High-content screening (HCS) technology combines automated high-speed imaging hardware and single-cell quantitative analysis. It can greatly accelerate data acquisition in cellular fluorescence imaging and is a powerful research technique in traditional Chinese medicine (TCM). An increasing number of laboratories and platforms, including TCM laboratories, have begun utilizing HCS systems. However, this technology is still in its infancy in TCM research and there is a lack of sufficient experience with the associated concepts, instrument configurations, and analysis methods. To improve the understanding of HCS among researchers in the field of TCM, this paper summarizes the concept of HCS, software and hardware configuration, the overall research process, as well as common problems and related solutions of HCS in TCM research based on our team's previous research experience, providing several research examples and an outlook on future perspectives, aiming to provide a technical guide for HCS in TCM research.
Acupuncture is an effective treatment for ischemic stroke (IS) and plays a key role in neurological rehabilitation after IS. Acupuncture can improve the clinical symptoms of various complications after IS, including motor dysfunction, swallowing disorders, speech disorders, cognitive impairment, depression, insomnia, and fatigue. However, the mechanisms underlying the effects of acupuncture in IS remain unclear. Available evidence suggests that acupuncture may exert neuroprotective effects through neuroplasticity (neurogenesis and synaptogenesis), angiogenesis, cell proliferation and apoptosis, and regulation of oxidative stress, inflammation, and immunity. Further studies should be conducted to improve the high-quality evidence-based system of acupuncture intervention for IS, by focusing on the clinical and basic research design, increasing the sample size, standardizing and quantifying the standards of acupuncture operations, using multidisciplinary techniques and methods to systematically explore the key targets of acupuncture intervention for IS, and reveal the efficacy and mechanism of acupuncture in the treatment of IS.
Sepsis is a life-threatening inflammatory syndrome with high morbidity and mortality rates. However, options for sepsis are still limited to general treatment in intensive care units (ICUs), and effective therapies that improve sepsis survival are required. Immune disturbances play a vital role in the pathology of sepsis and are associated with protracted inflammation, susceptibility to infections, and death. Therefore, many investigators have focused on the potential benefits of immunomodulation therapy for sepsis. Electroacupuncture (EA) has been practiced in clinics for many years and has shown advantages in treating infectious diseases. Over the last few decades, our understanding of the efficacy and mechanisms of EA in sepsis has undergone considerable developments. We searched the literature regarding “CNKI, Wan Fang Data, VIP Database, PubMed, and Ingenta Connect” from 2010 to 2023, using the keywords “sepsis” “septic” and “electroacupuncture” and 336 sources were searched. Finally, we included 82 studies that targeted the immune system to determine EA's anti-inflammatory and immunomodulatory effects on sepsis. In this review, we found that EA has clinical benefits in relieving septic inflammation, improving immune function, and attenuating related multi-organ injury through several mechanisms, such as activation of the cholinergic anti-inflammatory pathway (CAP), vagal-adrenal axis, inhibition of the nuclear factor Kappa-B (NF-κB) signaling pathway, signal transducers and activators of transcription (STAT) signaling pathway, and improvement of immune cell function. Therefore, EA may be a promising complementary therapy for sepsis treatment. We also expect these data will contribute to further studies on EA in sepsis.
Traditional medicine has garnered significant global recognition, with an estimated 80% of the global population using it. Therefore, it is essential to fully understand the integration of traditional medicines into current healthcare systems. This review aims to provide a comprehensive overview of the standard process to modernize traditional medicine scientifically in the context of modern biomedicine, further termed here as “scientization”. Specifically, we aim to summarize the advancements made in understanding the efficacy, effectiveness, and underlying mechanisms of herbal medicine. We also examined the transition from experience- to evidence-based medicine during acupuncture. Furthermore, we explore the development of universal safety and quality control standards. Finally, we discuss international trade and export markets for Chinese medical products. The development and integration of traditional medicine have allowed it to further improve human health, resulting in a more comprehensive health solution for the global population.
Volatile oil (VO) is the main chemical component of common plants in Chrysanthemum genus, and it possesses several beneficial pharmacological properties, including bacteriostatic, antioxidant, anti-tumor, anti-inflammatory, antipyretic, analgesic, anti-osteoporotic, antihypertensive, sedative, and hypnotic effects. To date, research on the effective components of Chrysanthemum extract has mainly focused on flavonoids, whereas limited data are available on the chemical constituents and underlying mechanisms of action of the VO components. In this review, the pharmacological activities and mechanisms of VO are comprehensively reviewed with the aim of providing a foundation for further development for medicinal, aromatherapy, and diet therapy applications.
Objective: Celastrol is a pentacyclic triterpenoid extracted from the traditional Chinese medicinal herb, Tripterygium wilfordii. This study aims to provide a scientific basis for the rational development and use of celastrol in breast cancer.
Method: A quantitative chemical biology approach was used to investigate the protein targets and molecular mechanisms of celastrol in breast cancer cells.
Results: Low-concentration celastrol exerted an anti-tumor effect by directly binding to hydroxysteroid dehydrogenase-like 2 (HSDL2) and inhibiting its expression. Moreover, the expression of the pro-apoptotic protein, Bcl-2-associated X (BaX), increased, the level of the anti-apoptotic protein, B-cell lymphoma-2 (Bcl-2), decreased, and the rate of apoptosis increased. After the transfection of cells with si-HSDL2, the apoptosis rate was similar to that observed after the administration of celastrol. However, apoptosis was reversed by the overexpression of HSDL2. Furthermore, our mass spectrometry (MS) data indicated a relationship between HSDL2 and the mitogen-activated protein kinase (MAPK) signaling pathway. We also found that the expression of HSDL2 was directly related to the degree of extracellular signal-regulated kinase (ERK) phosphorylation.
Conclusion: Celastrol may promote apoptosis by suppressing the HSDL2/MAPK/ERK signaling pathway.
Objective: Gut-derived serotonin strongly inhibits bone formation by inhibiting osteoblast proliferation. Our previous study demonstrated that the lignan-rich fraction prepared from Sambucus willimasii Hance, a folk herbal medicine used to treat bone fractures and joint diseases in China, exerted bone-protective effects, and its actions were modulated by suppressing the synthesis of gut-derived serotonin via the inhibition of intestinal tryptophan hydroxylase 1 (TPH-1). However, there is no direct evidence for the action of lignans on TPH-1. This study aimed to verify the direct action of lignans on the TPH-1 and its influence on serotonin synthesis and bone properties.
Methods: Molecular docking and surface plasmon resonance were performed to determine the affinities of lignans to TPH-1. The cell viability and the protein activity and expression of TPH-1 were measured in RBL2H3 cells. The serum serotonin level and bone mineral density upon lignan treatment in ovariectomized mice were determined.
Result: The lignans showed high binding scores and binding affinities to TPH-1, inhibited the activity and protein expression of TPH-1, suppressed the serum serotonin levels in ovariectomized mice as well as promoted bone mineral density.
Conclusion: This is the first study to report that lignans are novel TPH-1 inhibitors and that these lignans could be potential agents for the management of serotonin-related diseases, including osteoporosis.
Objective: In this study, we aim to enhance the anti-prostate cancer efficacy of cabazitaxel (CTX) and reduce its immunosuppression and systemic toxicity by developing CTX-loaded liposomes modified with ginsenoside Rk1 (Rk1/CTX-Lip).
Methods: Physical and chemical properties of Rk1/CTX-Lip were investigated. We evaluated the biological functions of Rk1/CTX-Lip, both in vitro and in vivo. A subcutaneous prostate cancer (RM-1)-bearing mouse model was established to study the efficacy of Rk1/CTX-Lip inhibition in tumors. Simultaneously, a Candida albicans infection model was established in tumor-bearing mice to study the infection-relieving efficacy of Rk1/CTX-Lip. Finally, biocompatibility and in vivo safety of Rk1/CTX-Lip were evaluated.
Results: We successfully prepared Rk1/CTX-Lip, achieving high CTX encapsulation efficiency (97.24β±β0.75)% and physical stability. Rk1/CTX-Lip demonstrated evasion of macrophage phagocytosis, effective tumor tissue targeting, and a significant reduction (>50%) in average tumor volume compared with Chol/CTX-Lip. Moreover, it relieved the concurrent infection burden and effectively regulated immune organs and cells, demonstrating superior biocompatibility.
Conclusion: Rk1/CTX-Lip presents a promising new therapy for prostate cancer and holds potential for relieving concurrent fungal infections in cancer patients with low immunity.
Objective: Chronic fatigue syndrome (CFS) is a prevalent symptom of post-coronavirus disease 2019 (COVID-19) and is associated with unclear disease mechanisms. The herbal medicine Qingjin Yiqi granules (QJYQ) constitute a clinically approved formula for treating post-COVID-19; however, its potential as a drug target for treating CFS remains largely unknown. This study aimed to identify novel causal factors for CFS and elucidate the potential targets and pharmacological mechanisms of action of QJYQ in treating CFS.
Methods: This prospective cohort analysis included 4,212 adults aged ≥65 years who were followed up for 7 years with 435 incident CFS cases. Causal modeling and multivariate logistic regression analysis were performed to identify the potential causal determinants of CFS. A proteome-wide, two-sample Mendelian randomization (MR) analysis was employed to explore the proteins associated with the identified causal factors of CFS, which may serve as potential drug targets. Furthermore, we performed a virtual screening analysis to assess the binding affinity between the bioactive compounds in QJYQ and CFS-associated proteins.
Results: Among 4,212 participants (47.5% men) with a median age of 69 years (interquartile range: 69-70 years) enrolled in 2004, 435 developed CFS by 2011. Causal graph analysis with multivariate logistic regression identified frequent cough (odds ratio: 1.74, 95% confidence interval [CI]: 1.15-2.63) and insomnia (odds ratio: 2.59, 95% CI: 1.77-3.79) as novel causal factors of CFS. Proteome-wide MR analysis revealed that the upregulation of endothelial cell-selective adhesion molecule (ESAM) was causally linked to both chronic cough (odds ratio: 1.019, 95% CI: 1.012-1.026, Pβ=β2.75 e-05) and insomnia (odds ratio: 1.015, 95% CI: 1.008-1.022, Pβ=β4.40 e-08) in CFS. The major bioactive compounds of QJYQ, ginsenoside Rb2 (docking score: -6.03) and RG4 (docking score: -6.15), bound to ESAM with high affinity based on virtual screening.
Conclusions: Our integrated analytical framework combining epidemiological, genetic, and in silico data provides a novel strategy for elucidating complex disease mechanisms, such as CFS, and informing models of action of traditional Chinese medicines, such as QJYQ. Further validation in animal models is warranted to confirm the potential pharmacological effects of QJYQ on ESAM and as a treatment for CFS.
Licorice, a perennial herb of Leguminosa, is one of the oldest and most widely used herbal medicines worldwide. Its distinct sweet flavor and rich medicinal value make it an integral component of traditional Chinese medicine (TCM) formulations, which continue to be widely employed. The main chemical constituents of licorice include triterpenoid saponins, flavonoids, and polysaccharides. Experimental and clinical studies have demonstrated that various extracts and pure compounds derived from licorice exhibit a wide range of pharmacological properties including anti-inflammatory, antioxidant, antimicrobial, antiviral, antitumor, immune-regulatory, and neuroprotective activities. The bioactive constituents of licorice offer therapeutic benefits for cardiovascular and cerebrovascular diseases, diabetes mellitus, and liver disorders. This comprehensive review discusses the primary chemical constituents of licorice and their pharmacological activities, describes in vivo and in vitro models employed for studying licorice, and its potential targets and mechanisms of action. Furthermore, we discuss the toxicological profile, side effects, dosage recommendations, and clinical applications of licorice. This review aims to establish a foundation for further research on the safe and effective utilization of licorice while facilitating an in-depth exploration of its properties and fostering the development of novel therapeutic agents.