Updating the therapeutic role of ginsenosides in breast cancer: a bibliometrics study to an in-depth review.

Breast cancer is currently the most common malignancy and has a high mortality rate. Ginsenosides, the primary bioactive constituents of ginseng, have been shown to be highly effective against breast cancer both in vitro and in vivo. This study aims to comprehensively understand the mechanisms underlying the antineoplastic effects of ginsenosides on breast cancer. Through meticulous bibliometric analysis and an exhaustive review of pertinent research, we explore and summarize the mechanism of action of ginsenosides in treating breast cancer, including inducing apoptosis, autophagy, inhibiting epithelial-mesenchymal transition and metastasis, and regulating miRNA and lncRNA. This scholarly endeavor not only provides novel prospects for the application of ginsenosides in the treatment of breast cancer but also suggests future research directions for researchers.

UPLC-Q-TOF-MS/MS-based urine metabolomics studies on the toxicity and detoxication of Tripterygium wilfordii Hook. f. after roasting.

Tripterygium wilfordii (TW), a well-known traditional Chinese medicine, was widely used in the treatment of autoimmune disorders and inflammatory diseases. However, the clinical use of TW was limited by severe toxicities, such as hepatotoxicity and nephrotoxicity. Our previous studies indicated that roasting was an effective approach for reducing TW-induced toxicity. After roasting, celastrol was completely decomposed, partially converted into 1-hydroxy-2,5,8-trimethyl-9-fluorenone and the total alkaloids content were significantly reduced. However, the detoxication mechanisms of roasting on TW were poorly unknown. This study aimed to explore the toxicity and detoxification mechanisms of TW after roasting based on urine metabolomics. Promising biomarkers were evaluated by multiple comparison analyses. Sixteen toxicity biomarkers were identified between control group and total extract group. Twelve toxicity biomarkers were identified between control group and total alkaloids group. Eight toxicity biomarkers were identified between control group and celastrol group. These metabolites were mainly involved in seven metabolic pathways, summarized as pentose and glucuronate interconversions, lipid metabolism (sphingolipid metabolism, glycerophospholipid metabolisms, fatty acid biosynthesis and steroid hormone biosynthesis) and amino acid metabolism (taurine and hypotaurine metabolism, tryptophan metabolism). After roasting, the toxicities of total extract, total alkaloids and celastrol were relieved by ameliorative serum parameters and pathological changes in hepatic and renal tissues which revealed that the reduction of celastrol and total alkaloids played important roles in the detoxification of roasting on TW. Furthermore, roasting regulated the levels of fourteen potential biomarkers in the total extract group, ten potential biomarkers in the total alkaloids group and seven candidate biomarkers in the celastrol group to normal levels. Biological pathway analysis revealed that roasting may ameliorate TW-induced metabolic disorders in pentose and glucuronate interconversions, lipid metabolism and amino acid metabolism. This study provided evidence for the application of roasting in TW.

Pseudotargeted metabolomics-based random forest model for tracking plant species from herbal products.

BACKGROUND: The "one-to-multiple" phenomenon is prevalent in medicinal herbs. Accurate species identification is critical to ensure the safety and efficacy of herbal products but is extremely challenging due to their complex matrices and diverse compositions. PURPOSE: This study aimed to identify the determinable chemicalome of herbs and develop a reasonable strategy to track their relevant species from herbal products. METHODS: Take Astragali Radix-the typical "one to multiple" herb, as a case. An in-house database-driven identification of the potentially bioactive chemicalome (saponins and flavonoids) in AR was performed. Furthermore, a pseudotargeted metabolomics method was first developed and validated to obtain high-quality semi-quantitative data. Then based on the data matrix, the random forest algorithm was trained to predict Astragali Radix species from commercial products. RESULTS: The pseudotargeted metabolomics method was first developed and validated to obtain high-quality semi-quantitative data (including 56 saponins and 49 flavonoids) from 26 batches of AR. Then the random forest algorithm was well-trained by importing the valid data matrix and showed high performance in predicting Astragalus species from ten commercial products. CONCLUSION: This strategy could learn species-special combination features for accurate herbal species tracing and could be expected to promote the traceability of herbal materials in herbal products, contributing to manufacturing standardization.

Comparison of Semen Aesculi species from different geographical origins and horse chestnut based on metabolomics and chemometrics analysis.

BACKGROUND: Semen Aesculi, a traditional Chinese herbal medicine, has a long history of use for treating chest and abdominal pain with distension. In addition, the horse chestnut (Aesculus hippocastanum L.) is another species of Aesculus in Europe and has notable clinical significance in alleviating chronic venous insufficiency, hemorrhoids, and postoperative edema. Thus, highlighting the comparative study of Semen Aesculi and horse chestnut may broaden clinical applications. OBJECTIVES: To conduct a comprehensive comparative analysis on the chemical profiling of these two varieties and determine whether they have equivalent clinical efficacy by integrating plant metabolomics and multivariate statistical methods. METHODS: Initially, a comprehensive characterisation was performed using ultra-performance liquid chromatography quadrupole time-of-flight tandem mass spectrometry (UPLC-QTOF-MS/MS) platform, and in total 44 active ingredients were identified. Then, untargeted metabolomics combined with principal component analysis (PCA) and partial least squares-discriminant analysis (PLS-DA) was applied for the discrimination of a German species and three official Chinese species. Next, 24 marker compounds responsible for the discrimination of different species were screened out and used to predict the species of unknown samples by genetic algorithm-optimised support vector machine (GA-SVM) with a high prediction accuracy. Finally, a heatmap visualisation was employed for clarifying the distribution of the identified active ingredients. RESULTS: The three species of Chinese Semen Aesculi showed distinct separation from each other, while European horse chestnut and Aesculus chinensis Bunge were similar in chemical composition. CONCLUSIONS: This work provided experimental evidence for further expanding the clinical application of Chinese Semen Aesculi and promoted the species identification and quality control of Semen Aesculi.

Pharmacological mechanism and therapeutic efficacy of Icariside II in the treatment of acute ischemic stroke: a systematic review and network pharmacological analysis.

BACKGROUND AND OBJECTIVE: Epimedii has long been used as a traditional medicine in Asia for the treatment of various common diseases, including Alzheimer's disease, cancer, erectile dysfunction, and stroke. Studies have reported the ameliorative effects of Icariside II (ICS II), a major metabolite of Epimedii, on acute ischemic stroke (AIS) in animal models. Based on network pharmacology, molecular docking, and molecular dynamics (MD) simulations, we conducted a systematic review to evaluate the effects and neuroprotective mechanisms of ICS II on AIS. METHODS: First, we have searched 6 databases using studies with ICS II treatment on AIS animal models to explore the efficacy of ICS II on AIS in preclinical studies. The literature retrieval time ended on March 8, 2022 (Systematic Review Registration ID: CRD42022306291). There were no restrictions on the language of the search strategy. Systematic review follows the Patient, Intervention, Comparison and Outcome (PICO) methodology and framework. SYCLE's RoB tool was used to evaluate the the risk of bias. In network pharmacology, AIS-related genes were identified and the target-pathway network was constructed. Then, these targets were used in the enrichments of Kyoto Encyclopedia of Genes and Genomes (KEGG) pathways and gene ontology (GO). Molecular docking and MD simulation were finally employed between ICS II and the potential target genes. RESULTS: Twelve publications were included describing outcomes of 1993 animals. The literature details, animal strains, induction models, doses administered, duration of administration, and outcome measures were extracted from the 12 included studies. ICS II has a good protective effect against AIS. Most of the studies in this systematic review had the appropriate methodological quality, but some did not clearly state the controlling for bias of potential study. Network pharmacology identified 246 targets with SRC, CTNNB1, HSP90AA1, MAPK1, and RELA as the core target proteins. Besides, 215 potential pathways of ICS II were identified, such as PI3K-Akt, MAPK, and cGMP-PKG signaling pathway. GO enrichment analysis showed that ICS II was significantly enriched in subsequent regulation such as MAPK cascade. Molecular docking and MD simulations showed that ICS II can closely bind with important targets. CONCLUSIONS: ICS II is a promising drug in the treatment of AIS. However, this systematic review reveals key knowledge gaps (i.e., the protective role of ICS II in women) that ICS II must address before it can be used for the treatment of human AIS. Our study shows that ICS II plays a protective role in AIS through multi-target and multi-pathway characteristics, providing ideas for the development of drugs for the treatment of AIS.

Chinese Medicine Syndrome Differentiation for Early Breast Cancer: A Multicenter Prospective Clinical Study.

Background: Chinese medicine (CM) syndrome differentiation is one of the fundamental principles that guide the practice of Chinese herbal medicine (CHM). CHM has been widely used among breast cancer patients. Contemporary literature varies in syndrome diagnosis, and there is a need to standardize syndrome differentiation according to the different stages of breast cancer treatment. This multicenter clinical study aims to identify the CM syndromes and the clinical signs and symptoms in women with early breast cancer. Methods: Participants who met the inclusion and exclusion criteria were interviewed during the five treatment stages: preoperative, postoperative, chemotherapy, radiation therapy, and endocrine therapy. Patient demographic data and CM syndrome (as recorded by the treating CM clinicians in medical records) were gathered. Signs and symptoms were analyzed using descriptive statistics to derive the standardized CM syndromes using hierarchical cluster analysis. Results: The analysis included 964 interviews with 620 participants enrolled between April 29, 2020 and May 30, 2021 from eight participating hospitals in China. The two most frequent syndromes recorded in medical records were dual deficiency of qi and blood, and dual deficiency of qi and yin during all but the preoperative stage. The symptoms of lassitude, lack of strength, and insomnia were common in all but the preoperative stage. Cluster analysis identified two clusters in the preoperative stage that most closely resembled the syndrome diagnoses of liver stagnation with congealing phlegm, and dual deficiency of the liver and kidney. Two clusters-dual deficiency of qi and blood, and dual deficiency of qi and yin-were common to multiple treatment stages. The syndrome cluster of spleen and stomach disharmony existed in both the postoperative and chemotherapy stages. Cluster analysis of the radiation therapy stage identified the unique syndrome of yin deficiency with fire toxin, while the endocrine therapy included the syndromes of liver depression and kidney deficiency. Conclusions: This multicenter clinical study showed consistency between results from cluster analysis and the most common syndromes recorded in the medical records. Findings from this clinical study will be further validated in a Delphi study to standardize CM syndromes for various stages of breast cancer treatment. Clinical Trial Registration: www.chictr.org.cn/index.aspx, identifier ChiCTR2000032497.

The efficacy and safety of Xihuang Pill/capsule in adjuvant treatment of breast cancer: A systematic review and meta-analysis of 26 randomized controlled trials.

ETHNOPHARMACOLOGICAL RELEVANCE: Xihuang Pill is a traditional Chinese medicine prescription for the treatment of breast cancer. There are many randomized controlled trials (RCTs) of Xihuang Pill in the treatment of breast cancer that have been published. Hence, a comprehensive systematic review and meta-analysis is needed. AIM: To evaluate the safety of Xihuang pill/capsule and its effect on the improvement of tumor progression, quality of life, immunity and prognosis in adjuvant treatment of breast cancer. METHODS: Chinese and English databases such as Sinomed, PubMed, Embase were searched to collect the RCTs of Xihuang pill/capsule in adjuvant treatment of breast cancer. Then the researchers extracted data from the RCTs that met the inclusion criteria, and used Cochrane standard risk bias to assess the quality of the data, and used Rev Man 5.3 statistical software for statistical analysis. RESULTS: A total of 26 RCTs with 2272 participants were included. The primary outcomes showed that Xihuang pill combined with chemotherapy and with endocrine therapy may suppress of tumor progression {Chemotherapy: risk ratio (RR) = 0.59, 95%Confidence interval (CI) [0.48,0.73], P < 0.00001; Endocrine therapy: RR = 0.56, 95%CI [0.33,0.96], P = 0.04}. Xihuang pill combined with chemotherapy, with endocrine therapy and with radiotherapy may improve the quality of life (chemotherapy: RR = 1.73, 95%CI[1.11, 2.70], P = 0.02; Endocrine therapy: RR = 1.18, 95%CI [1.01,1.38], P = 0.03; radiotherapy:RR = 1.51, 95%CI [1.01,2.27], P = 0.05). Xihuang pill combined with TCM + chemotherapy may decrease the inefficiency rate for clinical symptom improvement (RR = 0.50, 95%CI [0.28, 0.88], P = 0.02). Xihuang pill combined with chemotherapy may increase the Karnofsky Performance Scale (KPS) {Weighted Mean Difference (WMD) = 15.40, 95%CI [8.18, 22.62], P < 0.0001}. For adverse events, Xihuang pill combined with chemotherapy may alleviate adverse digestive events and leukopenia; Xihuang pill combined with endocrine therapy will not increase adverse events; Xihuang pill combined with non-antitumor therapy may reduce the incidence of leukopenia and red blood cell or hemoglobin reduction. CONCLUSION: The addition of Xihuang pill/capsule to breast cancer in conventional anti-tumor therapy may inhibit tumor progression, improve patient quality of life, reduce toxic reactions, regulate immunity, and reduce tumor markers. However, due to the overall low quality of RCTs, the research results need more high-quality RCTs to further test the conclusions.

An in-house database-driven untargeted identification strategy for deep profiling of chemicalome in Chinese medicinal formula.

Deep profiling of chemicalome in Chinese medicinal formulas is vital for disclosing the secret underlying their effectiveness. To address this issue, an in-house database-driven untargeted identification strategy was proposed with the use of ultra-performance liquid chromatography coupled to quadrupole time of flight mass spectrometry. Firstly, an in-house mass spectral database for the analyzed herbs was constructed, and database querying was performed for rapid recognition of known compounds. Secondly, a chemical diagnostic characteristics algorithm was originally developed for deep mining unrecorded ions, and thus expanding coverage of components beyond the database. Additionally, we proposed evaluation criteria for the untargeted identification of compounds with different confidence levels. As a case study, the integrated strategy was applied to comprehensively characterize complex multi-type components in Gegen-Qinlian Decoction. A total of 381 compounds were characterized and annotated with four different confidence levels, and 88.40% of these annotated compounds were successfully re-identified in triplicate analyses with a different instrument. The integrated strategy was demonstrated powerful in deep profiling of chemicalome in Chinese medicinal formulas with higher throughput, analytical sharpness, and lower omission ratios.

Liquiritigenin Blocks Breast Cancer Progression by Inhibiting Connective Tissue Growth Factor Expression via Up-Regulating miR-383-5p.

The objective of this study was to investigate the effect of liquiritigenin (LQ) on breast cancer (BC) and its mechanism. After BC cell lines and normal mammary epithelial cells were cultured with LQ, CCK-8, and Scratch, Transwell assays and flow cytometry were applied to test the effect of LQ on cell proliferation, migration, invasion, and apoptosis. The effect of LQ on the expression of microRNA-383-5p (miR-383-5p) and connective tissue growth factor (CTGF) was measured by qRT-PCR and Western blotting. Bioinformatics prediction was used to evaluate the binding relationship between miR-383-5p and CTGF, which was verified by dual-luciferase reporter assay. After miR-383-5p and/or CTGF expression was upregulated through cell transfection, the relationship between miR-383-5p and CTGF, as well as their effects on BC, was further assessed. The results showed that LQ can significantly inhibit CTGF expression and the proliferative, migratory, and invasive abilities of BC cells, while facilitating apoptosis of BC cells and miR-383-5p expression. The inhibiting effect of LQ was dose-dependently enhanced in BC cells. Dual-luciferase reporter assay verified that miR-383-5p targeted CTGF. CTGF expression was inversely regulated by miR-383-5p. CTGF upregulation repressed the suppressive effect of miR-385-5p on BC cell development. In conclusion, LQ can inhibit CTGF expression by upregulating miR-383-5p, thereby inhibiting proliferative, migratory, and invasive abilities and promoting apoptosis of BC cells.

Metabolomics Tools Assisting Classic Screening Methods in Discovering New Antibiotics from Mangrove Actinomycetia in Leizhou Peninsula.

Mangrove actinomycetia are considered one of the promising sources for discovering novel biologically active compounds. Traditional bioactivity- and/or taxonomy-based methods are inefficient and usually result in the re-discovery of known metabolites. Thus, improving selection efficiency among strain candidates is of interest especially in the early stage of the antibiotic discovery program. In this study, an integrated strategy of combining phylogenetic data and bioactivity tests with a metabolomics-based dereplication approach was applied to fast track the selection process. A total of 521 actinomycetial strains affiliated to 40 genera in 23 families were isolated from 13 different mangrove soil samples by the culture-dependent method. A total of 179 strains affiliated to 40 different genera with a unique colony morphology were selected to evaluate antibacterial activity against 12 indicator bacteria. Of the 179 tested isolates, 47 showed activities against at least one of the tested pathogens. Analysis of 23 out of 47 active isolates using UPLC-HRMS-PCA revealed six outliers. Further analysis using the OPLS-DA model identified five compounds from two outliers contributing to the bioactivity against drug-sensitive A. baumannii. Molecular networking was used to determine the relationship of significant metabolites in six outliers and to find their potentially new congeners. Finally, two Streptomyces strains (M22, H37) producing potentially new compounds were rapidly prioritized on the basis of their distinct chemistry profiles, dereplication results, and antibacterial activities, as well as taxonomical information. Two new trioxacarcins with keto-reduced trioxacarcinose B, gutingimycin B (16) and trioxacarcin G (20), together with known gutingimycin (12), were isolated from the scale-up fermentation broth of Streptomyces sp. M22. Our study demonstrated that metabolomics tools could greatly assist classic antibiotic discovery methods in strain prioritization to improve efficiency in discovering novel antibiotics from those highly productive and rich diversity ecosystems.

Exploring the Mechanism of Baicalin Intervention in Breast Cancer Based on MicroRNA Microarrays and Bioinformatics Strategies.

OBJECTIVE: To explore the mechanism of baicalin intervention in breast cancer based on microRNA microarrays. METHODS: The inhibitory rate of baicalin intervention in MCF-7 breast cancer cells was determined by MTT. Then, the miRNA microarrays were used to validate the key microRNAs. After that, reverse transcription-quantitative polymerase chain reaction (RT-qPCR) was used to validate microRNA, hsa-miR-15a, hsa-miR-100, hsa-miR-16, and hsa-miR-7t. Finally, the potential targets of these key microRNAs are predicted by miRWalk, and DAVID was utilized for gene ontology (GO) enrichment analysis and pathway enrichment analysis. RESULTS: Baicalin may inhibit the proliferation of MCF-7 cells in a dose-dependent and time-dependent manner. The concentration of baicalin 150 µmol/L was determined for the subsequent miRNA chip research. A total of 92 upregulated microRNAs and 35 downregulated microRNAs were obtained. The upregulated miRNAs include hsa-miR-6799-5p, hsa-miR-6126, hsa-miR-4792, hsa-miR-6848-5p, hsa-miR-3197, hsa-miR-6779-5p, and hsa-miR -654-5p. The downregulated miRNAs include hsa-miR-3911, hsa-miR-504-5p, hsa-miR-30a-3p, hsa-miR-193b-3p, and hsa-miR-181b-5p. Then, differentially expressed miRNA was verified by qRT-PCR. The results showed that the expression of hsa-miR-15a, hsa-miR-100, hsa-miR-16, and hsa-let-7c was upregulated (P < 0.05), which was consistent with the results of the miRNA microarray. The enrichment analysis showed that baicalin might regulate the DNA-templated proliferation, DNA-templated transcription, p53 signaling pathway, etc., of MCF-7 breast cancer cells through miRNA. CONCLUSION: Baicalin inhibits the proliferation of breast cancer cells. It may achieve antitumor effects through regulating microRNAs so as to affect the DNA replication (such as cellular response to DNA damage stimulus and DNA binding), RNA transcription (such as regulation of transcription, DNA-templated, transcription from RNA polymerase II promoter, and transcription factor binding), protein synthesis (such as mRNA binding, Golgi apparatus, and protein complex), endocytosis, pathways in cancer, p53 signaling pathway, and so on.

In silico production of relative correction factor for the quantitative analysis of multi-components by single marker method.

INTRODUCTION: Traditional methods to derive experimentally-generated relative correction factors (RCFs) for the quantitative analysis of herbal multi-components by single marker (QAMS) method require reference standards and multiple validations with different instruments and columns, which hampers high throughput implementation. OBJECTIVES: To effectively reduce the application amounts of raw material and provide higher and more stable accuracy, this study aimed to develop a method to computationally generate RCFs of herbal components. MATERIALS AND METHODS: This strategy included the published data collection, calibration curves screening, computer algorithm-based RCFs generation and accuracy validation. RESULTS: Using the in silico approach, we have successfully produced 133 RCFs for the multi-component quantitative analysis of 63 widely used herbs. CONCLUSION: Compared with conventional RCFs, this in silico method would be a low cost and highly efficient way to produce practical RCFs for the QAMS method.

Abdominal skin inflammation as an initial symptom of a perforating gastric foreign body: A case report.

RATIONALE: Foreign bodies are frequently ingested, but only approximately 1% of them cause perforation. Perforations in the lesser curvature of the stomach are exceedingly rare. Here, we report a case of gastric perforation in the lesser curvature caused by a foreign body. The patient presented to the clinic complaining of abdominal skin swelling and reddening with upper abdominal discomfort as the initial symptoms. PATIENT CONCERNS: An 83-year-old female presented with a mass in the middle of the epigastrium for 10 days. Physical examination found an apparent local tenderness and inflammatory mass in the upper abdominal wall. Her body temperature was normal (37.5°C) and the white blood cell count was elevated (8.12 × 10/L [reference value 3.5-9.5 × 10/L]). DIAGNOSES: The ultrasound examination of the abdomen revealed a 4 cm strip-like hyperechoic object entangled in the muscles of the abdominal wall. The computed tomography scan revealed a thin strip of bone-like hyperdense shadow. Intraoperative findings showed a sharp fishbone protruding from the lesser curvature of the stomach into the abdominal cavity, part of which remained in the gastric cavity. The postoperative pathological report revealed chronic suppurative inflammation with abscess and sinus canal formation. INTERVENTIONS & OUTCOMES: The patient underwent a gastric foreign body removal with partial gastrectomy. Anti-inflammatory treatment post-surgery rapidly relieved the patient's symptoms of discomfort in the upper abdomen. At the 1-month follow-up, the patient showed no discomfort in the upper abdomen and the inflammatory mass was no longer present. LESSONS: A foreign body had penetrated through the lesser curvature of the stomach, an area with a flat gastric wall, which occurs infrequently. In such cases, computed tomography is the gold standard for diagnosis of foreign bodies in the digestive tract. Ultrasound can also be used as a supplemental diagnostic technique. It is recommended that people who wear dentures should exercise caution while eating, especially when the food contains bones.

Effect of sulfur-fumigation process on ginseng: Metabolism and absorption evidences.

ETHNOPHARMACOLOGICAL RELEVANCE: Sulfur-fumigation has been developed to prevent insects and molds during post-harvest handling of Panax ginseng C.A. Mey (ginseng) in the near decades. Our previous study indicated sulfur-fumigation could transform ginsenosides, the active components of ginseng, into sulfur-containing derivatives (SFCDs), the artifacts with unknown toxicity. However, whether the biotransformation could be occurred and absorption characteristics between ginsenosides and SFCDs are still needed to further investigate. AIM OF THE STUDY: To evaluate the effect of sulfur-fumigation process on ginseng through comparing the metabolic profile and absorption characteristics between ginsenoside Rg1, Re and their SFCDs. MATERIALS AND METHODS: Intestinal microflora and liver S9 fraction were utilized to compare the metabolic profile, and single-pass intestinal perfusion and Caco-2 cell models were applied to compare the absorption characteristics, between Rg1, Re and their SFCDs. RESULTS: Rg1 and Re were metabolized to 7 none sulfur-containing metabolites, while their SFCDs were metabolized to 18 sulfur-containing metabolites. The intestinal absorption and transport of Rg1 and Re were much greater than their SFCDs. Besides, the uptakes of Rg1 and Re were transport-dependent, but their SFCDs were non-transport-dependent. CONCLUSION: Ginsenosides and their SFCDs could not be bio-transformed with each other and their absorption characteristics were quite different, which suggested that sulfur-fumigation is not a feasible post-harvest process of ginseng.

Chemical constituents from common vetch (Vicia sativa L.) and their antioxidant and cytotoxic activities.

Vicia sativa L. (common vetch) is a potential food source for both human beings and animals because of its abundant nutritional composition. There is a lack of phytochemical study on the whole plant, and thus the objective of this study was to investigate the isolation of phytochemicals and evaluate their biological activities. A new flavanol, (2R,3S)-3,3'-dihydroxy-4',7-dimethoxyflavanol (1), together with nine known compounds, two flavones (2-3), one coumarin (4), and six oleanane triterpenoids (5-10), was obtained from Vicia sativa L.. The structure of the new compound 1 was determined via its NMR spectra, IR and CD data. Compound 3 displayed the potential of the DPPH (1,1-diphenyl-2-picrylhydrazyl) radical scavenging effect in antioxidant test. In terms of cytotoxic activities, compound 3 showed moderate cytotoxic activities against three human tumor cells, especially HeLa cells.

Isopimarane-type diterpenoids from Croton laevigatus.

A new isopimarane-type diterpenoid, crolaevinoid A, along with four known analogues was isolated from the twigs and leaves of Croton laevigatus. The structures of the isolated compounds were established on the basis of NMR and MS spectroscopic analyses. The isolated compounds were examined the antibacterial activities. Unfortunately, the compounds showed no antibacterial activity against Micrococcus luteus, Methicillin-resistant Staphylococcus aureus, Aeromonas hydrophila, Klebsiella pneumoniae ssp pneumoniae, Acinetobacter Baumanii, and Escherichia coli.

Effects of chromatographic conditions and mass spectrometric parameters on the ionization and fragmentation of triterpene saponins of Ilex asprella in liquid chromatography-mass spectrometry analysis.

High performance liquid chromatography coupled with quadrupole-time-of-flight mass spectrometry (HPLC-QTOF-MS) is widely used to qualitatively characterize the chemical profiles of herbal medicines, in which the generated adducts and fragments are crucial for confirming molecular ion (deprotonated/protonated ion) and deducing structure of detected components. However, how chromatographic and mass spectrometric (LC-MS) conditions/parameters affect the quantity and intensity of adducts and fragments of detected components is scarcely concerned. In present study, three types of triterpene saponins from the root of Ilex asprella (RIA) were selected as a case study to systematically investigate the effects of LC/MS conditions/parameters on their ionization and fragmentation, so as to obtain higher intensity (higher detection sensitivity) and quantity (rich information) of adducts and fragments for the characterization of components in RIA. It was found that for LC conditions, methanol as organic phase was more benefit for generating more adducts with higher intensity; formic acid as a modifier suppressed the formation of [M-2H]2-, thus promoted the generation of other types of adducts at lower concentration but inhibited the generation when the concentration exceeded 0.1%. MS parameters affect scarcely the quantity but mainly intensity of adducts, cone voltage, source temperature and desolvation gas flow have relatively higher impacts when compared with other parameters. Collision energy affected both quantity and intensity of fragments. MS parameters at the medium value largely increased the quantity and intensity of adducts and fragments. Three-types of triterpene saponins presented structurally specific ionization and fragmentation due to their amounts of acidic substitutes. A total of 55 components were detected and definitely or tentatively identified in RIA under the optimized LC-MS conditions, among which 35 triterpene saponins were firstly discovered. This is the first report that proposes and validates a systematic approach for assessing the effects of LC/MS conditions/parameters on the ionization and fragmentation of analytes, which could be helpful for the optimization of LC-MS conditions for effective chemical profiling analysis of herbal medicines.

Paeonol: pharmacological effects and mechanisms of action.

Paeonia suffruticosa possesses various medicinal benefits and has been used extensively in traditional oriental medicine for thousands of years. Paeonol is the main component isolated from the root bark of Paeonia suffruticosa. The pharmacological effects of Paeonia suffruticosa are mostly attributed to paeonol. Paeonol injection has been successfully applied in China for nearly 50 years for inflammation/pain-related indications. Currently, the dosage forms of paeonol approved by China Food and Drug Administration include tablet, injection, and external preparations such as ointment and adhesive plaster. So far, the clinical applications of paeonol are mainly focusing on the anti-inflammatory activity. Studies of other pharmacological activities of paeonol are developing rapidly, and which may play an important role in the future. Besides, substantial mechanisms of pharmacological action of paeonol have been clarified in recent years. In this review, we summarize the pharmacological effects anti-inflammatory, neuroprotective, anti-tumor, anti-cardiovascular diseases and associated mechanisms of action of paeonol up to date.

Iridoid Derivatives with Cytotoxic Activity from Pedicularis uliginosa Bunge.

Three new iridoids, rel-(4aR,7S,7aS)-7-hydroxy-7-methyl-1,4a,5,6,7,7a-hexahydrocyclopenta[c]pyran-4-carbaldehyde (1), 1-methoxy-7-methyl-1,3,5,6-tetrahydrocyclopenta[c]pyran-4-carbaldehyde (2), and rel-(1R,4S,4aS,7R,7aR)-7-methylhexahydro-1,4-(epoxymethano)cyclopenta[c]pyran-3(1H)-one (3), together with seven known analogues, were isolated from the 95 % EtOH extract of the whole plants of Pedicularis uliginosa Bunge. Their structures were elucidated via extensive NMR spectroscopy and mass spectral data. In terms of inhibitory effects on human tumor cells, compounds 1, 2, 6, 7, and 8 exhibited better inhibitory activities against ACHN cells than the positive control (vinblastine).

Cancer survivorship: an integral part of Europe's research agenda.

Cancer survivorship has traditionally received little prioritisation and attention. For a long time, the treatment of cancer has been the main focus of healthcare providers' efforts. It is time to increase the amount of attention given to patients' long-term well-being and their ability to return to a productive and good life. This article describes the current state of knowledge and identifies research areas in need of development to enable interventions for improved survivorship for all cancer patients in Europe. The article is summed up with 11 points in need of further focus.