Two cardenolide glycosides from the seed fairs of Asclepias curassavica and their cytotoxic activities / 中国天然药物

Two cardenolide glycosides, corotoxigenin 3-O-[β-D-glucopyranosyl-(1→4)-6-deoxy-β-D-glucopyranoside] (1) and coroglaucigenin 3-O-[β-D-glucopyranosyl-(1→4)-6-deoxy-β-D-glucopyranoside] (2), were isolated from the seed fairs of Asclepias curassavica. The structures of 1-2 were determined based on the combination of the analysis of their MS, NMR spectroscopic data and acid hydrolysis. The inhibitory effects of compounds 1 and 2 on human colorectal carcinoma cells (HCT116), non-small cell lung carcinoma cells (A549) and hepatic cancer cells (SMMC-7721) were evaluated. The results showed that both compounds 1 and 2 significantly inhibited the viability, proliferation, and migration of A549, HCT116 and SMMC-7721 cells, suggesting that compounds 1 and 2 can be applied in the treatment of lung, colon and liver cancers in clinical practice. This study may not only provide a scientific basis for clarifying the active ingredients in A. curassavica, but also help to understand its antitumor activity, which can promote the application of A. curassavica in clinical treatment of various cancers.

3, 4-seco-Labdane diterpenoids from the leaves of Callicarpa nudiflora with anti-inflammatory effects / 中国天然药物

Four new 3, 4-seco-labdane diterpenoids, nudiflopenes J-M, were isolated from the leaves of Callicarpa nudiflora along with six known compounds. The structures of these diterpenoids were determined by comprehensive spectroscopic analysis. All the isolated compounds were evaluated for their inhibitory effects on NO production in LPS-stimulated RPMs and RAW264.7 cells. The results suggest that nudiflopenes J-M and other four known compounds showed significant inhibitory effects against NO production comparable to the positive control dexamethasone.

Development of a hydrophilic interaction chromatography-UPLC assay to determine trigonelline in rat plasma and its application in a pharmacokinetic study / 中国天然药物

AIM@#Trigonelline (Tr) is the second most abundant alkaloid in coffee beans. This study developed an assay combining hydrophilic interaction chromatography with ultra performance liquid chromatography (HILIC-UPLC) for the quantification of Tr in rat plasma to determine its pharmacokinetic behavior.@*METHODS@#After the administration of Tr by gavage as well as intravenous injection and that of methanol extract of coffee beans (MECB) orally, blood samples from the experimental rats were analyzed using the HILIC-UPLC assay. Pharmacokinetic parameters were determined using the standard non-compartmental method and calculated using Practical Pharmacokinetic Program Version 87/97.@*RESULTS@#The HILIC-UPLC assay was validated with the linear range of 0.12-100 μg·mL(-1) and a lower limit of quantitation of 0.12 μg·mL(-1). Its accuracy, precision, recovery, and stability were within acceptable limits. The AUC(0-∞) (where AUC is the area under the plasma concentration-time curve) values were determined to be (4 066.83 ± 1 244.41) and (3 544.29 ± 908.80) min·μg·mL(-1) after Tr was orally and intravenously administered, respectively. It was (4 566.75 ± 1 435.64) min·μg·mL(-1) after MECB was orally administered. The absolute bioavailability of Tr alone reached 57.37%, whereas that of Tr in MECB was 64.42%. The relative bioavailability of the alkaloid was 112.29%.@*CONCLUSIONS@#The HILIC-UPLC assay for Tr determination is simple and accurate, and also exhibits good reproducibility. The bioavailability of stand-alone Tr and that of Tr in MECB were both good. Tr alone and that in MECB orally administered did not exhibit any significant difference.

Evaluation of Amberlite XAD-1600 resin-based purification of the bioactive components from Radix Paeoniae Alba and Rhizoma Curcumae Longae extracts by pharmacodynamic and toxicological models / 南方医科大学学报

<p><b>OBJECTIVE</b>To evaluate the pharmacodynamics and toxicicity of the major bioactive components extracted and purified from Radix Paeoniae Alba and Rhizoma Curcumae Longae using Amberlite XAD-1600 resin.</p><p><b>METHODS</b>Amberlite XAD-1600 was used to purify the bioactive components from the crude 75% ethanol extracts of the two herbs. The pharmacodynamic and toxic effects of the crude extracts and extract purified using XAD-1600 resin were comparatively examined with two acute inflammatory models, two pain models and acute toxicity test in vivo.</p><p><b>RESULTS</b>The anti-inflammatory and analgesic effects of the purified extract were significant stronger with lower toxicity than those of the crude ethanol extract.</p><p><b>CONCLUSION</b>Amberlite XAD-1600 resin allows efficient extraction and purification of the bioactive components from the two herbs.</p>

Absorption characteristics of ginsenoside Rb2 in Caco-2 cell monolayer / 南方医科大学学报

<p><b>OBJECTIVE</b>To determine the concentration of ginsenoside Rb(2) and study the absorption characteristics of ginsenoside Rb(2) in Caco-2 cell monolayer.</p><p><b>METHODS</b>LC-MS-MS was used to determine the concentration of ginsenoside Rb(2), and the apparent permeability coefficient (P(app)) of ginsenoside Rb(2) was calculated.</p><p><b>RESULTS</b>P(app(AP-BL)) was 3.27 x 10(-7) cm.s(-1), P(app(BL-AP)) was 3.16 x 10(-6) cm.s(-1), and the efflux ratio (P(app(BL-AP))/P(app(AP-BL))) was 9.63.</p><p><b>CONCLUSION</b>The absorption characteristics of ginsenoside Rb(2) in Caco-2 cell model have been demonstrated.</p>

Changes of dehydroandrographolide's contents of andrographis tablet in the process of production / 中国中药杂志

<p><b>OBJECTIVE</b>To recognize changes in the contents of ingredients of Andrographis Tablet in the process of production.</p><p><b>METHOD</b>Adopting TLCS, TLC, HPLC to detect effective contents of ingredients which are produced in every stage of process of Andrographis Table's production.</p><p><b>RESULT</b>Handling with the fresh Herba Andrographis according to current pharmacopeoia's technology, it showed that only dehyandrographolide can be detected. It indicated that the main factor that leads to chemical change is the heating process in the process of production.</p><p><b>CONCLUSION</b>Avoiding heating treatment or reducing heating treatment time is the main factor to protect the effective ingredients.</p>