Advances in Research on the Effectiveness and Mechanism of Active Ingredients from Traditional Chinese Medicine in Regulating Hepatic Stellate Cells Autophagy Against Hepatic Fibrosis.

Hepatic fibrosis (HF) is a pathological process of structural and functional impairment of the liver and is a key component in the progression of chronic liver disease. There are no specific anti-hepatic fibrosis (anti-HF) drugs, and HF can only be improved or prevented by alleviating the cause. Autophagy of hepatic stellate cells (HSCs) is closely related to the development of HF. In recent years, traditional Chinese medicine (TCM) has achieved good therapeutic effects in the prevention and treatment of HF. Several active ingredients from TCM (AITCM) can regulate autophagy in HSCs to exert anti-HF effects through different pathways, but relevant reviews are lacking. This paper reviewed the research progress of AITCM regulating HSCs autophagy against HF, and also discussed the relationship between HSCs autophagy and HF, pointing out the problems and limitations of the current study, in order to provide references for the development of anti-HF drugs targeting HSCs autophagy in TCM. By reviewing the literature in PubMed, Web of Science, Embase, CNKI and other databases, we found that the relationship between autophagy of HSCs and HF is currently controversial. HSCs autophagy may promote HF by consuming lipid droplets (LDs) to provide energy for their activation. However, in contrast, inducing autophagy in HSCs can exert the anti-HF effect by stimulating their apoptosis or senescence, reducing type I collagen accumulation, inhibiting the extracellular vesicles release, degrading pro-fibrotic factors and other mechanisms. Some AITCM inhibit HSCs autophagy to resist HF, with the most promising direction being to target LDs. While, others induce HSCs autophagy to resist HF, with the most promising direction being to target HSCs apoptosis. Future research needs to focus on cell targeting research, autophagy targeting research and in vivo verification research, and to explore the reasons for the contradictory effects of HSCs autophagy on HF.

Research progress on the active ingredients of traditional Chinese medicine in the intervention of atherosclerosis: A promising natural immunotherapeutic adjuvant.

Atherosclerosis (AS) is a chronic inflammatory disease caused by disorders of lipid metabolism. Abnormal deposition of low-density lipoproteins in the arterial wall stimulates the activation of immune cells, including the adhesion and infiltration of monocytes, the proliferation and differentiation of macrophages and lymphocytes, and the activation of their functions. The complex interplay between immune cells coordinates the balance between pro- and anti-inflammation and plays a key role in the progression of AS. Therefore, targeting immune cell activity may lead to the development of more selective drugs with fewer side effects to treat AS without compromising host defense mechanisms. At present, an increasing number of studies have found that the active ingredients of traditional Chinese medicine (TCM) can regulate the function of immune cells in multiple ways to against AS, showing great potential for the treatment of AS and promising clinical applications. In this paper, we review the mechanisms of immune cell action in AS lesions and the potential targets and/or pathways for immune cell regulation by the active ingredients of TCM to promote the understanding of the immune system interactions of AS and provide a relevant basis for the use of active ingredients of TCM as natural adjuvants for AS immunotherapy.

Icariin as an emerging candidate drug for anticancer treatment: Current status and perspective.

Icariin (ICA) is a kind of natural flavonoid compound monomer, which is derived from the extract of dried stems and leaves of Epimedium. Modern pharmacological studies have found that ICA has broad bioactive function in affecting the biological processes of a variety of cancers, including breast cancer, colorectal cancer, hepatocellular carcinoma, esophageal cancer and other cancers, which indicates that ICA has promising application value in the treatment of cancer patients in the future. Nevertheless, the targets and molecular mechanisms of ICA in cancer treatment have not been elucidated in detail. Therefore, in this review, we systematically summarizes the current research progress of ICA in a series of cancers. In particular, an emphasis is placed on the mechanism of ICA and its future development direction, aiming at providing relevant theoretical basis for the development and application of ICA in the future cancer treatment strategies.

Progress of experimental research on prevention and treatment of diabetic kidney disease by traditional Chinese medicine / 中国药科大学学报

@#Diabetic kidney disease (DKD) is one of the main complications of diabetes, and also the leading cause of the end-stage renal disease (ESRD).The main clinical manifestations are albuminuria and decreased glomerular filtration rate.DKD seriously affects the quality of life of sufferers and places a huge financial burden on them. Traditional Chinese medicine (TCM) has accumulated rich experience in treating DKD.This paper analyzed and summarized the recent treatment of DKD with traditional Chinese medicine from three aspects: active ingredients of TCM, TCM pairs and TCM prescriptions, so as to provide new ideas for the majority of researchers in experimental research.

Research progress of active ingredients of traditional Chinese medicine in the intervention of diabetic nephropathy by regulating mTOR signaling pathway / 中国药房

Diabetic nephropathy （DN） has become one of the main causes of end-stage renal disease，and its pathogenesis is still unclear. Currently，it is believed to be closely related to kidney injury mediated by various factors such as autophagy disorder under the condition of high glucose，oxidative stress and inflammation. Mammalian target of rapamycin （mTOR） signaling pathway is crucial for protein synthesis and autophagy regulation，which plays an important role in the occurrence and development of DN. In recent years，the research on the prevention and treatment of DN with traditional Chinese medicine （TCM） has made important progress. Plenty of evidence has shown that the active ingredients of TCM can enhance autophagy，improve oxidative stress and inflammation，inhibit cell apoptosis and abnormal proliferation by regulating mTOR signaling pathway，so as to relieve pathological changes in the kidney such as podocyte injury，glomerular basement membrane thickening，mesangial tissue abnormalities and renal tubule dysfunction，thereby reducing proteinuria and improving renal function. All of the above are of great significance for delaying the progression of DN. This article systematically summarizes the research progress of saponins，flavonoids，polyphenols，alkaloids， terpenoids and other active ingredients of TCM intervening in DN through mTOR signaling pathway，in order to provide some reference for further basic research and the development of new drugs.

Research on natural products from traditional Chinese medicine in the treatment of myocardial ischemia-reperfusion injury.

Myocardial ischemia-reperfusion injury (MIRI) is a complicated pathologic process that involves multiple factors including oxidative stress (free radical damage), inflammatory response, calcium overloading, and apoptosis in cardiomyocytes. According to Traditional Chinese Medicine (TCM), MIRI belongs to the categories of "chest numbness", "palpitations" and "angina pectoris". Present data indicate that the application of TCM in myocardial ischemia-reperfusion injury is promising and continues to attract research attention. While the efficacy of Chinese herbal medicine has been well-proven, the underlying molecular mechanisms remain elusive. The common proven mechanisms of Chinese herbal medicine in the treatment of MIRI include regulating lipid metabolism, protecting mitochondria, and improving energy metabolism, attenuating calcium (Ca2+) overload, scavenging oxygen free radicals, inhibiting apoptosis, and reducing autophagy. Others are the regulation of inflammatory cytokine expressions and healing of inflammatory lesions, modulation of cell signaling pathways, improvement of endothelial cell function, and protection of myocardial cells. In this review, we highlight recent studies that focus on elucidating these molecular mechanisms and the therapeutic effects of natural compounds deriving from TCM in MIRI, to ascertain the research progress made and the prospects in this field.

Research progress on antipyretic effect of Chinese medicine / 中国临床药理学与治疗学

Fever is a sign of infection and inflammatory diseases in the body. Persistent high fever will lead to cell degeneration, causing multiple organ dysfunction, and seriously affecting brain nerve and tissue function. Although the fever process is common and ordinary, its pathological mechanism involves multiple signaling pathways, such as nuclear transcription factor κB signaling pathway, Toll-like receptor 4 signaling pathway. A large number of studies have shown that traditional Chinese medicine compound and its active components can reduce serum inflammatory factors (TNF-α, IL-1β and IL-6) and hypothalamic thermoregulatory mediators (PGE

Recent advances of traditional Chinese medicine on the prevention and treatment of COVID-19.

Coronavirus disease-2019 (COVID-19) is a new highly infectious disease caused by a novel coronavirus. Recently, the number of new cases infected pneumonia in the world continues to increase, which has aroused great concern from the international community. At present, there are no small-molecule specific anti-viral drugs for the treatment. The high mortality rate seriously threatens human health. Traditional Chinese medicine (TCM) is a unique health resource in China. The combination of TCM and Western medicine has played a positive and important role in combating COVID-19 in China. In this review, through literature mining and analysis, it was found that TCM has the potential to prevent and treat the COVID-19. Then, the network pharmacological studies demonstrated that TCM played roles of anti-virus, anti-inflammation and immunoregulation in the management of COVID-19 via multiple components acting on multiple targets and multiple pathways. Finally, clinical researches also confirmed the beneficial effects of TCM on the treatment of patients. This review may provide meaningful and useful information on further drug development of COVID-19 and other viral infectious diseases.

Recent advances of traditional Chinese medicine on the prevention and treatment of COVID-19 / 中国天然药物

Coronavirus disease-2019 (COVID-19) is a new highly infectious disease caused by a novel coronavirus. Recently, the number of new cases infected pneumonia in the world continues to increase, which has aroused great concern from the international community. At present, there are no small-molecule specific anti-viral drugs for the treatment. The high mortality rate seriously threatens human health. Traditional Chinese medicine (TCM) is a unique health resource in China. The combination of TCM and Western medicine has played a positive and important role in combating COVID-19 in China. In this review, through literature mining and analysis, it was found that TCM has the potential to prevent and treat the COVID-19. Then, the network pharmacological studies demonstrated that TCM played roles of anti-virus, anti-inflammation and immunoregulation in the management of COVID-19 via multiple components acting on multiple targets and multiple pathways. Finally, clinical researches also confirmed the beneficial effects of TCM on the treatment of patients. This review may provide meaningful and useful information on further drug development of COVID-19 and other viral infectious diseases.

Anti-breast Cancer Mechanism of Active Ingredients of Traditional Chinese Medicine in Vitro / 中国实验方剂学杂志

Breast cancer mainly occurs in woman's mammary epithelial tissues, with a complex and unclear pathogenesis. The mortality rate is high and increasing year by year, and the patients become younger and younger, which seriously threatens woman's health. Therefore, it's urgent to find high-efficiency and low-toxicity medicines against breast cancer. The breast is not an essential organ for life support, but the cancer cells can easily fall off and metastasize throughout the body with blood or lymph fluid. It's a main cause of death. Surgery, radiotherapy, chemotherapy, molecular targeting, endocrine therapy, immunity therapy have certain limitations due to serious toxicity and side effects and the difficulty in controlling the invasion and metastasis of the cancer cell. In recent years, traditional Chinese medicine（TCM）has been widely studied and valued by researchers at home and abroad due to its unique advantages, such as multiple pathways, multiple targets, low toxicity and fewer side effects, and a lot of TCMs and their active ingredients with the anti-breast cancer activity have been studied by the researchers. Based on flavonoids, polyphenols, alkaloids, terpenes and other TCM ingredients, the mechanism in inhibiting breast cancer cell proliferation, inducing it apoptosis, inhibiting it invasion and migration in vitro were taken as the main content, which was supplemented by the summary of main relevant signal pathways targeted by the ingredients. This study reviewed the mechanism of ingredients in suppressing breast cancer in vitro by viewing and screening relevant literature at home and abroad in the past 10 years. The in-depth study of effective ingredients of TCM is expected to provide a reference for the development of effective targeting preparations for treating breast cancer. On the basis of in-depth excavation of active ingredients of TCM, relevant studies in the future are suggested to apply the ingredients of TCM acting on the same or similar pathways, factors, proteins, and make use of the basic theory of TCM, so as to achieve the effect in against breast cancer.

Advances in Mechanism of Traditional Chinese Medicines and Its Active Ingredients Treating Dyslipidemia / 中国实验方剂学杂志

Dyslipidemia is a disease of lipid metabolism. At present, the prevalence of dyslipidemia in adults in China is as high as 40.40%. In the United States, there are more than 100 million individuals with abnormal low-density lipoprotein cholesterol (LDL-C), and the incidence rate is increasing year by year and showing a trend of becoming younger. Dyslipidemia is closely related to a variety of diseases such as fatty liver, atherosclerosis , hypertension, coronary heart disease, diabetes, and stroke. It has now developed into a global public health problem that seriously threatens human life and health. Modern medicine believes that its pathogenesis is complicated and is related to abnormal glucose and lipid metabolism, insulin resistance (IR) and other factors. Chinese medicine ascribes it to primary asthenia-secondary sthenia syndrome, which is closely related to the liver, spleen, and kidney. It is believed that excessive fat and grease can cause phlegm and cause many diseases. In terms of its treatment, western medicine mainly uses statin chemical synthesis preparations, with stable therapeutic effect, but many adverse reactions such as myalgia, myositis, rhabdomyolysis and acute renal injury are the main factors restricting its clinical application. Traditional Chinese medicine (TCM) has a long history, and multi-pathway, multi-target, multi-level regulation of dyslipidemia, few adverse reactions and low drug dependence are the principal advantages of TCM in treating dyslipidemia. At present, there are more and more researches on the prevention and treatment of dyslipidemia by TCM, but they are mainly focused on the observation of curative effect and the summary of prescription, and there are relatively few in-depth discussion and summary of the mechanism of TCM. Through comprehensively retrieving and collating the relevant domestic and foreign literatures in the past five years, we reviews from the perspective of effective ingredients, therapeutic pathways, and targets of action, and comprehensively introduces the latest research progress of TCM on the mechanism of regulating dyslipidemia, and put forward some suggestions for the possible research direction in the future, in order to provide new ideas and theoretical basis for TCM in clinical prevention and treatment of this disease.

Binary code, a flexible tool for diagnostic metabolite sequencing of medicinal plants.

The principle of chromatographic fingerprint is that certain diagnostic metabolites should be always distributed in a given plant and currently, it has been widely accepted as a promising means for medicinal plant authentication. Moreover, the chemical profile is the only evidence to clarify the ingredients of those consumable plant products, e.g. traditional Chinese medicine (TCM) prescriptions. Herein, efforts were made to describe the diagnostic metabolome of medicinal plant or TCM prescription using a binary code sequence. Forty-five well-known medicinal plants along with six relevant prescriptions were employed for concept illustration and proof. Each plant was subjected to chemical characterization, and diagnostic metabolites of all plants were gathered into a chemical pool containing 595 compounds. A robust method enabling the detection of all 595 constituents was then developed using LC coupled to scheduled multiple reaction monitoring. Analyst™ software was responsible for automatically judging the presence (defined as "1") or absence (defined as "0") of each analyte with a defined signal-to-noise threshold (S/N > 100). After converting each medicinal plant to a binary sequence consisting of 595 codes, an in-house database was built by involving all sequences. The potentials of sequence library retrieval towards plant authentication, preliminary chemical characterization, and deformulation of TCM prescriptions were demonstrated after that the diagnostic metabolome of each test sample was translated to a binary code sequence. Above all, binary code is a flexible tool for diagnostic metabolite sequencing of medicinal plants, and it should be an alternative tool of DNA barcoding towards plant authentication.

Review of antidepressants in clinic and active ingredients of traditional Chinese medicine targeting 5-HT1A receptors.

Serotonin, which also named as 5-hydroxytryptamine (5-HT), is a neurotransmitter, which plays significant roles in a wide range of physiological and pathological processes. Depression is a complex disease that involves numerous factors, increasing evidences have showed that the level of 5-HT was lower in depressed patients and the administration of some selective serotonin re-uptake inhibitors exhibited antidepressant effects. The 5-HT1A receptor is a key protein in the brain serotonin system, modulating the release of 5-HT and other neurotransmitters. Behavioral and molecular biological studies have demonstrated that the differences of 5-HT1A receptor regulation was connected with depression and the responses to antidepressants. In this review, the authors will introduce the structure and function of 5-HT1A receptor and summarize some antidepressants targeting 5-HT1A receptor, including 5-HT1A receptor agonists and antagonists in a clinic, active ingredients of traditional Chinese medicine. And we found the major of drugs by targeting 5-HT1A receptor on the market or in clinical trials mostly have the similar functional groups, such as piperazine, piperidine, and pyrimidine. There are also some literatures found that these functional groups may be the site produce activity. So, we hope that it may provide basis and references for the research of the clinical drugs for depression.

[Method for active ingredients' in vivo target identification of traditional Chinese medicine using magnetic nanoparticles].

Target identification is an important prerequisite for the study of medicine action mechanism. Currently,drug target identification is mostly based on various cell models in vitro. However,the growth microenvironment,nutrition metabolism,biological properties as well as functions are quite different between in vitro cell culture and physiological environment in vivo; wherefore,it is a challenging scientific issue to establish an effective method for identifying drug targets in vivo condition. In this study,we successfully prepared a kind of magnetic nanoparticles( MNPs) which can be chemically modified by the hydroxyl structure of natural bioactive compound echinacoside( ECH) via the epoxy group label on the surface of MNPs. Therefore,organ-selective and recoverable nanoscale target-recognizing particles were prepared. We then intravenously injected the ECH-binding MNPs into rats and distributed them to specific organs in vivo. After cell endocytosis,ECH-binding MNPs captured target proteins in situ for further analysis. Based on this method,we discovered several potential target proteins in the spleen lysates for ECH,and preliminarily clarified the immuno-regulation mechanism of ECH. Collectively,our strategy developed a proof-of-concept technology using nanoparticles for in vivo target identification,and also provided a feasible approach for drug target prediction and pharmacological mechanism exploration.

[Application of active components from traditional Chinese medicine in treatment of inflammatory bowel disease].

Inflammatory bowel disease(IBD) is a non-specific and chronic recurrent autoimmune disease that involves the gastrointestinal tract. Clinical symptoms of intestinal bleeding, diarrhea, and weight loss threat to human health and induce colorectal cancer. The pathogenesis included living environment, genetic factors, immune cell infiltration and immune stress, weakened mucosal barrier defense and intestinal flora imbalance. At present, clinical treatment drugs mainly include aminosalicylic acid, corticosteroids, immunosuppressants, biological agents, etc., in view of the disadvantages of poor therapeutic effect and expensive price. The active ingredients of traditional Chinese medicine(TCM) in the treatment IBD have various biological activities and multiple targets such as anti-inflammatory, antibacterial, anti-tumor and immune regulation. This article summarized the application and the research progress in protecting intestinal epithelial barrier, maintaining intestinal microbial homeostasis, inhibiting causative factors, and regulating Th1/Th17/Treg balance about TCM in the treatment of IBD. The review provided new ideas for further development of the new drugs on the mechanism based on active ingredients of TCM in IBD treatment.

Application of active components from traditional Chinese medicine in treatment of inflammatory bowel disease / 中国中药杂志

Inflammatory bowel disease(IBD) is a non-specific and chronic recurrent autoimmune disease that involves the gastrointestinal tract. Clinical symptoms of intestinal bleeding, diarrhea, and weight loss threat to human health and induce colorectal cancer. The pathogenesis included living environment, genetic factors, immune cell infiltration and immune stress, weakened mucosal barrier defense and intestinal flora imbalance. At present, clinical treatment drugs mainly include aminosalicylic acid, corticosteroids, immunosuppressants, biological agents, etc., in view of the disadvantages of poor therapeutic effect and expensive price. The active ingredients of traditional Chinese medicine(TCM) in the treatment IBD have various biological activities and multiple targets such as anti-inflammatory, antibacterial, anti-tumor and immune regulation. This article summarized the application and the research progress in protecting intestinal epithelial barrier, maintaining intestinal microbial homeostasis, inhibiting causative factors, and regulating Th1/Th17/Treg balance about TCM in the treatment of IBD. The review provided new ideas for further development of the new drugs on the mechanism based on active ingredients of TCM in IBD treatment.

Method for active ingredients' in vivo target identification of traditional Chinese medicine using magnetic nanoparticles / 中国中药杂志

Target identification is an important prerequisite for the study of medicine action mechanism. Currently,drug target identification is mostly based on various cell models in vitro. However,the growth microenvironment,nutrition metabolism,biological properties as well as functions are quite different between in vitro cell culture and physiological environment in vivo; wherefore,it is a challenging scientific issue to establish an effective method for identifying drug targets in vivo condition. In this study,we successfully prepared a kind of magnetic nanoparticles( MNPs) which can be chemically modified by the hydroxyl structure of natural bioactive compound echinacoside( ECH) via the epoxy group label on the surface of MNPs. Therefore,organ-selective and recoverable nanoscale target-recognizing particles were prepared. We then intravenously injected the ECH-binding MNPs into rats and distributed them to specific organs in vivo. After cell endocytosis,ECH-binding MNPs captured target proteins in situ for further analysis. Based on this method,we discovered several potential target proteins in the spleen lysates for ECH,and preliminarily clarified the immuno-regulation mechanism of ECH. Collectively,our strategy developed a proof-of-concept technology using nanoparticles for in vivo target identification,and also provided a feasible approach for drug target prediction and pharmacological mechanism exploration.

[Advances in research on regulatory effects of chemical ingredients of traditional Chinese medicine on UDP-glucuronosyltransferase 1A1 expression and activity].

Uridine 5'-diphosphate-glucuronosyltransferase1A1(UGT1A1) is a major phase Ⅱ metabolism enzyme, responsible for glucuronidation and elimination of drugs and endogenous compounds, playing a vital role in sustaining endogenous metabolism balance. Therefore, changes in UGT1A1 expression/functional can not only cause adverse clinical drug/herbs-drug interactions, but also lead to metabolic disorder of endogenous substances, causing high blood bilirubin, bilirubin encephalopathy and liver injury, as well as other side effects. To date, many studies have found that a variety of clinical medicines and medicinal ingredients can regulate UGT1A1 activity. This article would summarize the advances in research on drug metabolism and toxicology in domestic and foreign literature, and investigate the regulatory effects of different types of traditional Chinese medicine(TCM) ingredients(such as flavonoids, coumarins, alkaloids) on UGT1A1 expression and activity, including inhibitory effect of TCM chemical ingredients on UGT1A1 and effect of TCM chemical ingredients on UGT1A1. It is hoped that this review could provide depth understanding and certain reference for the interaction between chemical ingredients of TCM and UGT1A1, which is of great significance to guide the rational clinical use in future.

[Characteristics of supramolecular imprinting template on liver meridian tropism of traditional Chinese medicine based on molecular connectivity index].

The molecular connectivity index was adopted to explore the characteristics of supramolecular imprinting template of herbs distributed to liver meridian, in order to provide scientific basis for traditional Chinese medicines(TCMs) distributed to liver meridian. In this paper, with "12th five-year plan" national planning textbooks Science of Traditional Chinese Medicine and Chemistry of Traditional Chinese Medicine as the blueprint, literatures and TCMSP sub-databases in TCM pharmacology of northwest science and technology university of agriculture and forestry were retrieved to collect and summarize active constituents of TCM distributed to liver meridian, and calculate the molecular connectivity index. The average molecular connectivity index of ingredients distributed to liver meridian was 9.47, which was close to flavonoid glycosides' (9.17±2.11) and terpenes (9.30±3.62). Therefore, it is inferred that template molecule of liver meridian is similar to physicochemical property of flavonoid glycosides and terpenes, which could be best matched with imprinting template of liver meridian.

Characteristics of supramolecular imprinting template on liver meridian tropism of traditional Chinese medicine based on molecular connectivity index / 中国中药杂志

The molecular connectivity index was adopted to explore the characteristics of supramolecular imprinting template of herbs distributed to liver meridian, in order to provide scientific basis for traditional Chinese medicines(TCMs) distributed to liver meridian. In this paper, with "12th five-year plan" national planning textbooks Science of Traditional Chinese Medicine and Chemistry of Traditional Chinese Medicine as the blueprint, literatures and TCMSP sub-databases in TCM pharmacology of northwest science and technology university of agriculture and forestry were retrieved to collect and summarize active constituents of TCM distributed to liver meridian, and calculate the molecular connectivity index. The average molecular connectivity index of ingredients distributed to liver meridian was 9.47, which was close to flavonoid glycosides' (9.17±2.11) and terpenes (9.30±3.62). Therefore, it is inferred that template molecule of liver meridian is similar to physicochemical property of flavonoid glycosides and terpenes, which could be best matched with imprinting template of liver meridian.