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This work describes an immunochemical approach for the quality control of Panax ginseng and a pharmacological study of ginsenoside Re, a major bioactive constituent in P. ginseng, using an enzyme-linked immunosorbent assay. A hybridoma secreting monoclonal antibody against ginsenoside Re was produced by fusing splenocytes immunized with a ginsenoside Re-bovine serum albumin conjugate with the hypoxanthine-aminopterinthymidine-sensitive mouse myeloma SP2/0 cell line. The method, at an effective measuring range of 7.8-500 ng ⋅ mL-1 of ginsenoside Re, successfully detected ginsenoside Re in Chinese traditional herb prescriptions. The results demonstrate that we generated a novel and reliable assay system for measuring ginsenoside Re in Chinese medicines more efficiently. Futhermore, we determined the ginsenoside Re concentrations in the saliva of six healthy adults after the oral administration of a ginseng capsule to study the pharmacokinetics of ginsenoside Re in human saliva. [ABSTRACT FROM AUTHOR]

Four new hydroxycinnamic acid amides, scotanamines A-D (1-4), and seven known alkaloids, including N¹, N10-di-dihydrocaffeoylspermidine (5), scopolamine (6), anisodamine (7), hyoscyamine (8), anisodine (9), caffeoylputrescine (10), and N¹-caffeoyl-N³-dihydrocaffeoylspermidine (11), were obtained from the roots of Scopolia tangutica. The present study represents the first recognition of hydroxycinnamic acid amides containing putrescine or spermidine in S. tangutica. Compound 1, in particular, contains a moiety resulting from the condensation of nortropinone and putrescine. Compound 2 exhibited moderate agonist activity at the µ-opioid receptor (EC50 = 7.3 µM). Compound 2 was tested in vivo and induced analgesia analgesia in mice. The analgesic effect was recorded using the tail-flick assay and was reversed by naloxone. [ABSTRACT FROM AUTHOR]

Ergot alkaloids are toxins which are produced biotechnologically on an industrial scale. The chemical investigation of endophytic Aspergillus fumigatus resulted in the isolation of five new ergot alkaloids named fumigaclavines D-H (2-6), along with three known analogues, fumigaclavine C (1), festuclavine (7), and fumigaclavine A (8). Their structures were unequivocally elucidated by extensive spectroscopic analyses in association with X-ray single-crystal diffraction. Fumigaclavines D-H are interesting clavine-type ergot alkaloids featuring a reverse prenyl moiety at C-2, with 1-4, 6, and 8 bearing additional substituents, e.g., an OH or OAc group at C-9. Compounds 2, 4, and 6-8 showed a broad spectrum of antimicrobial activity against a panel of anaerobic microorganisms, of which compounds 4 and 6 were the most active against Veillonella parvula with an MIC = 16 µg/mL compared to that (0.12 µg/mL) of tinidazole, co-assayed as a positive reference. [ABSTRACT FROM AUTHOR]

Eight new triterpenoid saponins, oleiferosides A-H(1-8), were isolated from the EtOH extract of the roots of Camellia oleifera. Their structures were elucidated by a combination of 1D and 2D NMR techniques, mass spectrometry, and chemical methods. All were characterized to be oleanane-type saponins with sugar moieties linked to C-3 of the aglycone. Cytotoxic activities of these saponins were evaluated against four human tumor cell lines (A549, B16, BEL-7402, and MCF-7) by using the MTT in vitro assay. Compound 3 exhibited potent cytotoxic activitiy against all the tested cell lines with IC50 values < 10 µM. Compounds 1, 2, 4,a n d 5 showed moderate cytotoxic activities toward the tested cell lines. [ABSTRACT FROM AUTHOR]

Seven new cinchona alkaloids, cinchonanines A-G (1-7), and 29 known alkaloids were isolated from the barks of Cinchona surrirubra and C. ledgeriana collected from Yunnan Province in China. The new structures were elucidated by extensive spectroscopic analysis. All compounds were evaluated for their cytotoxicity against five human cancer cell lines. Compounds 2, 13, 14, and 15 showed moderate cytotoxicity. [ABSTRACT FROM AUTHOR]

Two new xanthones, 1,8-dihydroxy-3-methoxyxanthone 7-O-[α-L-rhamnopyranosyl(1→2)-β- D-glucopyranoside] (1) and 1,8- dihydroxy-3- methoxyxanthone 7-O-[α-L-rhamnopyranosyl (1→3)-α-L-rhamno-pyranosyl (1→2)-β-D-xylopyranoside] (2), together with 26 known xanthones (3-28), were isolated from the aqueous ethanol extract of the traditional Chinese herb Swertia mussotii. Their structures were elucidated via spectroscopic analyses including 2D NMR. The inhibition of α-glucosidase by the isolated xanthones was evaluated by an in vitro high-throughput screening assay. Our results indicated that 1,3,5,8-tetrahydroxyxanthone is the best inhibitor with an IC50 value of 5.33 ± 0.09 μM, while the O-glycosylated xanthones were poor α-glycosidase inhibitors. [ABSTRACT FROM AUTHOR]

Carya cathayensis is a fruit-bearing plant that belongs to the Juglandaceae family and is widely distributed throughout the world. It possesses various important biological activities. We have previously isolated an antitumor compound from the shell of C. cathayensis fruits and named it E2S ((E)-3-[(2S,3R)-2,3-dihydro-2-(4'-hydroxy-3'-methoxyphenyl)-3-hydroxymethyl-7-methoxy-1-benzo[b]furan-5-yl]-2-propenal). In this study, we investigated the antitumor activity of E2S against various human colorectal cancer cell lines (HCT116, HT29, SW480, LoVo). The results showed that E2S could significantly inhibit the growth of cancer cells in a dose-dependent manner, as well as disrupt the progression of the cell cycle. Mechanistic study revealed that E2S could decrease the protein levels of β-catenin and its downstream targets (such as c-myc, a key transcriptional target of β-catenin) in the cells. In addition, it also significantly suppressed β-catenin/TCF transcriptional activity. Taken together, the results suggested that E2S might partially exert an antiproliferative effect on human colorectal cancer cells by targeting β-catenin signaling, a finding that might potentially translate into a chemotherapeutic strategy for the treatment of cancer. It might also have implications for cancer prevention strategies. [ABSTRACT FROM AUTHOR]

Total steroid saponins isolated from Dioscorea zingiberensis have shown a variety of beneficial bioactivities. However, there are no reports about their neuroprotective effects, until now. Therefore, in the present study, we explored the neuroprotective effects of the total steroid saponins from D. zingiberensis on rats against transient focal cerebral ischemia-reperfusion and their underlying mechanisms. Healthy adult Sprague- Dawley rats were randomly assigned to six groups. After pretreatment with D. zingiberensis total steroid saponins intragastrically for six days, the rats were subjected to an ischemia injury by surgery on the middle cerebral artery occlusion for 90min. Compared to the ischemia-reperfusion group, the D. zingiberensis total steroid saponin group of rats, especially those given a 30-mg/ kg dose, showed not only a marked reduction in neurological deficit scores, cerebral infarct volume, and brain edema, but also an increase in neuron survival (Nissl bodies) in the hippocampal cornuammons 1 and cortex hemisphere of the ipsilateral ischemia. At the same time, the inflammatory cytokines in serum induced by themiddle cerebral artery occlusion were significantly decreased by the preadministration of D. zingiberensis total steroid saponins. Furthermore, the increase of caspase-3 was evidently reduced in the hippocampal cornuammons 1 and cortex of the hemisphere injured brain. Finally, the downregulating antiapoptotic Bcl-2 and upregulating proapoptotic Bax proteins were obviously suppressed. Taken together, the current findings suggest that D. zingiberensis total steroid saponins played a potential neuroprotective role against a severe injury induced by transient focal cerebral ischemic reperfusion in a rat experimental model, and this role may be mediated by its anti-inflammatory and antiapoptotic actions. [ABSTRACT FROM AUTHOR]

A novel heteroglycan, Cordyceps sinensis polysaccharide 1 (molecular weight 1 17 x 105 Da), was isolated and purified from mycelia of the fungus C. sinensis obtained by solid-state culture. Structural characterization by chemical analysis, GC-MS, FTIR, and NMR spectroscopy showed that C. sinensis polysaccharide 1 was mainly composed of (1→6)-linked α-D-Glc and α-D-Gal, with minor β-(1→4)-D-Xyl and β-(1→4)-D-Man residues probably located in the side chains with a trace amount of α-(1→3)-L-Rha residue. In biological assays, C. sinensis polysaccharide 1 significantly inhibited proliferation of sarcoma 180 cells and induced apoptosis in a dose-dependent manner. Further studies will elucidate the antitumor mechanism of C. sinensis polysaccharide 1 and promote its utilization for the development of novel, effective anticancer drugs. [ABSTRACT FROM AUTHOR]

Baicalin is a major bioactive component of Scutellaria baicalensis and a substrate of multiple drug resistance-associated protein 2. Expression of multiple drug resistance-associated protein 2 is regulated by NF-E2-related factor 2. The aim of this study was to explore whether ursodeoxycholic acid, an NF-E2-related factor 2 activator, could influence the oral bioavailability of baicalin. A single dose of baicalin (200 mg/kg) was given orally to rats pretreated with ursodeoxycholic acid (75mg/kg and 150 mg/kg, per day, intragastrically) or normal saline (per day, intragastrically) for six consecutive days. The plasma concentration of baicalin was measured with the HPLC method. The result indicated that the oral bioavailability of baicalin was significantly and dosedependently reduced in rats pretreated with ursodeoxycholic acid. Compared with control rats, the mean area under concentration-time curve of baicalin was reduced from 13.25±0.24mg/L h to 7.62±0.15mg/L h and 4.97±0.21mg/L h, and the Cmax value was decreased from 1.31±0.03 mg/L to 0.62±0.05mg/L and 0.36±0.04 mg/L in rats pretreated with ursodeoxycholic acid at doses of 75 mg/kg and 150 mg/kg, respectively, for six consecutive days. Hence, ursodeoxycholic acid treatment reduced the oral bioavailability of baicalin in rats, probably due to the enhanced efflux of baicalin from the intestine and liver by multiple drug resistance-associated protein 2. [ABSTRACT FROM AUTHOR]

The pharmacokinetics and anti-inflammatory effects of Sanhuang Xiexin Tang, composed of Rhei Radix et Rhizoma, Scutellariae Radix, and Coptidis Rhizoma, prepared by decoction and maceration, were investigated and compared. Rats were orally administered with the decoction and maceration of Sanhuang Xiexin Tang at 30 g/kg. The concentrations of 10 active constituents (berberine, palmatine, jatrorrhizine, coptisine, wogonin, baicalin, wogonoside, emodin, aloe-emodin, and rhein) in plasma were determined by UPLC-MS/ MS. Mice were orally administered decoctions and macerations of Sanhuang Xiexin Tang continuously for 7 days at three doses and stimulated with lipopolysaccharide. The plasma concentrations of IL-10 and TNF-α were determined by ELISA. Different preparation methods resulted in significant differences in the pharmacokinetic characteristics of the SXT constituents, especially the protoberberine alkaloids. Maceration decreased the absorption of flavones while promoting the absorption of anthraquinones. Bioavailability of both flavones and anthraquinones increased after administration of macerated Sanhuang Xiexin Tang, especially those of baicalin and rhein, which increased by 3.27 and 7.10 times. Results of ELISA indicated that both the decoction and maceration of Sanhuang Xiexin Tang could significantly increase IL-10 production (p < 0.01) as well as decrease TNF-α production (p < 0.01). Macerated Sanhuang Xiexin Tang has a slightly higher antiinflammatory effect than the Sanhuang Xiexin Tang decoction. Different preparation methods affected the pharmacokinetic characteristics and anti-inflammatory effects of Sanhuang Xiexin Tang's active constituents. [ABSTRACT FROM AUTHOR]

Praeruptorin A and praeruptorin C, racemic to each other, are main bioactive constituents of the species Peucedanum praeruptorum, traditionally used as a Chinese herbal medicine (also known as Bai-Hua Qian Hu). In the present study, the ability of praeruptorins A and C to activate the constitutive androstane receptor and induce human multidrug resistance-associated protein 2 expressions in HepG2 cells was investigated. The changes in mRNA level, protein expression, and transport activity of multidrug resistance-associated protein 2 were determined by quantitative real-time PCR, Western blot, and the CDF uptake assay, respectively. The effects of constitutive androstane receptor knockdown on multidrug resistance-associated protein 2mRNA and protein expression were also measured by transient transfection of a specific constitutive androstane receptor siRNA. The results showed that praeruptorin A and praeruptorin C significantly induced the multidrug resistance-associated protein 2mRNA and protein expression, and enhanced the transport activity of multidrug resistance-associated protein 2. A further study showed that mRNA and protein upregulation were attenuated by transient transfection of a specific constitutive androstane receptor siRNA, suggesting that the upregulation of multidrug resistance-associated protein 2 was mediated by the constitutive androstane receptor. Taken together, our findings indicate that praeruptorin A and praeruptorin C can significantly upregulate multidrug resistance-associated protein 2 expression via the constitutive androstane receptor-mediated pathway in vitro, and this should be taken as an herb-drug interaction. [ABSTRACT FROM AUTHOR]