Three new diterpenoids from whole herb of Carpesium cernuum / 中国中药杂志

The study investigated the chemical constituents from the whole herb of Carpesium cernuum. Three new diterpenoids were isolated from the whole herb of C. cernuum by column chromatography on silica gel, Sephadex LH-20, and semi-preparative HPLC. Their structures were identified by MS, NMR and other spectral techniques. The isolates were identified as(5Z)-2-oxo-2, 10, 14-trimethylhexadeca-5, 13-diene-11α, 18-diol(1),(2E, 10E)-7-[(acetyloxy)methyl]-3, 11, 15-trimethylhexadeca-2, 10, 14-triene-1, 12α-diol(2),(2E, 6Z)-3, 11, 15-trimethylhexadeca-2, 6, 14-triene-1, 12α, 19-triol(3), respectively. The cytotoxic activity of compounds 1-3 were investigated with DU-145, MCF-7, and A549 cells by MTT. The results showed that compound 1 and 3 had certain inhibitory effects on MCF-7 cells, with the inhibition rates of 45.06% and 29.40%, respectively.

Mannich bases derivatives of 2-Phenyl-5-Benzimidazole sulfonic acid; Synthesis, Characterization, Computational studies and Biological evaluation

Abstract A new series of N-Mannich bases of 2-Phenyl-5-benzimidazole sulfonic acid have been synthesized through amino methylation reaction with secondary amines. The two moieties were held together through a methylene bridge, which comes from formaldehyde (Formalin Solution 37%) used in the reaction. Chemical structures of the newly synthesized compounds have been confirmed using FT-IR, 1HNMR and 13CNMR. Different in vitro assays including Anti-oxidant, Enzyme inhibition, Anti-microbial and Cytotoxicity assay were performed to evaluate the biological potential with reference to the standard drug. Among the synthesized library, compound 3a shows maximum alpha-glucosidase inhibition with an IC50 value of 66.66 µg/ml, compound 3d was found most toxic with LC50 value of 10.17 µg/ml. ADME evaluation studies were performed with the help of Molinspiration online software. Docking calculations were also performed. Given the importance of the nucleus involved, the synthesized compound might find extensive medicinal applications as reported in the literature.

Cytotoxicity activity of geldanamycin derivatives against various cancer cell lines

Geldanamycin (1) was isolated as a major compound from Streptomyces zerumbet W14. It was then used as a precursor tosynthesize two new geldanamycins: 17-(tryptamine)-17-demethoxygeldanamycin (2) and 17-(5′-methoxytryptamine)-17-demethoxygeldanamycin (3). The cytotoxicity activity of these two new compounds was evaluated and comparedwith the cytotoxicity of compound 1. Cytotoxicity activity was evaluated against a normal cell line, and three cancercell lines using an 3-(4, 5-Dimethylthiazol-2-yl)-2, 5-diphenyltetrazolium bromide (MTT) colorimetric assay. Thesolubility of these compounds was also determined. The solubility of compounds 2 and 3 in water was 290.69and 348.18 µM, higher than that of compound 1 by about 1.91 and 2.29 times, respectively. Compounds 2 and 3showed moderate cytotoxic activity on Vero and human cervical carcinoma cells with IC50 values of >200.00 µg/ml. The strongest cytotoxicity of compound 3 was observed in human breast carcinoma cells (MCF-7) and humanhepatocellular carcinoma cell line (HepG2) cells with IC50 values of 82.50 and 114.35 µg/ml, respectively, while theIC50 values of compound 2 against MCF-7 and HepG2 cells were 105.62 and 124.57 µg/ml, respectively. The findingsshowed that these new geldanamycin derivatives exhibited selective cytotoxicity toward some cancer cells at a lowerconcentration. Therefore, future studies on these compounds could be useful for the management of some cancers

New flavone and other compounds from Tephrosia egregia: assessing the cytotoxic effect on human tumor cell lines

ABSTRACT The organic extracts from stems, roots and leaves of Tephrosia egregia Sandwith, Fabaceae, provided a new flavone, 5-hydroxy-8-(1",2"-epoxy-3"-hydroxy-3"-methylbutyl)-7-methoxyflavone (1), in addition to eleven known compounds: pongaflavone (2), praecansone B (3), 12a-hydroxyrotenone (4), praecansone A, 2',6'-dimethoxy-4',5'-(2",2"-dimethyl)-pyranochalcone, pongachalcone, maackiain, β-sistosterol and its glucoside, p-cumaric acid and cinnamic acid. The structures of all compounds were established on the basis of spectroscopic methods, mainly 1D and 2D NMR and HRESIMS, involving comparison with literature data. Cytotoxicity of compounds 1-4 was evaluated against AGP-01 (cancerous ascitic fluid), HCT-116 (colon adenocarcinoma), HL-60 (leukemia), PC-3 (prostate carcinoma), SF-295 (glioblastoma) and SKMEL 28 (melanoma) cell lines.

Assessment Of Cytotoxicity Potency Of Paclitaxel In Combination With Clinacanthus Nutans Extracts On Human Mda-Mb-231 Breast Cancer Cells / Jurnal Sains Kesihatan Malaysia

Clinacanthus nutans (C. nutans) leaf extracts have been widely used by cancer patients in Malaysia and local practiceclaims a cure to cancer. There were several studies done to determine the cytotoxicity potency of C. nutans extracts onvarious types of cells. However, there is still lacking on the knowledge regarding the combination effect of C. nutanswith anticancer drugs. Thus, the study was carried out to determine the cytotoxicity potency of C. nutans extracts andpaclitaxel (PTX) alone and, in combination on MDA-MB-231 cells. The cells were treated with 100% ethanol extract ofC. nutans (CNE) and water extract of C. nutans (CNA), PTX and combination of both extracts and PTX for 72 hours andthe cytotoxic activity was determined using SRB assay. Result showed that CNE had little cytotoxic activity, whereas CNAshowed no cytotoxic activity on MDA-MB-231 cells. For combination treatment of C. nutans extracts and PTX, only CNEshowed significant enhanced PTX-induced cytotoxicity (p < 0.05), meanwhile CNA inhibited PTX-induced cytotoxicitysignificantly (p < 0.05). As a conclusion, CNE was able to increase PTX potency to inhibit the viability of MDA-MB-231cells.

TypeⅠ IFN-mediated enhancement of anti-osteosarcoma cytotoxicity of human gammadelta T cells / 中国免疫学杂志

Objective:To investigate the effect of typeⅠIFN on the cytotoxic activity ofγδT cells from peripheral blood mono-nuclear cells ( PBMCs) of healthy donors and osteosarcoma patients stimulated by zoledronate ( Zol) and IL-2 against OS.Methods:PBMCs from healthy donors and osteosarcoma patients were stimulated with Zol+IL-2 or Zol+IL-2+typeⅠIFN,respectively.After 14 days of culture,ex vivo expandedγδT cells were assessed by flow cytometry.γδT cell cytotoxicity against target cells was analyzed using a standard lactate dehydrogenase release assay.IFN-γsecreted fromγδT cells was determined by ELISA kits.Results:γδT cells from PBMCs of healthy donors and patients with OS were selectively expanded by Zol+IL-2 or Zol+IL-2+typeⅠIFN in vitro,respectively, and showed cytotoxicity against OS.In addition,γδT cells pre-treated by TypeⅠIFN showed significantly higher cytotoxicity against OS cells.Conclusion:Type I IFN can enhance humanγδT cells’ cytotoxic activity against OS.

Pentaclethra macroloba tannins fractions active against methicillin-resistant staphylococcal and Gram-negative strains showing selective toxicity

The ethanol extract of the vegetal species Pentaclethra macroloba (Willd.) Kuntze, Fabaceae, was fractioned and the antibacterial activity was determined. The active ethyl acetate (ea) fraction showed activity against Gram-positive (Staphylococcus spp. and Enterococcus spp.) and Gram-negative (Pseudomonas aeruginosa, Acinetobacter spp. and Klebsiella pneumoniae) multiresistant bacteria. Gallic acid derivatives were identified as the main compounds in inactive subfractions from the ea fraction, while the active one afforded ellagic acid as the major constituent when submitted to acid hydrolysis reaction, which suggests the presence of hydrolysable tannins. The minimum bactericidal concentration analysis showed a bactericide mechanism of action for the tannin subfraction found. The antibacterial mechanism of action of the active tannin subfraction against S. aureus reference strains (ATCC 29213 e 33591) was proposed adopting an in vitro assay of protein synthesis inhibition. For this, bacterial cells were labeled with [35S] methionine in the presence of the subfraction. The protein synthesis inhibition was observed at 256 µg/mL of this subfraction. At this concentration it did not present cytotoxicity in eukaryotic cells by the neutral red technique, suggesting selective toxicity. The present study is the first in vitro investigation of the antibacterial properties of tannin fractions obtained from a polar extract of P. macroloba.