As the main chemical component of aromatic traditional Chinese medicine (TCM), the volatile oil of TCM has significant pharmacological effects, such as antibacterial, anti-inflammatory, antioxidant and so on. However, TCM volatile oil is easy to volatilize and oxidize, which seriously limits its application. As a kind of grid structure material, porous material has the characteristics of high specific surface area, large pore volume, adjustable pore size, strong adsorption capacity and controllable surface chemical properties. It has been widely used in adsorption separation, biomedicine, industrial catalysis, wastewater treatment and other fields. In recent years, the use of porous materials to adsorb volatile oil has provided a new strategy and method for improving the stability of TCM volatile oils. At the same time, it can realize the solidification and stability of TCM volatile oils and the application of preparations. In this review, the development and characteristics of porous materials such as mesoporous silica, mesoporous carbon, mesoporous nano hydroxyapatite, porous metal organic framework, porous starch and their application in improving the stability of TCM volatile oils are summarized, and the research strategies affecting the adsorption stability of porous materials for TCM volatile oils are discussed, in order to provide reference for the stabilization control and application of TCM volatile oils.

We used metabolomics to investigate the ability of a traditional Mongolian medicine called modified Tabusen-2 (MT-2) to improve kidney yang deficiency (KYD) in rats. All animal experiments were conducted under the guidance and standards of the Medical Ethics Committee of Inner Mongolia Medical University. SD rats were divided into 6 groups of six rats: a normal group, a model group, Jinkuishenqi pill administration group (1.26 g·kg^-1), and MT-2 administration in high-, medium- and low-dose groups (1.512, 0.756, and 0.378 g·kg^-1). KYD was established by intramuscular injection of hydrocortisone (HC) and biochemical indicators and clinical characterization was used to confirm that KYD was established. All groups received intragastrically administered drug (Jinkuishenqi pill or MT-2) or saline. Serum from each group was collected after 8 weeks and analyzed by UPLC-Q-exactive-MS to measure various biochemical indicators. The biomarkers affected by MT-2 were identified and the metabolic pathways of KYD regulated by MT-2 were analyzed by metabolomic analysis. The results show that MT-2 can decrease serum creatinine (Cr) in KYD rats and significantly increase (P < 0.05) the content of thyroid stimulating hormone (TSH) and luteinizing hormone (LH). In serum samples, 38 biomarkers such as corticosterone, L-phenylalanine, and DL-tryptophan were measured as possible indicators for disease development in KYD rats. MT-2 lowered 18 biomarkers of KYD, including corticosterone, deoxycorticosterone, and L-phenylalanine, and altered 13 related metabolic pathways including phenylalanine, tyrosine and tryptophan biosynthesis, phenylalanine metabolism and steroid hormone biosynthesis, resulting in an overall improvement in KYD. MT-2 appears to be important in improving KYD in rats mainly by regulating metabolites such as amino acids, steroids and lipids.

The GPCR family component leukotriene B4 receptor 1 (LTB4R1) is the receptor of leukotriene B4 (LTB4), the metabolic product of ω6 fatty acid. LTB4R1 is a potential therapeutic target for the treatment of insulin resistance, chronic inflammation and type 2 diabetes. Here we established a LTB4R1 inhibitor screen model based on the GPCR family protein property that its activation causes the cytosolic escalation of calcium. The cytosolic calcium probe Fluo-8 represents the change of calcium ion. After adding LTB4, the fluorescent signal of Fluo-8 in the CHO cells which are co-transfected with LTB4R1 and Gα16 will change with the increase of cytosolic calcium, and LTB4R1 inhibitor blocked the effect of LTB4 on fluorescent signal of Fluo-8 in the CHO cells. Here, we used 0.2% DMSO as a negative control, and cp-105696 as a positive control in the screen model. After stimulation with LTB4, the Fluo-8 signal in 0.2% DMSO treated CHO cells increased 2 fold and fell back slowly, while the signal in inhibitor (cp-105696) treated cells was not induced by LTB4. The results showed that LTB4 increased the cytosolic calcium detected by Fluo-8 in a dose dependent manner. Similarly, cp-105696 inhibited the Fluo-8 signal dose dependently, indicating that this method can quantify the inhibitory activity of the compounds. The Z'-factor, reflecting the robustness of the screen model, was 0.777 with a series of experiments. In sum, we over-expressed LTB4R1α and Gα16 in CHO cell, used Fluo-8 to detect the calcium signal activated by LTB4, and established the in vitro screen model for LTB4 receptor 1.

T cell immune receptor with Ig and ITIM domains (TIGIT), a promising new target in cancer immunotherapy, plays a critical role in limiting adaptive and innate immunity against tumors. The extracellular domain of human TIGIT was used to immune BALB/c mice, and a new anti-human TIGIT chimeric antibody (c7D3) was developed. The mice in this study were used in accordance with the international guidelines for the care and use of laboratory animals, and the animal study was approved by the Institutional Animal Ethics Committee of AbMax Biotechnology. The biological activity of c7D3 was studied. The results showed that c7D3 exhibited high affinity for TIGIT and effectively inhibited the interaction between TIGIT and its ligands. Cell-based assays indicated that c7D3 induced strong luciferase signaling in TIGIT/CD155 signaling reporter assay and enhanced cytokine secretion in a T cell stimulation assay. The data showed that c7D3 has high binding affinity and excellent blocking bioactivity, supporting the further advancement for therapeutic application.

Synthetic organoselenium compounds can be used as antioxidants, enzyme inhibitors, neuroprotective agents, antitumor agents, anti-infectious agents, and immunomodulators. Diphenyl diselenide (DPDS) is a synthetic organoselenium compound with simple and stable structure, and possesses lower toxicity than inorganic selenium and most organoselenium compounds. Moreover, DPDS has strong antioxidant properties due to its strong glutathione peroxidase-mimetic activity, involvement in thioredoxin reductase catalytic reactions, and activation of the nuclear factor E2 associated factor 2 (Nrf2)/Kelch like epichlorohydrin associated protein-1 (Keap1) signaling pathway. DPDS has been shown to possess a variety of pharmacological activities including anti-inflammatory, anti-diabetic, antifungal, neuroprotective, antitumor, hepatoprotective, renoprotective, and cardiovascular protective effects in a variety of animal and cellular models. This paper reviews the research progress on the physicochemical properties, main pharmacological effects and mechanisms of DPDS by compiling relevant research results, so as to provide reference for future research and reasonable development and application of DPDS.

Natural products, rich in sources and diverse in structure, play an important role in drug discovery. It is a hotspot to identify efficiently bioactive components from complex mixtures in the field of natural product research. Traditional research methods, starting from extraction and isolation to structural elucidation, and finally to bioactivity assay, are generally time-consuming, laborious, and untargeted. Therefore, there is an urgent need to develop efficient screening methods for bioactive component discovery. Native mass spectrometry (native MS) is an underutilized method based on the interaction between target and ligand, which can rapidly discover potential active components in complex matrices. Due to the simple operation and the native state of the protein, the method is specific, efficient, and simple. Herein, we give a brief introduction of native MS and then review its recent application in natural product research, with its advantages and limitations, which would provide a reference for researchers in relevant fields.

The liver is an important organ of the body, which has many functions, such as metabolism and detoxification. Due to the rapid change of lifestyle and the improvement of public health, the incidence rate of non-communicable diseases has increased significantly, which fundamentally changed the disease characteristics in most parts of the world. At present, the global prevalence of non-alcoholic fatty liver disease (NAFLD) is about 25%. Moreover, about 59.10% of NAFLD patients progress to non-alcoholic steatohepatitis (NASH) within 5 years, and about 41% of NASH patients progress to fibrosis. NAFLD has become one of the most important liver diseases in the world and may become the main cause of end-stage liver disease in the next few decades. In addition, NAFLD and related cirrhosis will bring huge economic burden to patients, health care system and society. Since there are currently no medications available that have been approved by Food and Drug Administration (FDA), NAFLD is still treated mainly through lifestyle changes such as exercise and diet. Oxidative stress and inflammation are the most important pathological processes in the occurrence and development of liver diseases. Nuclear factor erythroid-2-related factor 2 (Nrf2) is a key regulator of the body's antioxidant stress system, with anti-inflammatory, antioxidant and other functions. Many studies have shown that Nrf2 pathway significantly affects the progression of liver diseases. In this review, we aimed to summarize the regulatory role of the Kelch-like ECH-associating protein 1 (Keap1)-Nrf2-antioxidant response element (ARE) signaling pathway in the pathogenesis of NAFLD, and to reveal the potential of Nrf2 as a therapeutic target for NAFLD.

This study aimed to evaluate the vasorelaxant effect and mechanisms of compound reserpine and triamterene tablets (CRTTs) and its component triamterene on isolated rat thoracic aorta rings. Isolated rat thoracic aorta rings pre-contracted by high potassium or norepinephrine (NE) were used to evaluate the vasodilatory effect of CRTTs and its component triamterene. The mechanisms concerning endothelium, potassium channels and calcium channels were studied through the interventions of several tool drugs. Animal welfare and experimental procedures followed the requirements of the Laboratory Animal Management and Animal Welfare Ethics Committee of the Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College. The results showed that both CRTTs and triamterene had potent relaxant effect on KCl and NE pre-contracted vessels. Triamterene showed partial endothelium dependency, and N-nitro-L-argininemethyl ester hydrochloride (L-NAME) could influence the relaxant effect, which may be related to the opening of calcium-activated potassium channels. Meanwhile, CRTTs could inhibit intracellular Ca²⁺ release and extracellular Ca²⁺ influx. Overall, CRTTs and its component triamterene have vasorelaxant effects on vessels in vitro, and the vasorelaxant effect of CRTTs may be related to intracellular Ca²⁺ release and extracellular Ca²⁺ influx, while this effect of triamterene may depend on vascular endothelial function and may also be related to the opening of calcium-activated potassium channels.

In order to establish the probabilistic risk assessment method for heavy metals and harmful elements in line with the characteristics of traditional Chinese medicine (TCM) and provide guidance for the safe use of TCM, the contents of lead (Pb), cadmium (Cd), arsenic (as), mercury (Hg) and copper (Cu) in 21 batches of Plantago asiatica L. were determined by inductively coupled plasma mass spectrometry (ICP-MS). By the comprehensive use of investigation of TCM consumption pattern and Monte Carlo simulation technology, the non-carcinogenic and carcinogenic health risks of heavy metals and harmful elements in TCM were assessed by hazard quotient (HQ) and cancer risk (CR), respectively. The greatest risk contributors were screened through sensitivity analysis. The results revealed that the mean contents of Pb, Cd, As, Hg and Cu in Plantago asiatica L. were 9.01, 0.28, 3.83, 0.01 and 12.82 mg·kg^-1, respectively. The P95, P99 and maximum values of HQ for males were 1.41, 2.83 and 10.97 mg·kg^-1, respectively. The P95, P99 and maximum values of HQ for females were 1.27, 2.63 and 9.80 mg·kg^-1, respectively. The P95, P99 and maximum values of HI for males were 1.44, 2.85 and 11.0 mg·kg^-1, respectively. The P95, P99 and maximum values of HI for females were 1.29, 2.66 and 10.0 mg·kg^-1, respectively. The P99 and maximum values for CR_As and total carcinogenic risk (TCR) were greater than 10^-4 for both men and women. The risk assessment results indicated that the non-carcinogenic and carcinogenic health risks of high exposure population caused by arsenic exposure are needed to be concern. The results of sensitivity analysis showed that the exposure frequency of TCM and the arsenic concentrations in Plantago asiatica L. were the main risk contributors. Based on Monte Carlo simulation technology and considering the characteristics of TCM, this study puts forward the first example of probabilistic risk assessment of heavy metals and harmful elements in Chinese herbal medicine, which provides a novel perspective for health risk assessment of heavy metals in TCM.

A new rapid, quality control method based on quantitative water tests has been established for the quality evaluation of Indigo Naturalis. The Turbiscan stability index (TSI) of 26 batches of Indigo Naturalis was measured by a stability analyzer. The parameters, including the method by which the ingredients are added, their particle size, amount, and the testing temperature, were systematically optimized and the methodological indexes such as repeatability and stability were determined. The content of indigo and indirubin in 26 batches of Indigo Naturalis was determined by high performance liquid chromatography and the total ash was measured. The correlation analysis between the active ingredients, total ash content and TSI value of Indigo Naturalis was determined by SPSS 26.0 and Origin 2021. This research shows that the best way to prepare samples for testing is to add 0.2 g of Indigo Naturalis powder which has passed through a No. 7 sieve but failed to pass through a No. 9 sieve to a glass bottle containing 20 mL pure water by a funnel and scan at 25 ℃ with a stability analyzer. Consistency analysis showed that the content ranking of indigo and indirubin is opposite to the TSI value, and the content ranking of total ash is generally consistent with the TSI value. Correlation analysis showed that the correlation coefficients of indigo and indirubin content and TSI value were -0.850 and -0.801, respectively, and R² was 0.72 and 0.64. The correlation coefficient between total ash content and TSI value was 0.724, R² was 0.52. Using the change in TSI value of Indigo Naturalis powder in water, this study establishes the range of classification of Indigo Naturalis decoction pieces and the content of relevant components, which can be used to authenticate Indigo Naturalis and evaluate its quality.