*Alkaloids ; *Antineoplastic Agents, Phytogenic ; Chemistry ; *Harringtonines

The tirucallane-type triterpenoids, composed of six isoprene units, belong to a group of tetracyclic triterpenoids. Although the naturally-derived tirucallane-type triterpenoids were found in a small amount, the kind of compounds showed various structures, which consist of apo-type, linear said-chain-type and cyclolike said-chain-type and broad bioactivities, such as cytotoxicity, anti-inflammation, antioxidation and anti-plasmin, etc. This paper summarized origins, structures and bioactivities of tirucallane-type triterpenoids in recent ten years. The future research and exploration of tirucallane-type triterpenoids were discussed and prospected.
Antineoplastic Agents, Phytogenic ; Molecular Structure ; Triterpenes

Alkaloids ; Antineoplastic Agents, Phytogenic ; Chemical Phenomena ; Chemistry ; Harringtonines

Paclitaxel, a tetracyclic diterpenoid compounds, was firstly isolated from the bark of the Pacific yew trees. Currently, as a low toxicity, high efficiency, and broad-spectrum natural anti-cancer drug, paclitaxel has been widely used against ovarian cancer, breast cancer, uterine cancer, and other cancers. As the matter of fact, natural paclitaxel from Taxus species has been proved to be environmentally unsustainable and economically unfeasible. For this reason, researchers from all over the world are devoted to searching for new ways of obtaining paclitaxel. At present, other methods, including artificial cultivation of Taxus plants, microbial fermentation, chemical synthesis, tissue and cell culture have been sought and developed subsequently. Meanwhile, the biosynthesis of paclitaxel is also an extremely attractive method. Unlike other anti-cancer drugs, paclitaxel has its unique anti-cancer mechanisms. Here, the source, production, and anti-cancer mechanisms of paclitaxel were summarized and reviewed, which can provide theoretical basis and reference for further research on the production, anti-cancer mechanisms and utilization of paclitaxel.
Antineoplastic Agents, Phytogenic/pharmacology* ; Humans ; Neoplasms/drug therapy* ; Paclitaxel/pharmacology*

Steroidal saponins have a wide range of pharmacological effects and biological activities, such as anti-tumor, antifungal, hypoglycemic, immune regulation, insecticides, etc. In the last ten years, some new structures of steroidal saponins compounds were found from natural plants, they have some new and different activities. In order to accelerate the research on the drug innovation of steroidal saponins, we summarized the new progress of the research on such compounds.
Animals ; Anti-Inflammatory Agents ; pharmacology ; Antifungal Agents ; pharmacology ; Antineoplastic Agents, Phytogenic ; pharmacology ; Humans ; Hypoglycemic Agents ; pharmacology ; Saponins ; pharmacology ; Steroids ; pharmacology

OBJECTIVETo investigate the constituents of the Annona squamosa and evaluate their anti-tumor activity.

METHODThe compounds were isolated and purified by various column chromatography. Their structures were elucidated by spectral data analysis. Their anti-tumor activity was assayed by SRB method.

RESULTEleven compounds were obtained from the 95% EtOH extract. The structures were determined as: annosquamosin C(1),15, 16-epoxy-17-hydroxy-ent-kau-ran-19-oic acid (2),16,17-dihydroxy-ent-kau-ran-19-oic acid(3), annosquamosin A(4), ent-kaur-16-en-19-oic acid (5), 19-nor-ent-kauran4-ol-17-oic acid (6),16-hydroxy ent-kau ran-19-oic acid (7), ent-15beta-hydroxy-kaur-16-en-19-oic acid (8), annosquamosin B (9), ent-16beta, 17-dihydroxykauran-19-al (10), 16, 17-dihydroxy-ent-kauran-19-oic acid me thyl ester (11). Compounds 1,2,3,5,9 showed different inhibitory activities against 95-D lung cancer cells,the effect of compound 5 was strongest with the IC50 value 7.78 micromol x L(-1); Compounds 2, 5, 9 showed inhibitory activities against A2780 ovarian cancer cells, the effects of compounds 2 and 9 were strong with the IC50 values being 0.89, 3.10 micromol x L(-1), respectively.

CONCLUSIONCompound 2 was firstly isolated from this family, while compound 8 and 10 were first found from this genus and the title species, respectively. The in vitro anti-tumor test showed compound 5 significantly inhibited 95-D lung cancer cells and compounds 2 and 9 exhibited remarkbale activity against A2780 ovarian cancer cells.

Nine triterpenes compounds were isolated from the male flowers of Eucommia ulmoides by recrystallization and chromatographic techniques over silica gel, Sephadex LH-20, and RP-18 gel. Their chemical structures were identified on the basis of spectral analysis and as 3-oxo-12-en-ursane-28-O-α-L-arabinofuranosyl (1 --> 6) -β-D-glucopyranoside (1), 2α, 3β-dihydroxyurs-12-en-28-oic acid(28 --> 1) -β-D-glucopyranosyl ester (2), ursolic acid (3), α-amyrin (4), uvaol (5), ursolic acid acetate (6), 3-O-acetate oleanoic acid (7), betulinic acid (8), and betulinol (9). Compound 1 was a new compound, and compounds 2, 4-7 were isolated from the Eucommiu genus for the first time. Cytotoxic activity was tested for all the compounds against K562 and HepG2 cells. The results showed that only compound 3, exhibited cytotoxic activity.
Antineoplastic Agents, Phytogenic ; pharmacology ; Eucommiaceae ; chemistry ; Hep G2 Cells ; Humans ; K562 Cells ; Triterpenes ; analysis ; pharmacology

To study the anti-tumor metastatic constituents in Rhodiola wallichiana (HK) S H Fu var Cholaensis (Praeg) S H Fu, chemical constituents were isolated and purified by repeated column chromatography (silica gel, Toyopearl HW-40C and preparative HPLC). Their structures were elucidated on the basis of spectral data analysis. The anti-tumor metastasis assay was applied to evaluate the activities of the isolated compounds. Ten compounds (1-10) were isolated and their structures were identified by comparison of their spectral data with literature as follows: syringic acid (1), salidroside (2), tyrosol (3), scaphopetalone (4), berchemol (5), 2,6-dimethoxyacetophenone (6), rhobupcyanoside A (7), miyaginin (8), chavicol-4-O-β-D-apiofuranosyl-(1 --> 6)-O-β-D-glucopyranoside (9), eugenyol-O-β-D-apiofuranosyl-(1 --> 6)-O-β-D-glucopyranoside (10). Compounds 4-6 and 8-10, were isolated from this genus for the first time, while compound 7 was isolated from this plant for the first time. Compounds 2, 6-8 showed positive anti-tumor metastatic activities, and compounds 2 and 8 showed significant anti-tumor metastatic activities.
Antineoplastic Agents, Phytogenic ; isolation & purification ; pharmacology ; Cell Line, Tumor ; Humans ; Neoplasm Metastasis ; prevention & control ; Rhodiola ; chemistry

OBJECTIVETo develop a fluorescence imaging-based novel system for quick screening of antitumor compounds in vitro.

METHODSThe antitumor activity of 26 components from Lindera aggregate were determined by relative number of viable cell labelled with fluorescein diacetate (FDA) in multiwell plates after exposure to these 26 different components. Then, the linearity and precision of this method were validated. The structures of active compounds in components with strong antitumor activity were deduced by LC/MS.

RESULTSThe linearity of this method for cells stained with FDA was validated (r² = 0.9858) in the range of 0-10⁴ cells per well, and the in-plate precision was 9.41 %. Two of 26 components from Lindera aggregate showed significant inhibition effect on proliferation of HepG2 cells (inhibition rate >90%).

CONCLUSIONThis proposed rapid and reliable approach can be used for screening compounds with antitumor activity from Traditional Chinese Medicine in vitro. The major active compound of Lindera aggregate was putatively identified as norboldine by LC/MS analysis.

OBJECTIVETo extract and isolate the component from myrsinane-type diterpenes of Euphorbia prolifera.

METHODSPetroleum extraction and chromatography on the silica gel were used to extract and isolate the diterpenes of Euphorbia prolifera.

RESULTSEight components of myrsinol diterpenes were isolated, namely: Proliferin A(1), Proliferin B (2), Proliferin C(3), Proliferin D(4), Euphorprolitherin B(5), Euphorprolitherin D(6), SPr5(7) and 14-desoxo-3-O-prorionyl-5, 15-di-O-acetyl-7-O-nicotinoyl-myrsinol-14β-acetate(8). Their structures were identified with mass-spectroscopic methods and NMR techniques. The cytotoxicity of compounds 1, 2, and 4 against cancer cells was evaluated, with compound 1 being active against A2780 cancer cells (IC(50) 7.7 μmol/L).

CONCLUSIONMyrsinane-type diterpene Proliferin A from Euphorbia prolifera shows cytotoxic effect against human ovarian cancer cell line A2780.