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Acute lung injury (ALI) is a life-threatening condition with high morbidity and mortality, underscoring the urgent need for novel treatments. Monochasma savatieri Franch. (LRC) is commonly used clinically to treat wind-heat cold, bronchitis, acute pneumonia and acute gastroenteritis. However, its role in the treatment of ALI and its mechanism of action are still unclear. This study aimed to demonstrate the pharmacological effects and underlying mechanisms of LRC extract, and provide important therapeutic strategies and theoretical basis for ALI. In this study, a research paradigm of integrated pharmacology combining histopathological analysis, network pharmacology, metabolomics, and biochemical assays was used to elucidate the mechanisms underlaying the effects of LRC extract on LPS-induced ALI in BALB/c mice. The research findings demonstrated that LRC extract significantly alleviated pathological damage in lung tissues and inhibited apoptosis in alveolar epithelial cells, and the main active components were luteolin, isoacteoside, and aucubin. Lung tissue metabolomic and immunohistochemical methods confirmed that LRC extract could restore metabolic disorders in ALI mice by correcting energy metabolism imbalance, activating cholinergic anti-inflammatory pathway (CAP), and inhibiting TLR4/NF- κ B signaling pathway. This study showed that LRC extract inhibited the occurrence and development of ALI inflammation by promoting the synthesis of antioxidant metabolites, balancing energy metabolism, activating CAP and suppressing the α7nAChR-TLR4/NF- κ B p65 signaling pathway. In addition, our study provided an innovative research model for exploring the effective ingredients and mechanisms of traditional Chinese medicine. To the best of our knowledge, this is the first report describing the protective effects of LRC extract in LPS-induced ALI mice. [Display omitted] • Monochasma savatieri Franch. (LRC) exerted protective effects against LPS-induced acute lung injury (ALI) via various mechanisms. • Luteolin, isolactoside, and aucubin were effective components of LRC. • LRC protected against ALI by balancing energy metabolism and activating cholinergic anti-inflammatory pathway. • LRC inhibited α7nAChR-TLR4/NF- κ B p65 pathway to reduce the Inflammation in ALI. [ABSTRACT FROM AUTHOR]

Based on the theory of traditional Chinese medicine (TCM), diabetic cardiomyopathy (DCM) belongs to the category of " Xiaoke disease" according to the symptoms, and "stasis-heat" is the main pathogenesis of DCM. The Chinese medicine Anemarrhena asphodeloides Bunge (AAB), as a representative of heat-clearing and engendering fluid, is often used clinically in the treatment of DCM. Anemarrhena asphodeloides Bunge total saponins (RATS) are the main bioactive components of AAB, the modern pharmacologic effects of RATS are anti-inflammatory, hypoglycemic, and cardioprotective. However, the potential protective mechanisms of RATS against DCM remain largely undiscovered. The primary goal of this study was to explore the effect of RATS on DCM and its mechanism of action. Streptozotocin and a high-fat diet were used to induce DCM in rats. UHPLC/Q-TOF-MS was used to determine the chemical components of RATS. The degenerative alterations and apoptotic cells in the heart were assessed by HE staining and TUNEL. Network pharmacology was used to anticipate the probable targets and important pathways of RATS. The alterations in metabolites and main metabolic pathways in heart tissue were discovered using 1 H-NMR metabolomics. Ultimately, immunohistochemistry was used to find critical pathway protein expression. First of all, UHPLC/Q-TOF-MS analysis showed that RATS contained 11 active ingredients. In animal experiments, we found that RATS lowered blood glucose and lipid levels in DCM rats, and alleviated cardiac pathological damage, and decreased cardiomyocyte apoptosis. Furthermore, the study found that RATS effectively reduced inflammatory factor release and the level of oxidative stress. Mechanistically, RATS downregulated the expression levels of PI3K, AKT, HIF-1α, LDHA, and GLUT4 proteins. Additionally, glycolysis was discovered to be a crucial pathway for RATS in the therapy of DCM. Our findings suggest that the protective effect of RATS on DCM may be attributed to the inhibition of the PI3K/AKT/HIF-1 α pathway and the correction of glycolytic metabolism. [Display omitted] • We found for the first time that the Anemarrhena asphodeloides Bunge total saponins could improve diabetes cardiomyopathy. • We discuss the chemical composition, pharmacological action, and mechanism of Anemarrhena asphodeloides Bunge total saponins. • We found that Anemarrhena asphodeloides Bunge total saponins could improve diabetes cardiomyopathy by regulating glycolytic metabolism. • We provide theoretical guidance for the application of Anemarrhena asphodeloides Bunge total saponins in modern medicine. [ABSTRACT FROM AUTHOR]

YMR-65​, 5-(5-bromo-1-methyl-1H-indol-3-yl)-3-(3-methoxyphenyl)-4, 5-dihydro-1H-pyrazole-1-carboxamide, is a potential tubulin inhibitor exhibiting good anticancer activity. In our study, we illustrated the biological activities in HepG2 cells and the pharmacodynamic and pharmacokinetic profiles were evaluated in murine H22 hepatoma-bearing mice. Molecular docking assay and colchicine competition assay indicated that YMR-65 could bind tightly to the colchicine binding site of tubulin. Further investigation demonstrated that YMR-65 arrested cells in the G2/M phase of cell cycle and induced apoptosis in HepG2 cells. Compared with control group, the tumor growth inhibition determined by final relative volume of tumor/the initial tumor volume were 32.57%, 24.00% and 34.95%, respectively, for YMR-65 (10 mg/kg), YMR-65 (20 mg/kg) and CA4P (10 m/kg) groups. Besides there were no obvious body change or tissue damage (enhanced by histopathology study). YMR-65 administration at 10 and 20 mg/kg in H22 tumor-bearing mice resulted in 1.87- and 1.80-fold longer half time (t 1/2 ) and 0.36- and 0.78-fold lower area under concentration-time curve (AUC 0–∞ ) in plasma in contrast with normal mice at 10 mg/kg. Furthermore, YMR-65 showed a wide distribution to various tissues or tumor and the highest distribution index (the ratio of AUC tissue or tumor /AUC plasma ) was found in tumor, which implied that it might accumulate in tumor after administration. In brief, our results indicated that YMR-65 was a promising candidate with high antitumor efficacy and low tissue damage. [ABSTRACT FROM AUTHOR]

Chronic obstructive pulmonary disease (COPD) is the third leading cause of death globally and thus imposes heavy economic burden on patients, their families, and society. Furthermore, COPD seriously affects the quality of life of patients. The concept of "overall regulation" of traditional Chinese medicine (TCM) plays an important role in the prevention and treatment of COPD. Aim of the study: The objective of this review is to summarize the TCM theories, experimental methods, TCM extracts, active TCM ingredients, and TCM formulas for the treatment of COPD and reveal the effects and mechanisms of TCM treatments on COPD. This article reviewed literature on TCM-based treatments for COPD reported from 2016 to 2021. Relevant scientific studies were obtained from databases that included PubMed, China National Knowledge Infrastructure, Web of Science, Google Scholar, The Plant List, ScienceDirect, and SciFinder. This review summarized TCM-based theory, experimental methods, active ingredients, and potential toxicities, the effects of TCM extracts and formulations, and their mechanisms for the treatment of COPD. Most investigators have used in vivo models of cigarette smoke combined with lipopolysaccharide induction in rats and in vitro models of cigarette smoke extract induction. The active ingredients of TCM used for the treatment of COPD in relevant studies were triterpenoids, flavonoids, phenolics, quinones, glycosides, and alkaloids. TCMs commonly used in the treatment of COPD include antipyretic drugs, tonic medicines, anticough medications, and asthma medications. TCM can treat COPD by suppressing inflammation, reducing oxidative stress, inhibiting apoptosis, and improving airway remodeling. This review enriches the theory of COPD treatments based on TCM, established the clinical significance and development prospects of TCM-based COPD treatments, and provided the necessary theoretical support for the further development of TCM resources for the treatment of COPD. [Display omitted] [ABSTRACT FROM AUTHOR]