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OBJECTIVE ：To est ablish the method for the determination of 20（S）-protopanaxadiol（PPD）concentration in human plasma. METHODS ：Plasma samples were precipitated with acetonitrile and determined by UPLC-MS/MS ，using finandrogen as internal standard. The determination was performed on Waters ACQUITY UPLC HSS T 3 column with mobile phase consisted of 5 mmol/L ammonium bicarbonate aqueous solution-acetonitrile （gradient elution ）at the flow rate of 0.4 mL/min. The column temperature was set at 40 ℃，and sample size was 10 μL. The ion source was electrospray ion source，and negative ion scanning was carried out with multiple reaction monitoring mode . The ion pairs used for quantitative analysis were m/z 459.40→ 375.20（PPD）and m/z 371.30→315.30（internal standard ）. At the same time ，the method was applied to the determination of clinical samples. RESULTS ：The linear range of PPD was 0.25-30.00 ng/mL（r＝0.999 2），and the limit of quantitation was 0.25 ng/mL. RSDs of intra-batch and inter-batch were all lower than 10％，and relative errors （RE）were －14.61％-12.69％. Extraction method and matrix effect did not affect the quantitative determination of PPD. In ginsenoside CK 100 mg group ，ginsenoside CK 200 mg group and ginsenoside CK 300 mg group ，mean cmax of patients with rheumatoid arthritis after oral administration of corresponding drugs were 18.06，30.03，27.00 ng/mL；median tmax were 12.0，6.0，12.0 h；mean AUC 0-t were 622.52，668.15， 1 155.97 ng·h/mL. CONCLUTIONS ：The method for the determination of PPD concentration in human plasma is successfully established. The method is sensitive ，accurate， kq1907011） stable，easy to operate and less plasma consumption. It can be used for the quantitative determination of clinical samples.
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The intracellular calcium ions (Ca) act as second messenger to regulate gene transcription, cell proliferation, migration and death. Accumulating evidences have demonstrated that intracellular Cahomeostasis is altered in cancer cells and the alteration is involved in tumor initiation, angiogenesis, progression and metastasis. Targeting derailed Casignaling for cancer therapy has become an emerging research area. This review summarizes some important Cachannels, transporters and Ca-ATPases, which have been reported to be altered in human cancer patients. It discusses the current research effort toward evaluation of the blockers, inhibitors or regulators for Cachannels/transporters or Ca-ATPase pumps as anti-cancer drugs. This review is also aimed to stimulate interest in, and support for research into the understanding of cellular mechanisms underlying the regulation of Casignaling in different cancer cells, and to search for novel therapies to cure these malignancies by targeting Cachannels or transporters.
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Aim To study the anti-tumor effect of 20(S)-Protopanaxadiol(PPD)at different concentration on human liver cell line SMMC-7721 in vivo and in vitro.Methods The subcutaneous transplantable tumor model of human liver cancer in nude mice was established and the anti-tumor effect was calculated.Cell growth rate was determined with MTT assay.The apoptosis was analyzed by FITC-AnnexinⅤ/PI and Hoechst33342 staining method,and the activity of Caspase-3 was detected.Results In vivo,PPD could obviously inhibit the growth of transplanted tumor.In vitro,PPD induced inhibition of human liver cancer SMMC-7721 cells was time-dependent and dose-dependent.The apoptotic body was observed by Hoechst33342 staining.PPD could induce cell apoptosis of SMMC-7721,and the increase of Caspase-3 activity was observed in each PPD group.Conclusion PPD could inhibit the growth of human liver cancer SMMC-7721 cells in vivo and in vitro by up-regulating the activity of Caspase-3 and inducing the cell apoptosis.
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Objective To study the chemical components from the pericarps of Juglans mandshurica with anti-tumor activity.Methods It showed that pericarps of J.mandshurica had a good performance in treating cancer and low toxicity from CHCl3 and EtOAc portions by a lot of pharmacological experiments and modern clinical application in the past.Compounds were isolated by chromatography on silica gel columns and AB-8 macroporous resin.On the basis of spectral evidences including 1D-NMR and 2D-NMR,the structures of these compounds were determined.Results These compounds from CHCl3 portion were identified as 20(S)-protopanaxadiol-3-one(1),dammara-20,24-dien-3?-ol(2),galeon(3),juglanin A(4),2?,3?,23-trihydroxy olean-12-en-28-oic acid(5),2?,3?,23-trihydroxy urs-12-en-28-oic acid(6),oleanolic acid(7),ursolic acid(8).Conclusion Compound 1 is a new natural product.Compounds 2 and 5-8 are isolated firstly from the plants of Juglans L.which are due to pentacyclic triterpane.Compound 3 is isolated from the pericarps of J.mandshurica for the first time.