Design, synthesis and cytotoxic evaluation of novel betulonic acid-diazine derivatives as potential antitumor agents.

With the purpose to improve antiproliferative activity, 26 new betulonic acid-diazine derivatives were designed and synthesized from betulinic acid. The anticancer activity of these semi-synthetic compounds was evaluated by MTT assay in both tumor cell lines and normal cell line. The results indicated that majority of new compounds exhibited improved antitumor activity compared with the parent compound betulonic acid.

Hepatoprotective Effect of Against APAP-induced Liver Injury by Regulating Liver Lipid Metabolism and Apoptosis.

Acetaminophen (APAP) refers to a medication used to manage pain and fever symptoms, but it always causes liver injury when overdosed. Zhishi, dried young fruit of , is a famous herbal medicine in Asian countries which is rich in dietary phenolic substances. In this study, the mechanism of Zhishi protected against APAP-induced liver injury was studied more deeply by metabolomic strategy and pharmacological study.

Synergistic enhancement and hepatoprotective effect of combination of total phenolic extracts of Citrus aurantium L. and methotrexate for treatment of rheumatoid arthritis.

Rheumatoid arthritis (RA) is an autoimmune inflammatory disorder characterized by joint destruction and bone damage. Methotrexate (MTX) is recommended as the first-line disease-modifying agent for the treatment of RA. However, the clinical efficacy of MTX is limited due to its low response and side effects, especially hepatotoxicity.

[Metabolic and excretory process of Citri Reticulatae Pericarpium Viride and Citri Reticulatae Pericarpium in rats' urine and feces analyzed by RRLC-QqQ-MSn].

This present study was to investigate the metabolism and excretion of characteristic polyphenols such as flavonoids and coumarins in urine and feces of rats after intragastric administration of ethanol extracts of Citri Reticulatae Pericarpium Viride and Citri Reticulatae Pericarpium. The urine and feces of rats were collected after intragastric administration of 70% ethanol extracts of Citri Reticulatae Pericarpium Viride and Citri Reticulatae Pericarpium. Rapid resolution liquid chromatography coupled with quadrupole tandem mass spectrometry (RRLC-QqQ-MSn) was applied to compare the contents of polyphenols in ethanol extract, urine and feces.

Anti-inflammatory effects of Zhishi and Zhiqiao revealed by network pharmacology integrated with molecular mechanism and metabolomics studies.

Background: The inflammatory response has a complex pathogenesis; thus, it is a critical contributor to the development and complication of many diseases. Zhishi and Zhiqiao are famous Citrus herbal medicines that are rich in bioactive phenolic constituents with multiple anti-inflammatory activities.

Purpose: Establishment of a multi-component-target-pathway network strategy to investigate the usage of Zhishi and Zhiqiao on inflammatory diseases can provide a reference for mechanisms of traditional Chinese medicine (TCM).

Treatment of Rheumatoid Arthritis Using Combination of Methotrexate and Tripterygium Glycosides Tablets-A Quantitative Plasma Pharmacochemical and Pseudotargeted Metabolomic Approach.

Rheumatoid arthritis (RA) is a chronic inflammatory disease characterized by chronic destructive synovitis and is associated with progressive disability, systemic difficulties, premature death, and socioeconomic costs. Early intervention with disease-modifying antirheumatic drugs (DMARDs) like methotrexate (MTX) and its combination regimen would provide obvious benefits to patients, healthcare systems and society. MTX and tripterygium glycosides tablets (TGT) are most frequently prescribed medicines for RA, and the combination of them occurs frequently in anti-RA prescriptions.

Chemotaxonomic Classification Applied to the Identification of Two Closely-Related Citrus TCMs Using UPLC-Q-TOF-MS-Based Metabolomics.

This manuscript elaborates on the establishment of a chemotaxonomic classification strategy for closely-related fruits in Traditional Chinese Medicines (TCMs). UPLC-Q-TOF-MS-based metabolomics was applied to depict the variable chemotaxonomic markers and elucidate the metabolic mechanism of TCMs from different species and at different ripening stages. Metabolomics can capture a comprehensive analysis of small molecule metabolites and can provide a powerful approach to establish metabolic profiling, creating a bridge between genotype and phenotype.

[Study on HPLC fingerprint and chemical constituent difference of different species of Aurantii Fructus Immaturus].

This study is to establish an HPLC fingerprint by HPLC-DAD method and simultaneous quantitative analysis of 17 components of 18 batches of Citrus aurantium and 10 batches of C. sinensis. The separation was performed on an Agilent Poroshell 120 SB-C₁₈ (4.

Integrated and global pseudotargeted metabolomics strategy applied to screening for quality control markers of Citrus TCMs.

Traditional Chinese medicine (TCM) exerts its therapeutic effect in a holistic fashion with the synergistic function of multiple characteristic constituents. The holism philosophy of TCM is coincident with global and systematic theories of metabolomics. The proposed pseudotargeted metabolomics methodologies were employed for the establishment of reliable quality control markers for use in the screening strategy of TCMs.

Pharmaceutical prospects of naturally occurring quinazolinone and its derivatives.

Quinazolinones belong to a family of heterocyclic nitrogen compounds that have attracted increasing interest because of their broad spectrum of biological functions. This review describes three types of natural quinazolinones and their synthesized derivatives and summarizes their various pharmacological activities, including antifungal, anti-tumor, anti-malaria, anticonvulsant, anti-microbial, anti-inflammatory and antihyperlipidemic activities. In addition, structure-activity relationships of quinazolinone derivatives are also reviewed.

Preparation and quantification of the total phenolic products in Citrus fruit using solid-phase extraction coupled with high-performance liquid chromatography with diode array and UV detection.

Citrus fruit is an important health-promoting food that is rich in dietary phenolic metabolites. Traditional Chinese medicines, such as Zhishi and Zhiqiao, come from young and immature fruits of Citrus cultivars. The preparation of diversified bioactive phenolic products and establishment of the corresponding quality control methodology are challenging and necessary.

[Research on concentration of 5 different ginsenosides in Panax japonica collected from different cultivated geographic regions].

In this paper, an HPLC-QqQ-MS method for determination of 5 different ginsenosides of Panax japonica collected from different cultivated geographic regions was established. The separation was performed on a Zorbax XDB-C₁₈ (4.6 mm×100 mm, 1.

Citrus fruits as a treasure trove of active natural metabolites that potentially provide benefits for human health.

Citrus fruits, which are cultivated worldwide, have been recognized as some of the most high-consumption fruits in terms of energy, nutrients and health supplements. What is more, a number of these fruits have been used as traditional medicinal herbs to cure diseases in several Asian countries. Numerous studies have focused on Citrus secondary metabolites as well as bioactivities and have been intended to develop new chemotherapeutic or complementary medicine in recent decades.