Marsdenia tenacissima injection induces the apoptosis of prostate cancer by regulating the AKT/GSK3β/STAT3 signaling axis / 中国天然药物

Marsdenia tenacissima injection, a standard Marsdenia tenacissima extract (MTE), has been approved as an adjuvant therapeutic agent for various cancers. Our previous study showed that MTE inhibited the proliferation and metastasis of prostate cancer (PCa) cells. However, the underlying mechanisms and active ingredients of MTE against PCa were not completely understood. This study revealed that MTE induced significant decreases in cell viability and clonal growth in PCa cells. In addition, MTE induced the apoptosis of DU145 cells by reducing the mitochondrial membrane potential and increasing the expression of Cleaved Caspase 3/7, Cyt c, and Bax. In vivo, DU145 xenografted NOD-SCID mice treated with MTE showed significantly decreased tumor size. TUNEL staining and Western blot confirmed the pro-apoptotic effects of MTE. Network pharmacology analysis collected 196 ingredients of MTE linked to 655 potential targets, and 709 PCa-associated targets were retrieved, from which 149 overlapped targets were screened out. Pathway enrichment analysis showed that the HIF-1, PI3K-AKT, and ErbB signaling pathways were closely related to tumor apoptosis. Western blot results confirmed that MTE increased the expression of p-AKTSer473 and p-GSK3βSer9, and decreased the expression of p-STAT3Tyr705in vitro and in vivo. A total of 13 compounds in MTE were identified by HPLC-CAD-QTOF-MS/MS and UPLC-QTOF-MS/MS. Molecular docking analysis indicated that six compounds may interact with AKT, GSK3β, and STAT3. In conclusion, MTE induces the endogenous mitochondrial apoptosis of PCa by regulating the AKT/GSK3β/STAT3 signaling axis, resulting in inhibition of PCa growth in vitro and in vivo.

Validation of Microbial Limit Test for Compound Benzocaine Gel / 中国药师

Objective: To establish a microbial limit test method for compound benzocaine gel.Methods: According to the general principles of Chinese Pharmacopoeia (2015 edition), method applicable experiments were performed respectively for the routine method, neutralization method and dilution & neutralization method.Using the recovery ratio of test bacteria as the index, the medium of dilution & neutralization method was adopted in the total aerobic microbial count and total combined yeasts and molds count, and the neutralization method was used for the control bacteria detection.The neutralizing agents were polysorbate 80 and lecithin.Results: The method of dilution & neutralization could eliminate the bacteriostasis of the drug, and the recovery ratio of each test bacteria was within the range of 0.5-2.0, which was in line with the requirements of Chinese Pharmacopoeia.Escherichia coli, Pseudomonas aeruginosa and Staphylococcus aureus could be detected out in the positive control bacterial test,and bacteria were not detected out in the negative test.Conclusion: The method can be used for the microbial limit test for compound benzocaine gel.

Establishment of HPLC fingerprints of Cajanus cajan leaves and determination of two constituents / 中成药

AIM To establish the HPLC fingerprints of Cajanus cajan (L.) Millsp.leaves and to determine the contents of orientoside and luteolin.METHODS The analysis of 65％ methanol extract from C.cajan leaves was performed on a 25 ℃ thermostatic Agilent Zorbax SB-C18 column (4.6 mm ×250 mm,5 μm),with the mobile phase comprising of methanol-1％ acetic acid flowing at 1.0 mL/min in a gradient elution manner,and the detection wavelength was set at 260 nm.RESULTS There were twenty-one common peaks in ten batches of samples (S1-S10),whose similarities were more than 0.950,except for that of S3 (0.516).Orientoside and luteolin showed good linear relationships within the ranges of 0.089 5-3.960 μg and 0.015 5-0.408 μg,whose average recoveries were 99.43％ (RSD =1.32％) and 98.50％ (RSD =0.82％),respectively.The contents of two constituents in the samples from three growing areas (Guangdong,Yunnan and Hainan) showed obvious differences.CONCLUSION This simple,accurate and reproducible method can be used for the quality control of C.cajan leaves.

Determination of Feruloyltyramine in Pothi Chinensis Herba by HPLC / 中国药师

Objective: To develop an HPLC method for determining feruloyltyramine in Pothi chinensis herba. Methods: The HPLC determination was performed on a Thermo ODS-2 Hypersil column(250 mm × 4. 6 mm, 5 μm) with isocratic elution of metha-nol-0. 4% phosphoric (35:65) as the mobile phase. The flow rate was 1. 0 ml·min-1 . The column temperature was at 25℃, and the detection wavelength was set at 318 nm. Results: Feruloyltyramine showed good linearity,and the recovery was 99. 40% with RSD of 1. 44% (n =9). Conclusion: The method is quick, simple and reproducible, which can be used to control the quality of Pothi chinensis herba.

Protective Effects of (-)-Epigallocatechin Gallate on Daunorubicin-induced Cardiotoxicity in Mice / 医药导报

Objective To investigate the protective effects of (-)-epigallocatechin gallate ( EGCG ) on daunorubicin ( DNR)-induced cardiotoxicity in mice. Methods The qualified mice were randomly divided into four groups:normal control group, myocardial injured model control group,high dose group (80 mg·kg-1 ) and low dose group (40 mg·kg-1 ) of EGCG. EGCG was administered intragastrically once daily for 7 days,followed by a single intraperitoneal injection of DNR (15 mg·kg-1 ) except in the normal control group. The electrocardiogram,myocardial enzymes and TNT-Hs in serum,cardiac ultrastructure of mice were detected after 48 h. Results In DNR model control group,the incidence of arrhythmia was 64. 7%. The activity of serum cardic enzymes including CK,CK-MB,LDH,α-HBDH and ALT,AST, level of TNT-Hs were significantly higher than those in the normal control group(P<0. 01),and myocardial ultrastructure was injured remarkably. The incidence of arrhythmia was 44. 4% in mice treated with high dose of EGCG and 31. 6% in mice with low dose of EGCG. Compared to the model control group, the activity of CK,CK-MB,LDH,α-HBDH and ALT,AST, level of TNT-Hs in serum decreased remarkably in EGCG groups( P<0. 05 or P<0. 01). Low can EGCG alleviated the injury to the ultrastructure of myocardium compared to the model control group. Conclusion EGCG can prevent the cardiac toxicity induced by DNR in mice.

Determination of Pd-Ⅰa and Pd-Ⅱ in Peucedanum praeruptorum by GC / 中国药学杂志

OBJECTIVE　To establish a GC method for the determination of the contents of Pd-Ⅰa and Pd-Ⅱ in roots of Peucedanum Praeruptorum.METHODS　The determination was performed on a silica capillary SE-30(0.25 μm 0.22 mm×25 m)column by FID detector;with n-C25H52 as the internal standard.RESULTS　The standard curves of Pd-Ⅰa and Pd-Ⅱ were linear over the range from 0.175 μg to 1.919 μg(r=0.9995) and 0.086 μg to 0.950 μg (r=0.9996),respectively.The average recoveries were (98.28±2.07)% for Pd-Ⅰa and (99.58±2.44)% for Pd-Ⅱ.Compared with HPLC,there was no significant difference in the results between GC and HPLC.CONCLUSION　The method appeared to be simple,sensitive,rapid and accurate and can be used for the quality control of Chinese medicine Qianhu.