A cytotoxic compound from the leaves of Juglans mandshurica

From Juglans mandshurica leaves, a new quinone compound was isolated through bioassay-guided fractionation. The structure elucidation of the compound was established based on spectroscopic studies, notably of the 2D NMR spectra. The compound exhibited moderate cytotoxic activities against Hela, MCF-7, BGC823 and 3T3-Llcell lines with IC50 ranges from 7.5 to 26.8 μmol/L.     

Cordycedipeptide A, a new cyclodipeptide from the culture liquid of Cordyceps sinensis (Berk.) Sacc

A new cyclodipeptide named as cordycedipeptide A, a new natural compound and two known compound were isolated from the culture liquid of Cordyceps sinensis (BERK.) SACC. Their structures were elucidated as 3-acetamino-6-isobutyl-2,5-dioxopiperazine (1), 3-isopropyl-6-isobutyl-2,5-dioxopiperazine (2) and 3,6-di(4-hydroxy)benzyl-2,5-dioxopiperazine (3) by 1D and 2D-NMR techniques. The cytotoxic assay showed compound 1 had the cytotoxic activities to L-929, A375, and Hela.     

Chemical constituents from rauvolfia verticillata and bioactivities research

A new acridone alkaloid, named 9-hydroxynoracronycine (1), together with four known compounds, including coumarins, lignan, and indole alkaloid, was isolated and identified from the roots and rhizomes of Rauvolfia verticillata. The structure of the new compound was determined by spectroscopic means (UV, IR, MS, and NMR). The acridone alkaloid and coumarins were identified as new constituents of Rauvolfia genus. The cytotoxic activities of the new compound were tested against human breast cancer cell line MCF-7 and human promyelocytic leukemia HL-60. Results showed that compound 1 decreased MCF-7 cell proliferation in a statistically IC₅₀ significant manner at 102.8 μmol/L. In addition, compound 1 exhibited moderate small intestine smooth muscle relaxation.     

新的19-降海绵烷二萜的分离及结构确定

从海洋海绵Spongiazimoccaaubspeclesirregularia中分离到一种新的19-降海绵烷二萜(ZimoclactoneA,1)和胆甾-5,7-二烯-3β-醇,化合物1的化学结构和立体化学通过波谱方法和X射线单晶衍射分析确定,化合物1对P388肿瘤细胞具有中等程度的细胞毒活性.     

Isolation and Stucture Elucidation of Diterpenes from Wedelia prostrata and Their Cytotoxicity Activities

In this paper, a new diterpene together with seven known diterpenes was isolated from Wedelia prostrata. The chemical structure of the new compound was elucidated via 1D and 2D nuclear magnetic resonance(NMR) techniques and mass spectrometry and identified to be 3α-phenylpropionoyloxy-ent-kaur-16-en-oic acid(1). The isolated diterpenes were tested for their cytotoxicity activities via 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide(MTT) assay. The results show that compounds 1, 2, 3, 4 and 6 exhibit different levels of cytotoxic activities. Especially, compound 2 shows significant cytotoxicity toward HeLa and A549 cell lines(IC₅₀=6.14 and 8.76 μmol/L).     

Phenolic compounds from <Emphasis Type="Italic">Clinopodium urticifolium</Emphasis>

A new phenolic compound, clinopodphenol A (1), together with six known ones, was isolated from the whole plant of Clinopodium urticifolium. The structure of 1 was elucidated by spectroscopic methods, including extensive 1D- and 2D NMR techniques. The anti-HIV-1 activity and cytotoxicity were evaluated for compound 1. It showed significant potential cytotoxic ability and moderate anti-HIV-1 activity.     

Chlovalicin B,a Chlorinated Sesquiterpene Isolated from the Marine Mushroom Digitatispora marina

As part of our search for bioactive metabolites from understudied marine microorganisms, the new chlorinated metabolite chlovalicin B (1) was isolated from liquid cultures of the marine basidiomycete Digitatispora marina, which was collected and isolated from driftwood found at Vannøya, Norway. The structure of the novel compound was elucidated by spectroscopic methods including 1D and 2D NMR and analysis of HRMS data, revealing that 1 shares its molecular scaffold with a previously isolated compound, chlovalicin. This represents the first compound isolated from the Digitatispora genus, and the first reported fumagillin/ovalicin-like compound isolated from Basidiomycota. Compound 1 was evaluated for antibacterial activities against a panel of five bacteria, its ability to inhibit bacterial biofilm formation, for antifungal activity against Candida albicans, and for cytotoxic activities against malignant and non-malignant human cell lines. Compound 1 displayed weak cytotoxic activity against the human melanoma cell line A2058 (~50% survival at 50 µM). No activity was detected against biofilm formation or C. albicans at 50 µM, or against bacterial growth at 100 µM nor against the production of cytokines by the human acute monocytic leukemia cell line THP-1 at 50 µM.     

A new azafluorenone from the roots of Polyalthia cerasoides and its biological activity

Chromatographic separation of the ethyl acetate extract of roots of Polyalthia cerasoides has led to the isolation of the new compound, 6,8-dihydroxy-7-methoxy-1-methyl-azafluorenone. This compound exhibited potent cytotoxic activities with IC50 values in the range of 2.64-3.58 microg x mL(-1) for A549, GLC4 and GLC4/Adr cells, but was not recognized by ABCC1/MRP1 protein. The compound also showed very strong inhibition of M. tuberculosis using a broth microdilution method, with an MIC value of 0.78 microg x mL(-1), which was equal to that of ofloxacin, one of the four antibiotic drugs used as a positive control.     

杯菊中的倍半萜内酯

摘要杯菊(Cyathocline purpurea)是云南民间民族药, 全株用于治疗各种炎症和肺结核. 采用L1210细胞系对杯菊的粗提物、 分步萃取物的成分进行了细胞毒试验; 用柱层色谱法同步对活性组分进行化学成分分离纯化; 通过理化数据测定及波谱分析鉴定单体结构. 杯菊的氯仿及乙酸乙酯萃取物具有细胞毒活性, 其IC50分别为3.5和2.8 μg/mL. 从活性组分中分离出3种成分, 分别鉴定为Santamarin(1)、 9β-乙酰基广木香内酯(9β-acetoxycostunolide, 2)和9β-乙酰基小白菊内酯(9β-acetoxypathenolide, 3), 其IC50分别为0.41, 0.89, 0.59 μg/mL. 这三个化合物都有较强的抗癌活性, 其中化合物3为新化合物.     

A new lavandulyl flavonoid from Sorphora flavescens Ait

A new lavandulyl flavonoid was isolated from the rhizome of Sorphora flavescens. The structure of new compound was elucidated on the basis of spectral methods including 2D NMR. And it showed potent cytotoxic activity against Hela cells with IC50 of 1.1 μmol/L.     

Structure elucidation and NMR assignments for two new quinones from fructus rhodomyrti of <Emphasis Type="Italic">Rhodomyrtus tomentosa</Emphasis>

Two new quinones, 1,4,7-trihydroxy-2-methoxy-6-methylanthracene-9,10-dione (1) and compound 2, were isolated from fructus rhodomyrti of Rhodomyrtus tomentosa (Ari.) Hassk., which was collected from Guangdong Province. The structures were elucidated by 1D, 2D NMR, and HR-EI-MS spectroscopy methods. The cytotoxic activities of two compounds in vitro were tested. Compound 1 showed cytotoxicity against KB and KBv200 cell lines with IC50 of 17.1 and 19.5 )μg/mL, and compound 2 with IC50 of 18.1 and 25.4 )μg/mL, respectively.     

A New Cytotoxic Compound from Penicillium auratiogriseum, Symbiotic or Epiphytic Fungus of Sponge Mycale plumose

To investigate the bioactive metabolites from marine microbes,the fungus Penicillium auratiogriseum was isolated from the sponge Mycale plumose collected in Qingdao,China.The ethyl acetate extract of the fermentation broth of P.auratiogriseum showed significant cytoxicity in the mouse cdc2mutant cell line(tsFT210).Thus5L of liquid medium was inoculated with the purely isolated fungus and incubated at25?C for9days.The cultured broth was extracted three times with the equivalent volume of et…     

A new cytotoxic bufadienolide from Chinese medicine Chansu

A new cytotoxic bufadienolide was isolated from the traditional Chinese medicine-Chansu. The structure of new compound was elucidated on the basis of spectral methods including 2D NMR. And it showed strong in vitro cytotoxic activity against Hela cells with IC50 of 8.06 × 10^-2μmol/L.     

New synthesis of two tridentate bipyrazolic compounds and their cytotoxic activity tumor cell lines

Two new tripodal compounds - 4-{bis[(3,5-dimethyl-1H-pyrazole-1-yl)methyl]amino}butane-1-ol (1); ethyl 1-[((2-hydroxyethyl){[3-(ethoxycarbonyl)-5-methyl-1H-pyrazole-1-yl]methyl} amino)methyl]-5-methyl-1H-pyrazole-3-carboxylate (2) were reported. The evaluation of the cytotoxic properties in vitro of these ligands, was examined on two tumor cell lines - P815 (mastocytome murine) and Hep (carcinoma of human larynx). The concentration required to induce 50% of lysis (IC(50)) was more pronounced against P815 cell line (IC(50): 39.42 microg mL(-1) for the compound 1 and 97.74 microg mL(-1) for the compound 2) than the Hep cell line (IC(50): 83.49 microg mL(-1) for compound 1 and 185.30 microg mL(-1) for compound 2). Statistical analysis shows that the compound 1 is two to three folds more cytotoxic than the compound 2 (p < 0.05). Interestingly, the cytotoxic activity depends strongly on both the substituents linked to the aminic nitrogen and pyrazolic rings.     

Njaoamine I,a cytotoxic polycyclic alkaloid from the Haplosclerida sponge Haliclona (Reniera) sp.

A new cytotoxic polycyclic alkaloid containing a quinoline moiety, njaoamine I (1) has been isolated from the methanol extract of the sponge Haliclona (Reniera) sp. collected at Okuza Island, Tanzania. The structure of compound 1 was determined by 1D and 2D NMR and HRMS data analysis. Its relative configuration was elucidated by a NOESY experiment and confirmed by comparison of its NMR spectral data to those of njaoamines A–H. Moreover, njaoamine G (2) was also detected by LC/MS analysis of the methanol extract. Njaoamine I (1) displays cytotoxic activity against a panel of three human tumor cell lines in the micromolar range.     

Identification of a new cytotoxic biflavanone from Selaginella doederleinii

A new biflavanone, 2,2',3,3'-tetrahydrorobustaflavone 7,4',7'-trimethyl ether (1) was isolated from the whole plant of Selaginella doederleinii HIERON. (Selaginellaceae) together with the known biflavonoid, robustaflavone 7,4',7'-trimethyl ether (2) as the cytotoxic constituents against the three human cancer cell lines, HCT, NCI-H358, and K562. The structure of the new compound 1 was elucidated by spectral analysis including various 1D- and 2D-NMR experiments.     

Isolation, structural assignment, and total synthesis of barmumycin

Barmumycin was isolated from an extract of the marine actinomycete Streptomyces sp. BOSC-022A and found to be cytotoxic against various human tumor cell lines. On the basis of preliminary one- and two-dimensional (1)H and (13)C NMR spectra, the natural compound was initially assigned the structure of macrolactone-type compound 1, which was later prepared by two different routes. However, major spectroscopic differences between isolated barmumycin and 1 led to revision of the proposed structure as E-16. On the basis of the synthesis of this new compound, and subsequent spectroscopic comparison of it to an authentic sample of barmumycin, the structure of the natural compound was indeed confirmed as that of E-16.     

Anticancer effect of three pyrazole derivatives

The evaluation of the cytotoxic properties in vitro of three synthetic tripods containing pyrazole: N,N-bis[(3,5-dimethylpyrazol-1-yl)methyl]aniline (1); N,N-tetrakis[(3,5-dimethylpyrazol-1-yl)methyl]-para-phenylenediamine (2); and N,N-tetrakis-[(1,5-dimethylpyrazol-3-yl)methyl]-para-phenylenediamine (3), was examined for their cytotoxic activity on two tumor cell lines: P815 (murin mastocytoma) and Hep (human laryngeal carcinome). While the compound 2 shows a small cytotoxic activity, compounds 1 and 3 are more cytotoxic against both cell lines. However, this cytotoxicity is more pronounced against Hep cell line (IC50: 3.25 microg mL(-1) for compound 1 and 6.92 microg mL(-1) for compound 3) than P815 cell line (IC50: 17.82 microg mL(-1) for compound 1 and 37.21 microg mL(-1) for compound 3). Statistical analysis shows that the compound 1 is two- to threefold more cytotoxic than compound 3 (P < 0.05). Interestingly, the cytotoxicity induced by compound 1 against Hep cell line is more important than that induced by adriamycin used as a positive control.     

中国南海海绵Cinachyrella australiensis中(3E)-胆甾-4-烯-3,6-二酮-3-肟的结构鉴定

从南中国海海绵Cinachyrella australiensis的乙酸乙酯萃取部分分离出一个结构特别的甾体化合物, 应用UV, IR, MS, ¹H NMR, ¹³C NMR, DQCOSY, NOESY, TOCSY, HMQC和HMBC等光谱分析技术, 确定它为(3E)-胆甾-4-烯-3,6-二酮-3-肟(1). 化合物1为新天然甾体化合物, 通过生理活性实验表明其对乙肝病毒Hep G2细胞有较强的细胞毒活性. 本文对其波谱数据作了详细报道.     

A new triterpenoid compound from stems and leaves of American ginseng

A new dammarane-type triterpenoid compound was isolated from stems and leaves of American ginseng. The structure of the new sapogenin was elucidated by the combined analysis of NMR and HR-ESI-MS as dammar-20S, 25S-epoxy-3β, 12β, 26-triol (1). Compound 1 showed cytotoxic effect on human SM7721 and human Hela cells in vitro.