ABSTRACT
The poor stability of the ligustilide (LIG) makes its quantitation in Angelica sinensis (AS) difficult. This study establishes a chemical conversion method for the determination of ligustilide content in AS and proposes a national pharmacopoeia standard. Mechanical agitation and sonication of a powdered AS extract in a methanol/cyprolamine mixture facilitated the stabilization and transformation of ligustilide. Using an external reference HPLC-DAD method, the cyclopropyl-ligustilide (LIGc) content in the mixture could be determined. The content of ligustilide was greater than 1.0% based on 144 AS specimens including 68 obtained from the originally planted areas of Qinghai and Gansu Province; 55 specimens were obtained from Minxian and Weiyuan County medicine markets, and 21 specimens for which the storage period reached or exceeded 1.5 years. According to the Hong Kong Chinese materis medica standards, the content of ligustilide in AS should not be lower than 0.6%. The developed method could also be applied to the quality control of other Chinese medicinal materials (such as Ligusticum chuanxiong) or Chinese patent medicines in which ligustilide is the main component.
ABSTRACT
Purpose To investigate the mutation rate of EGFR,KRAS,ALK and ROS1 in non-small cell lung cancer (NSCLC) and its association with clinical or pathological characteristics.Methods 86 NSCLC tissues were included.Fluorescence PCR was used to detect the EGFR,KRAS mutation and ALK,ROS1 fusion gene.The association between EGFR,KRAS,ALK and ROS1 gene and age,gender,smoking history,histological type,lymph node metastasis and other clinical pathological features were analyzed.Results The total mutation rate of the driver gene in NSCLC patients was 62.8％ (54/86).EGFR mutation rate was 76％ (41/54).KRAS mutation rate was 9.3％ (5/54).ALK gene fusion mutation rate was 13.0％ (7/54),and in one of the patients,EGFR 19 deletion mutation and ALK fusion co-exist.ROS1 gene fusion mutation was 3.8％ (2/54).EGFR gene mutation rate was higher in adenocarcinoma and female (P ＜ 0.05),but no significant association was found in age,smoking history and lymph node metastasis (P ＞0.05).KRAS,ALK,ROS1 genes had no obvious correlation with clinical pathological features (P ＞ 0.05).Conclusion The EGFR mutation and ALK fusion was rather high in patients with NSCLC.More attention should be paid to them.Though KRAS,ROS1 mutations and double mutations were low in NSCLC patients,they should not be ignored.
ABSTRACT
Isocorydine and its analogs were extracted from Dicranostigma leptopodum and Stephania yunnanensis through the method of natural products chemistry. Its derivatives were prepared by chemical structure modifications from isocorydine. MTT method was used to study the inhibitory effect of those compounds on the growth of HepG2, HeLa and MGC-803 cancer cell lines in vitro. The results showed that isocorydine and its analogs all have the growth inhibition for those cancer cell lines. This paper investigated the structure-activity relationship of isocorydine and its derivatives with anticancer activity in the aspect of stereochemical structure, functional groups positions of the compounds and the electron density of aromatic rings based on the single crystal diffraction structure and the molecular docking of EGFR and isocorydine.
ABSTRACT
Transforming technology for semi-synthesized isocorydione from the natural product ofisocorydine was studied. The factors affecting on the reaction yield were investigated. UV spectrophotometry was used to indicate the semi-synthesized yield of isocorydione. The optimum reaction conditions were determined as following: reacting for 12 h in the solution of sodium dihydrogen phosphate at pH 10, the temperature was 25 degrees C and the ratio of isocorydine to Fremy's radical was 1 : 2. Under the optimum conditions, the yield could reach up to 50.0%. The molecular structure of isocorydione was elucidated by X-ray single-crystal diffraction analysis for the first time.