Barrigenol-like triterpenoids (BATs) showed promising anti-tumor, anti-inflammatory and anti-Alzheimer's activities, while, the inhibitory strength was usually affected by their states with aglycones or glycosides. In order to find more BATs as new anti-tumor agents with much more efficiency, the chemical and pharmaceutical studies were carried out on the acid hydrolysate product (AHP) of Semen Aesculi crude extract. Thirteen BATs, including three new aglycones (1–3), two new glycosides (4, 5) and eight known glycosides (6–13) were obtained. Compound 1, as the main product in AHP, with a tigloyl unit linked at the C-16 position was an unusual aglycone. All compounds exhibited various degrees of inhibitory activity against human breast cell line (MCF-7) and cervical cancer cell line (HeLa) growth, moreover, new aglycones 1 and 2, and the known glycoside 6 (escin Ia) and 9 were found to exhibit potent inhibitory activity which were similar to the positive control (doxorubicin hydrochloride). Compound 1, named 16-tigloyl-O-protoaescigenin, could suppress tumor progression and decreased lung metastasis focuses in mice, and no pathological change was observed at the end of the treatment course. Besides that, the hemolysis experiment between 1 and 6 revealed that the hemolysis toxicity of 1 was much less than that of 6. According to these results, 16-tigloyl-O-protoaescigenin, with the powerful anti-tumor activity and cancer cell apoptosis induction, might be considered as a new promising anti-tumor agent.
Abstract Oleanolic and ursolic acids are two ubiquitous isomeric triterpene phytochemicals known for their anticancer activity. A set of derivatives of the two compounds with a modified oxidation state and lipophylicity at C-3 and C-28 positions, were prepared and tested as anticancer agents versus the lines HepG2, Hep3B and HA22T/VGH of hepatocarcinoma, a strongly aggressive tumor that is not responsive toward the standard therapies. New derivatives containing a three carbons side chain on the ...
Last. Yuanqiang Guo(NKU: Nankai University)H-Index: 20
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Abstract A search for bioactive natural products as anticancer lead compounds has led to the isolation of five new clerodane diterpenoids (1–5) from the twigs of Casearia kurzii. Their structures were elucidated by extensive analysis of their NMR, IR, and HRESIMS data, and the absolute configurations were determined by experimental and calculated electronic circular dichroism (ECD) data analysis. The isolates were biologically evaluated and showed cytotoxic activities toward human lung cancer ce...
: Nano-sized hydroxyapatite (nHA) particles have been demonstrated to exert anti-cancer effects on multiple cancer cell lines and animal models of cancer biology. However, the molecular mechanism underlying the effects of nHA particles on glioma cells remains unclear. The present study aimed to examine the effects of nHA on the behavior of glioma cells and investigate its underlying molecular mechanism. Rat glioma C6 cells and human glioma U87MG ATCC cells were exposed to nHA (20-100 µg/ml), and...
Last. Huiyuan Gao(SPU: Shenyang Pharmaceutical University)H-Index: 12
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Abstract Barrigenol-like triterpenoids (BATs), which contain an unusual oleanane substituted by many hydroxyl groups as the skeleton, are subdivided into five subtypes: barrigenol A 1 , barrigenol A 2 , barrigenol R 1 , barringtogenol C, and 16-deoxybarringtogenol C. The variations in acyl derivatives, hydroxyl groups, and carbohydrate chains in their structures have enhanced the diversity of BATs. Moreover, the stable polyhydroxy-replaced pentacyclic skeleton provides an ideal platform for stru...
Last. Kwhanmien Kim(Seoul National University Bundang Hospital)H-Index: 47
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Photodynamic therapy (PDT) with a suitable photosensitizer molecule is a promising anticancer treatment. We evaluated two chlorin molecules as potential photosensitizers, methyl pyropheophorbide a (MPPa) and N-methoxyl purpurinimide (NMPi), against A549 human lung adenocarcinoma cells in vitro as well as in A549 tumor-bearing mice in vivo. Cell viability, microscopy, and fluorescence-activated cell sorting (FACS) analyses were performed for the in vitro studies. MPPa and NMPi showed high phototo...
Last. Thai Tran(NUS: National University of Singapore)H-Index: 18
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Abstract Escin is a mixture of triterpenoid saponins extracted from the horse chestnut tree, Aesculus hippocastanum. Its potent anti-inflammatory and anti-odematous properties makes it a choice of therapy against chronic venous insufficiency and odema. More recently, escin is being actively investigated for its potential activity against diverse cancers. It exhibits anti-cancer effects in many cancer cell models including lung adenocarcinoma, hepatocellular carcinoma and leukemia. Escin also att...
Last. Huiyuan Gao(SPU: Shenyang Pharmaceutical University)H-Index: 12
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AbstractThe Xanthoceras sorbifolia Bunge husks were known for their abundant triterpenoids resource, which contributed to many bioactivities, such as antitumor, antiinflammatory and neuroprotection. The present study has led to the purification of a new triterpenoid saponin, 21β-O-acetyl-xanthohuskiside A (1), together with six known barrigenol derivatives (2–7), whose structures were authenticated on the basis of NMR, HR-MS, IR spectrum and acid hydrolysis experiment. Compound 7 showed more not...
Background: Rhein, an anthraquinone derivative of rhubarb, is traditionally used in Chinese herbal medicine. Now emerging studies suggest its antitumor properties in many human cancers. The present study aims to investigate the antitumor role of Rhein and its possible mechanism in human renal cell carcinoma (RCC). Materials and methods: Three RCC cell lines (A489, 786-O and ACHN) were used as the cell models. We applied CCK-8, cell counting, colony formation, wound healing and Transwell assays t...
Last. Yongri Jin(JLU: Jilin University)H-Index: 12
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Two new steroidal saponins(2, 3) and two known compounds(1, 4) were isolated from 75% ethanol extract of Allii macrostemonis bulbus by various spectral methods. The two new steroidal saponins were respectively elucidated as (25S)-26-O-β-D-glucopyranosyl-5α-furostanol-2α,3β,22,26-tetrol-3-O0-β-D-glucopyranosyl(1→2)-[β-D-glucopyranosyl(1→3)]-β-D-glucopyranosyl(1→4)-β-D-galactopyranoside(2) and 26-O-β-D-glucopyranosyl-5α-furostanol-25(27)-ene-3β,22,26-tetrol-3-O-β-D-glucopyranosyl(1→2)-[β-D-glucopy...
: Colorectal cancer, one of the most commonly diagnosed and lethal cancers worldwide, is accompanied by the disorders of immune system. However, the underlying mechanism is still not fully understood. In this study, our goal was to determine whether interleukin 33 promotes tumorigenesis and progression of colorectal cancer through increased recruitment of tumor-infiltrating ST2+ regulatory T cells in CT26 tumor-bearing mice. We found that the mRNA or protein levels of interleukin 33, soluble ST2...