A new megastimane sesquiterpenoid from the leaves of Cinnamomum cassia.

A new megastimane sesquiterpenoid, cassianol A (1), and five known analogues (2-6) were isolated from the leaves extract of Cinnamomum cassia. Their structures were elucidated by extensive spectroscopic methods and single-crystal X-ray diffraction analyses. All the isolates were isolated from C. cassia for the first time. The anti-inflammatory activities of compounds 1-6 were evaluated against nitric oxide (NO) production in LPS-induced RAW 264.7 mouse macrophages.

Nine new dichapetalin-type triterpenoids from the twigs of Dichapetalum gelonioides (Roxb.) Engl.

Nine previously undescribed dichapetalin-type triterpenoids (1-9), along with 12 reported compounds (10-21), were isolated from the twigs of Dichapetalum gelonioides. Their chemical structures were mainly elucidated by comprehensive analysis of HRMS, 1D and 2D NMR spectroscopic data. The absolute configuration of compound 1 was further determined based on single-crystal X-ray diffraction. In addition, a part of compounds were evaluated the effects of inhibitory NO production in LPS-induced RAW264.7 macrophages.

Metabolites from the endophytic fungus HP-1 of Chinese eaglewood.

AIM: To study the chemical constituents from the fermentation of the endophytic fungus HP-1 of Chinese eaglewood. METHODS: The chemical constituents were isolated by column chromatography on silica gel and Sephadex LH-20, and their structures were elucidated on the basis of spectroscopic analysis. RESULTS: Four compounds were isolated and identified as 3α, 3ß, 10ß-trimethyl-decahydroazuleno[6, 7]furan-8, 9, 14-triol (1), 4-hydroxyphenylacetic acid (2), 4-hydroxyphenethyl alcohol (3), and 5-hydroxymethyl-2-furancarboxaldehyde (4). CONCLUSION: Compound 1 was a new compound. Compound 2 showed antibacterial activity against Staphylococcus aureus.

Comparative bioavailability of ferrous succinate tablet formulations without correction for baseline circadian changes in iron concentration in healthy Chinese male subjects: a single-dose, randomized, 2-period crossover study.

BACKGROUND: Ferrous succinate is used for the treatment of iron deficiency anemia. Determining the bioavailability of iron products is a challenge, because iron is naturally present in the blood and some tissues. Therefore, bioequivalence evaluation of ferrous formulations can be affected by the presence of endogenous iron species. Little information regarding the pharmacokinetics of ferrous supplements is available in the healthy Chinese population. OBJECTIVES: The aim of the study was to assess the comparative bioavailability of 200-mg of a test (ferrous succinate,100 mg × 2, Hunan Huana Pharmaceutical Co., Ltd., Hunan, China) and reference (Sulifei, 100 mg × 2, Nanjing Jinling Pharmaceutical Co., Ltd., Nanjing, China) formulation in healthy Chinese male subjects. The study was conducted to meet Chinese State Food and Drug Administration regulatory requirements for approval of a generic formulation of ferrous succinate. METHODS: This study utilized a single-dose randomized, 2-period, crossover design with alternate assignment of subjects to treatment (a single 200-mg [100 mg × 2]) or reference formulation groups. Both groups underwent a 4-day diet equilibration before 2 days of treatment and, finally, a 4-day washout period for the bioequivalence study. Blood samples were collected at 8:00 am on every diet equilibration day, 0 (baseline), 1, 2, 3, 4, 4.5, 5, 6, 9, 12, 24, and 36 hours after drug administration. Iron concentrations were determined using an inductively coupled plasma mass spectrometry. Subjects in both groups were given a standardized diet, with known amounts of iron and calories. The formulations were assumed to be bioequivalent if the 90% CI ratios for C(max) were within 70% to 143% and AUC(0-last) were within 80% to 125%-criteria established by the Chinese Food and Drug Administration. Tolerability was monitored throughout the study by assessing clinical parameters (vital signs, chemistry laboratory) and subject reports. RESULTS: Twenty healthy Han Chinese male subjects (mean age, 26.8 years [range, 20-39 years]; weight, 61.9 kg [range, 52-72 kg]; body mass index, 21.5 kg/m(2) [range,19.1-23.8 kg/m(2)]; and baseline iron values, 1271 µg/L [range 1113-1429 µg/L]) were enrolled and completed the study. Without baseline correction for endogenous iron compound, the mean C(max) measurements of iron for the test and reference formulations were 2981 [621.1] and 3028 [707.4] µg/L, respectively; AUC(0-last) values were 48,460 [9242] and 48,390 [8420] µg/L/h, respectively; T(max) values were 4.3 [1.6] and 3.7 [1.3] hours. The 90% CIs for the ratios of C(max) and AUC(0-last) were 89.9% to 109.2% and 92.5% to 107.7%. No significant difference was found between groups with regard to pharmacokinetic parameters. Both test and reference formulations were well tolerated, with only 2 (10%) subjects who received the reference formulation complaining of mild heartburn that resolved after approximately 1 hour. Another subject (5%) complained of nausea 10 minutes after the test administration, which resolved within 2 hours. The relative bioavailability of the test-reference preparations was 101.6%. CONCLUSION: In this single-dose crossover study in healthy Chinese male subjects, the test and reference formulations of ferrous succinate 200-mg (100 mg × 2,) tablets met the criteria for assuming bioequivalence as defined by the Chinese Food and Drug Administration. Both formulations were well tolerated. Chinese Clinical Trials registration number: ChiCTR-TRC-11001646.

[Study on arsenic speciation changes in crude and processed traditional Chinese medicines by HPLC-ICP-MS].

A HPLC-ICP-MS method for simultaneous determination of As(III), As(V), MMA and DMA in traditional Chinese medicines (TCMs) was established, and the contents of As(III), As(V), MMA and DMA in a TCM with high total arsenic content (Cordyceps) and 5 crude and processed TCMs (Radix Astragali, Radix et Rhizoma Rhei, Radix Scutellariae, Radix Polygoni Multiflori and Radix Rehmanniae) were determined and analyzed. The method validation indicated that the correlative coefficients (r) for all speciations were bigger than 0.9984; the limits of quantitation (LOQ) were from 0.8 to 1.0 microg x L(-1); the reproducibility and stability were satisfactory with all RSDs less than 10%; the spiked recoveries ranged from 82.40% to 119.5%. The results of samples analysis showed that the inorganic arsenic (As(III) and As(V)) was the dominating speciation in the tested TCMs; MMA and DMA were not found in all plant resourced TCMs, but MMA was found in Cordyceps; all the tested TCMs indicated a content increasing of inorganic arsenic after processing.