP during aging, the regulatory pathways associated with SASP, and the anti-aging drugs that regulate SASP. This article aims to present a more comprehensive understanding of SASP and lay the foundation for SASP-based anti-aging research and the discovery of new targets for anti-SASP drugs.
Based on the structure of inhibitors XL765 and WR23, the quinoxaline scaffold was selected as an attractive structure for drug design. In this protocol, the 2-position of quinoxaline was modified with a substituted phenoxy fragment. Meanwhile, the linking chain at the 3-position was changed to a sulfonyl hydrazine or was removed. A series of substituent groups were added at the 6-position of the quinoxaline scaffold. Twenty-two quinoline derivatives were designed and synthesized, and their structures were confirmed by 1H NMR, 13C NMR, and ESI-MS. All compounds were screened for anti-tumor activity in vitro in A549, MCF-7, HCT-116 and HepG2 cancer cells. The results showed that P6b was effective, P6e and P6f had better activity against HCT116 (IC50=3.24, 4.78 and 4.50 μmol·L-1), and P6d had strong inhibitory effect on MCF-7 (IC50=0.228 7 μmol·L-1).
A new carbazole alkaloid was isolated from the aqueous extract of the stems of Clausena lansium (Lour.) Skeels by various chromatographic methods, including HPD-100, PRP-512A, silica gel, and reverse phase C18. Its structure was determined by spectroscopic and chemical methods, including UV, IR, HR-ESI-MS, 1D/2DNMR and ECD. Compound 1, named as Claulamine F, showed no antimicrobial activity on Staphylococcus aureus, Escherichia coli or Pseudomonas aeruginosa. In addition, compound 1 exhibited no cytotoxicity on five kinds of cancer cells through MTT methods.
Notoginseng (Sanqi), the root of Panax notoginseng (Burk.) F. H. Chen (Araliaceae), is one of the most valuable traditional Chinese medicines (TCM). It has been widely used in China with a long history for treatment of haemorrhage, edema, and cardiovascular disorders. Steamed P. notoginseng has been considered to have stronger therapeutic functions than raw P. notoginseng in the treatment of tumors, cardiovascular diseases, etc. Saponins are the principal chemical and pharmacological constituents in P. notoginseng. Thus, it is of great importance to determine the constituent saponins and determine any differences between fresh P. notoginseng and steamed P. notoginseng. We used a rapid and direct analytical method based on liquid extraction surface analysis combined with mass spectrometry (LESA-MS) to identify saponins in the xylem, phloem and cambium of fresh and steamed P. notoginseng root slices. The results revealed that ginsenosides Rg1, Rb1, Re, Rd, notoginsenoside R1 and their malonyl group versions were most abundant in fresh root slices, while in steamed slices ginsenosides Rg5, Rk1 and other minor polar components could be detected, and the relative content of large polar components was lower. The described method is fast, robust and sensitive and the process does not need traditional and cumbersome pretreatment such as crushing, extraction and separation. It is the first non-destructive study on the differences in saponins between fresh and steamed P. notoginseng root slices.
The p21-activated kinase 1 (PAK1) is a member of the P21-activated protein kinase family that plays an important role in the proliferation and on cogenesis of pancreatic cancer. PAK1 is an important target for the treatment of pancreatic cancer. At present, akinase inhibitor targeting PAK1 is still in the preclinical research stage. Therefore, screening for new PAK1 kinase inhibitors is of great significance. In this study the natural compound celastrol was found to have a significant inhibitory effect on PAK1, with an IC50 value of 3.614 μmol·L-1. Molecular docking results showed that celastrol had good binding to PAK1. An MTT assay indicated that celastrol inhibited the proliferation of pancreatic cancer cells BxPC-3 and PANC-1. Mechanistic studies revealed that the inhibition of pancreatic cancer cells by celastrol was reversed by PAK1 siRNA. Celastrol inhibited PAK1 and the subsequent activation of downstream signaling pathways, thereby activating apoptosis signaling pathways and triggering apoptosis in pancreatic cancer cells. These findings suggested that celastrol induced apoptosis in pancreatic cancer cells by suppressing the PAK1 kinase signaling pathway and has potential value for the treatment of pancreatic cancer.
Impurity profiling is one of the most important activities in both assuring drug safety and improving the quality of domestic drugs. Since the basic strategy of impurity profile control was put forward in 2010, a mature control procedure for impurity profile in drugs has been formed in China after nearly ten years of continuous efforts. The progress in impurity profiling before 2010 and from 2010 to 2015 have been reviewed. Since 2015, the concepts, analytical techniques and the application of these techniques in this field have developed rapidly. As a result, the progress in impurity profiling of chemical drugs since 2015 was reviewed in this paper. And the views on future development of impurity profiling in drugs were also put forward.
A bioassay method for inhibiting platelet aggregation in vitro was established to quantify the pharmacological effects of Compound Danshen Tablets and support its quality control. The inhibition of platelet aggregation in rabbit plasma in vitro by Compound Danshen Tablets was used as the experimental system. The titer was calculated by using the method of dose-response parallel lines. As a result, a bioassay for the inhibition of platelet aggregation in vitro by Compound Danshen Tablets was established. Linearity was good in the concentration range of 0.128 g·mL-1 to 0.205 g·mL-1, and the titer of standard Compound Danshen tablets was 7 659 U·g-1 according to the titer definition. This in vitro assay was simple, reliable, reproducible and convenient. The activity of Compound Danshen Tablets in inhibiting platelet aggregation was quantified by potency assay and the quality of different batches was evaluated. The method can be applied for the quality control of Compound Danshen Tablets.
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