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Phytomedicine-14 May 2020
BackgroundIt is of utmost significance to choose the bioactive components as quality markers for ensuring the effectiveness of traditional Chinese medicine. Nonetheless, some markers are able to assess effectively the quality of TCM without considering the pharmacological mechanisms and intrinsic chemical complexities. ......
ObjectiveThis underscores the need to discover new and efficient markers which can assess both quality and mechanism of action. Herein, a strategy of bioactive-chemical quality markers combination was proposed to improve the level of the quality control of TCM by metabolomics coupled with chemometrics.......
Reference standards of typhaneoside, kaempferol-3-O-neohesperidoside, citric acid, linolenic acid, kaempferol-3-O-neohesperidoside, astragalin, naringenin, puerarin, and succinic acid with 98% purity on the basis of HPLC analysis were supplied by Chengdu Desite Biological Technology Co. Ltd. (Sichuan, China)
原文地址：https://www.sciencedirect.com/science/article/abs/pii/S0944711320300775?via%3Dihub
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Molecules-13 December 2019 coptisine
Alkaloids having acetylcholinesterase (AChE) inhibitory activity are commonly found in traditional Chinese medicine (TCM); for example, berberine from Coptis chinensis, galantamine from Lycoris radiata, and huperzine A from Huperzia serrata. In practice of TCM, Stephaniae Tetrandrae Radix (STR) is often combined with Coptidis Rhizoma (CR) or Phellodendri Chinensis Cortex (PCC) as paired herbs during clinical application. Fangchinoline from STR and coptisine and/or berberine from CR and/or PCC are active alkaloids in inhibiting AChE. The traditional usage of paired herbs suggests the synergistic effect of fangchinoline–coptisine or fangchinoline–berberine pairing in AChE inhibition. HPLC was applied to identify the main components in herbal extracts of STR, CR, and PCC, and the AChE inhibition of their main components was determined by Ellman assay. The synergism of herb combination and active component combination was calculated by median-effect principle. Molecular docking was applied to investigate the underlying binding mechanisms of the active components with the AChE protein. It was found that fangchinoline showed AChE inhibitory potency; furthermore, fangchinoline–coptisine/berberine pairs (at ratios of 1:5, 1:2, 1:1, and 2:1) synergistically inhibited AChE; the combination index (CI) at different ratios was less than one when Fa = 0.5, suggesting synergistic inhibition of AChE. Furthermore, the molecular docking simulation supported this enzymatic inhibition. Therefore, fangchinoline–coptisine/berberine pairs, or their parental herbal mixtures, may potentially be developed as a possible therapeutic strategy for Alzheimer’s patients.Keywords: acetylcholinesterase; fangchinoline; coptisine; berberine; synergistic effect
......coptisine (Lot DST170711-003,purity 99%) and epiberberine (Lot DST170711-109, purity 99%) were purchased from from Chengdu Desite Biological Technology Co. Ltd. (Sichuan, China).
原文地址：https://www.mdpi.com/1420-3049/24/24/4567
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Acta Pharmaceutica Sinica B-6 May 2020 Triptolide
The clinical application of triptolide (TPL) in tumor therapy has been greatly limited by its toxicity and inefficient delivery. Herein, a localized and sustained-release thermo-sensitive hydrogel was developed for the intra-tumor administration of TPL. Based on the amphiphilic structure of poly (N-isopropylacrylamide-co-acrylic acid)-g-F68 copolymer, it was able to form nano-micelles to efficiently encapsulate TPL, and then turn into a hydrogel at 37 °C. TPL@nano-gel exhibited a sustained drug release profile in vitro and a stronger anticancer effect caused by “two strikes”. The “first strike” was its enhanced cytotoxicity compared to free TPL, due to the enhanced pro-apoptosis effect observed in both MDA-MB-231 and MCF-7 cells caused by the regulation of endogenous mitochondrial pathways. Furthermore, TPL@nano-gel exhibited a “second-strike” through its anti-angiogenesis capabilities mediated through VEGFR-2 signaling inhibition. As expected, after intra-tumoral injection at a 0.45 mg/kg TPL-equivalent dose three times over 14 days in 4T1 tumor-bearing mice, TPL@nano-gel led to lower systemic toxicity and higher antitumor efficacy compared to multiple injections of TPL. In this regard, these findings indicate that this injectable thermo-responsive hydrogel carries great potential for TPL as a safe and effective cancer therapy.
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Triptolide (TPL) was purchased from Chengdu DeSiTe Biological Technology Co., Ltd. (Chengdu, China).
原文地址：https://www.sciencedirect.com/science/article/pii/S2211383520305967?via%3Dihub
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Isoliquiritigenin triggers developmental toxicity and oxidative stress–mediated apoptosis in zebrafish embryos/larvae via Nrf2-HO1/JNK-ERK/mitochondrion pathway
Isoliquiritigenin (ISL) is an emerging natural flavonoid found in the roots of licorice, exhibits antioxidant, anti-cancer, anti-inflammatory, anti-allergic, cardioprotective, hepatoprotective and neuroprotective properties. However, the effect of ISL in embryonic development is yet to be elucidated, and the mechanisms underlying its target-organ toxicity and harmful side effects are still unclear. In the present study, we employed zebrafish embryos to study the developmental toxicity effect of ISL and its underlying mechanisms. Zebrafish embryos upon treatment with either vehicle control (0.1% DMSO) or ISL solutions for 4–96 h post fertilization (hpf) showed that ISL exposure instigated severe developmental toxicity in heart, liver, and nervous system. Mortality and morphological abnormalities were also observed. High concentrations of ISL exposure resulted in abnormal phenotypes and embryonic malformations including pericardial edema, swim bladder defects, yolk retention, curved body shape and shortening of body length. Moreover, ISL exposure led to significant loss of dopaminergic neurons accompanied by reduced locomotor behaviour. Apoptotic cells were predominantly located in the heart area of 96 hpf embryo. Additionally, ISL significantly increased the levels of reactive oxygen species, lipid peroxidation content and decreased antioxidant enzyme activities. The expressions pattern of apoptosis-related genes Bad, Cyto c, Caspase-9, Caspase-3 and Bax/Bcl-2 indicated that the oxidative stress–induced apoptosis triggered by ISL suggest involvement of Nrf2-HO1/JNK-ERK/mitochondrion pathways. In conclusion, here we provide first evidence that demonstrate ISL-induced dose-dependent developmental toxicity in zebrafish embryos. Furthermore, gene expression patterns in the embryos correlate the above and reveal potential genetic mechanisms of developmental toxicity.......Isoliquiritigenin (ISL) is was purchased from Chengdu DeSiTe Biological Technology Co., Ltd. (Sichuan, China).
原文地址：https://www.sciencedirect.com/science/article/abs/pii/S0045653519329686?via%3Dihub
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Assessment of a developed HPLC-MS/MS approach for determining plasma eupatorin in rats and its application in pharmacokinetics analysis
Eupatorin, a bioactive compound extracted from Java tea (Orthosiphon stamineus), possesses potent anti-cancer, anti-inflammatory and vasodilation activities. To date, no pharmacokinetics studies on eupatorin have yet been performed. Here, we established and validated a sensitive and selective LC-MS/MS (liquid chromatography-tandem mass spectrometry) approach for determining plasma eupatorin in rats. Chromatographic fractionation was conducted on a Wonda Cract ODS-2 C18 Column (4.6 mm × 150 mm, 5 μm) with a mobile phase containing aqueous 0.1% formic acid and acetonitrile using a flow rate of 0.8 ml min−1. In multiple reaction monitoring mode, precursor-to-product ion transitions for quantification of eupatorin and the internal standard were set at 343.1 → 328.1 and 252.0 → 155.9, respectively. The intra- and inter-day precision and accuracy were found to be below 6.72% and within ±8.26% in rat plasma, respectively. Meanwhile, all values of the matrix effect, recovery and stability were within the accepted ranges. Furthermore, we carried out the pharmacokinetic analysis using the developed method. The pharmacokinetic study revealed that while the Cmax (maximum plasma concentration) of eupatorin and time for reaching the Cmax (Tmax) were 974.886 ± 293.898 μg L−1 and 0.25 h, respectively, the half-life was 0.353 ± 0.026 h. This study will be of great significance to the research on the pharmacology, clinical pharmacy and drug action mechanism of eupatorin.
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eupatorin （855-96-9）was purchased from Chengdu DeSiTe Biological Technology Co., Ltd. (Sichuan, China).
原文地址：https://pubs.rsc.org/en/Content/ArticleLanding/2020/RA/D0RA03350B#!divAbstract
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Frontiers in pharmacology-17 June 2020 geniposidic acid
Standard substances such as geniposidic acid, neochlorogenic acid, chlorogenic acid, caffeic acid, geniposide, genipin, pinoresinol di-o-glucopyranoside, syringaresinol di-o-glucopyranoside, isochlorogenic acid A, pinoresinol o-glucopyranoside, and isochlorogenic acid C were purchased from Chengdu Desite Bio-Technology Co., Ltd (Chengdu, China).
原文地址：https://www.frontiersin.org/articles/10.3389/fphar.2020.00838/full
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