Research progress of anti-tumor effect and mechanism of CDDO and its derivatives / 中国药房

2-cyano-3，12-dioxooleana-1，9 （11）-dien-28-oic acid （CDDO） is a compound synthesized by taking oleanolic acid， a natural triterpene， as a precursor or precursor， and transforming three modifiable functional groups in the molecule through a series of chemical structure modification. In order to improve its anti-tumor activity， CDDO derivatives are further synthesized. In this paper， the research results of anti-tumor effects and mechanisms of CDDO and its derivatives in recent years are summarized. It is found that CDDO and its derivatives have a wide range of anti-tumor effects， and can show significant anti-tumor effects on breast cancer， pancreatic cancer， lung cancer and ovarian cancer at low concentrations such as micromole or even nanomole， among which CDDO methyl ester compound （CDDO-Me） and CDDO imidazolidinone compound （CDDO-Im） have the most obvious effects. CDDO and its derivatives exert anti-tumor activity mainly by inducing tumor cell apoptosis， and regulating metabolic reprogramming and immune microenvironment. The involved pathways mainly include Janus protein tyrosine kinase （JAK）/ signal transduction and transcription activation protein 3（STAT3） signal pathway， nuclear factor E2-related factor 2 （NRF2） signal pathway， phosphatidylinositol 3 kinase （PI3K）/protein kinase B （also known as Akt）/mammalian rapamycin target protein （mTOR） signal pathway， Wnt/β-catenin signal pathway， nuclear factor κB signal pathway.

Effects of different processing methods on content of flavonoids from Sophorae Fructus / 中草药

Objective: To compare the content of flavonoids from Sophorae Fructus by different processing methods. Methods: HPLC method with Zorbax Eclipse Plus C18 column (250 mm × 4.6 mm, 5 μm) was used in the experiment; Methanol-0.4% acetic acid was used as mobile phase, with gradient elution; Column temperature was set as 30℃; The flow rate was 1.0 mL/min and detection wavelength was 256 nm. Results: Genistin: crude (0.86%) > stir-frying with honey (0.67%) > carbonizing by stir-frying (0.48%); Rutin: crude (3.0%) > stir-frying with honey (2.2%) > carbonizing by stir-frying (0.88%); Sophoricoside: crude (8.08%) > stir-frying with honey (5.73%) > carbonizing by stir-frying (3.58%); Quercetin: crude (0.04%) < stir-frying with honey (0.05%) < carbonizing by stir-frying (0.12%); Genistein: crude (0.06%) < stir-frying with honey (0.08%) < carbonizing by stir-frying (0.21%); Kaempferide: crude (0.01%) < stir-frying with honey (0.02%) < carbonizing by stir-frying (0.54%). Conclusion: Among the flavonoids from Sophorae Fructus after processing, the content of flavonoid glycosides is reduced and the content of flavonoid aglycone is increased simultaneously, which may be related to the different functions of crude Sophorae Fructus, Sophorae Fructus stir-fried with honey, and Sophorae Fructus carbonized by stir-frying pieces.