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One novel naphthalene derivative, 2-octa-2′,4′,6′-atriynenaphthalene (1), together with eighteen known compounds (2–19) were isolated from the aerial parts of Dracocephalum moldavica L. Compounds 2, 8, 10, 13, 15–17 and 19 were obtained from the family Lamiaceae for the first time, and compounds 11 and 18 were firstly identified from the genus of Dracocephalum. All the isolates were evaluated for anti-complementary activities through the classical and alternative pathways, and the targets of the most active compounds on the complement activation cascade were also investigated. [ABSTRACT FROM AUTHOR]

Two new cassane-type derivatives (1–2), together with three known compounds (3–5), were isolated from the seed kernels of Caesalpinia sinensis. Their structures were elucidated on the basis of interpretation of comprehensive spectroscopic data, including HRESIMS and 1D/2D NMR spectroscopy, and the absolute configuration were established by means of ECD calculation. Compound 2, possessing a 16-degradative cassane skeleton, was rarely encountered in cassane diterpenoids isolated from the genus Caesalpinia. All compounds were evaluated for their anti-inflammatory activities against the overproduction of NO in LPS-stimulated RAW 264.7 macrophages, and compounds 1–5 could inhibit production of NO at the concentration of 50 μM. [ABSTRACT FROM AUTHOR]

1,8-Cineole (also known as eucalyptol) is mostly extracted from the essential oils of plants, which showed extensively pharmacological properties including anti-inflammatory and antioxidant mainly via the regulation on NF-κB and Nrf2, and was used for the treatment of respiratory diseases and cardiovascular, etc. Although various administration routes have been used in the application of 1.8-cineole, few formulations have been developed to improve its stability and bioavailability. This review retrospects the researches on the source, biological activities, mechanisms, and application of 1,8-cineole since 2000, which provides a view for the further studies on the application and formulations of 1,8-cineole. [ABSTRACT FROM AUTHOR]

The effects of coptisine against advanced stage of human pancreatic carcinoma PANC-1 cells was investigated in vitro. Coptisine (25–150 μM) treatment for 48 h caused dose-dependent cell growth inhibition by using CCK-8 assay. Additionally, coptisine was found to inhibit PANC-1 cells metastasis by the wound healing assay. Flow cytometry data indicated that coptisine (25–100 μM) exhibited dose-dependent G1 phase arrest and moderate reduction of S phase. Coptisine was also found to inhibit ERK phosphorylation and total ERK levels. Our research suggested that coptisine would be a potential therapeutic drug for the treatment of pancreatic cancer. [ABSTRACT FROM AUTHOR]

The rhizomes of the medicinal plant Hemsleya amabilis (Cucurbitaceae) yielded three new cucurbitane-type triterpene saponins xuedanosides K-M (1–3) by silica gel column, ODS column, and pre-HPLC techniques. The structure was determined by spectroscopic analysis and examined alongside existing data from prior studies. Compounds 1–3 were evaluated for cytotoxic activity against HeLa and HCT-8 human cancer cell lines and showed significant cytotoxicity with IC50 values of 2.01–14.56 and 8.94–27.48 μM, respectively. [ABSTRACT FROM AUTHOR]

Three new Lycopodium alkaloids (1–3), together with 15 known alkaloids, were isolated from club moss Lycopodium japonicum. Their structures were determined by extensive spectroscopic analysis, including 1D and 2D NMR spectra. Compound 1 has an unusual β-oriented methyl group substituted at C-15 and an α-hydroxy cyclopentenone moiety. All new alkaloids were evaluated for the inhibition of T-type calcium channel. [ABSTRACT FROM AUTHOR]

A series of lamiridosin A derivatives were synthesized through simple procedures. Their antitumor activities were evaluated against EC9706, MGC803, and B16 cell linesin vitro. Several compounds showed potent antitumor activity, especially compound10, with IC50value of 2.36 μmol/L against MGC803 cell lines, is more potent than marketed positive drug 5-fluorouridine (5-FU). [ABSTRACT FROM AUTHOR]

Curcumin, the biologically active compound from the rhizome of Curcuma longa, could inhibit cell growth and induce apoptosis in gastric carcinoma. However, the underlying mechanism of curcumin on gastric carcinoma cells still needs further investigation. In this study, morphological observation indicated that curcumin inhibited the proliferation of AGS cells in a dose-dependent manner. According to the flow cytometric analysis, curcumin treatment resulted in G2/M arrest in AGS cells, accompanied with an increased expression of cyclin B1 and a decreased expression of cyclin D1. In addition, DNA ladders were observed by gel electrophoresis. Meanwhile, the activities of caspase-3, -8, and -9 were also enhanced in curcumin-treated AGS cells. Nevertheless, the increased activities could be inhibited by benzyloxycarbonyl-Val-Ala-Asp (OME)-fluoromethylketone (z-VAD-fmk), which suggested that the apoptosis was caspase-dependent. Furthermore, downregulation of rat sarcoma (Ras) and upregulation of extracellular-signal-regulated kinase (ERK) were also observed in AGS cells treated with curcumin by Western blot. U0126, an ERK inhibitor, blocked curcumin-induced apoptosis. The results suggested that curcumin inhibited the growth of the AGS cells and induced apoptosis through the activation of Ras/ERK signaling pathway and downstream caspase cascade, and curcumin might be a potential target for the treatment of gastric carcinoma. [ABSTRACT FROM AUTHOR]

A new apiose-containing kaempferol trioside, kaempferol-3-O-α-l-rhamnosyl-(1‴ → 6″)-O-β-d-galactopyranosyl-7-O-β-d-apiofuranoside, along with 16 known compounds, were isolated from 50% acetone extract of Silphium perfoliatum L. Their structures were elucidated by acid hydrolysis and spectroscopic techniques including UV, IR, MS, 1H, 13C, and 2D-NMR. In addition, the pharmacological activity of compound 1 was tested with HepG2 and Balb/c mice (splenic lymphocytes and thymic lymphocytes) in vitro, and it exhibited inhibitory effect on the proliferation of HepG2 cells and showed the immunosuppressive activity. [ABSTRACT FROM AUTHOR]

In this study, two new compounds and six known compounds were isolated from the aerial parts ofPteris semipinnata.The chemical structures of these two new compounds were elucidated as 6β,11α-dihydroxy-15-oxo-ent-kaur-16-en-19-oic acid (1) and 7α,11α-dihydroxy-15-oxo-ent-kaur-16-en-19-oic acid (2) by the extensive spectral methods including 2D NMR and HR-MS techniques. [ABSTRACT FROM PUBLISHER]

Multidrug resistance (MDR) has been a major problem in cancer chemotherapy. In this study, the aim was to explore the reversal effect and its potential mechanism of rosmarinic acid (RA) on SGC7901/Adr cells. 3-(4,5-Dimethylthiazol)-2,5-diphenyl tetrazolium bromide (MTT) assay was used to investigate the reversal index of RA in SGC7901/Adr cell line. The intracellular accumulation of adriamycin, rhodamine123 (Rh123), and the expression of P-glycoprotein (P-gp) were assayed by flow cytometry. The influence of RA on the transcription of MDR1 gene was determined by reverse transcription-polymerase chain reaction. The results showed that RA could reverse the MDR of SGC7901/Adr cells, increase the intracellular accumulation of Adr and Rh123, and decrease the transcription of MDR1 gene and the expression of P-gp in SGC7901/Adr cells. These results indicated that RA was a potential multidrug resistance-reversing agent and warranted further investigations. [ABSTRACT FROM AUTHOR]

In this paper, the microbial transformation of desacetylcinobufagin (1) by Fusarium avenaceum AS 3.4594 was investigated, and four metabolites were isolated and characterized as 3-keton-desacetylcinobufagin (2), 3-epi-desacetylcinobufagin (3), bufadienolide A (4), and 15β,16α-dihydroxyl-17βH-bufalin (5), respectively. Among them, 4 and 5 are new compounds. The cytotoxicities of transformed products (2–5) against Hela cells were also investigated. [ABSTRACT FROM AUTHOR]

The main purpose of this study was to illustrate the effect of borneol on pharmacokinetics of salvianolic acid B (SalB) in rats after oral administration of SalB with different doses of borneol. The concentrations of SalB in rat plasma were determined by an established and validated LC-MS/MS method. Our data showed that when 20, 40, and 80 mg kg− 1 of borneol were orally administrated with SalB at 50 mg kg− 1, C max of SalB was increased by 18.4%, 55.8%, and 103.2% compared with that of SalB alone. And AUC0 − t of SalB in plasma was increased by 14.4%, 48.5%, and 123.3%, respectively. The results indicated that borneol is able to enhance the intestinal absorption and relative bioavailability of SalB, with a positive dose-dependent relationship. The described herb–drug interactions might prove the scientific rationality of the compatible ratio of traditional Chinese medicines. [ABSTRACT FROM PUBLISHER]