Novel antiproliferative analogs of the Taq DNA polymerase inhibitor catalpol

Pungitore, Carlos Rodolfo; León, Leticia G.; García, Celina; Martı́n, Victor S.; Tonn, Carlos E.; Padrón, José M.

doi:10.1016/j.bmcl.2006.11.086

Cited by 47 publications

(35 citation statements)

References 17 publications

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“…Anthocyanins have been used as medicine or supplements for many years and it has been reported that depending on the nutrition habits, the daily intake of anthocyanins in humans could be up to 150 mg/day [14]. Catalpol is an iridoid glucoside and exhibits anti-inflammatory and anti-diabetes activities [17]–[19]. Quercetin is a natural flavonoid widely distributed in plants that acts as a neuroprotective, anti-cancer, anti-ROS formation agent [6], [20]–[23].…”

Section: Discussionmentioning

confidence: 99%

Selective Anti-Proliferation of HER2-Positive Breast Cancer Cells by Anthocyanins Identified by High-Throughput Screening

Liu

et al. 2013

PLoS ONE

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Overexpressed Human epidermal growth factor receptor 2 (HER2) drives the biology of 20% breast cancer and is a prediction of a poor prognosis for patients. HER2-targeted therapies significantly improve outcomes for HER2-positive patients. Traditional Chinese herbs/medicines have been used to treat breast cancer patients including HER2-positive patients in Asia for decades. Although the traditional medicines demonstrate efficacy in clinics for HER2-positive patients, the mechanism is largely unknown. In this article, we screened a 10,000 natural product library in 6 different cell lines representing breast cancer, and assessed the ability of each drug to cause cytotoxicity through a high-throughput screening approach. We have identified eight natural compounds that selectively inhibit the proliferation of HER2-positive cells. Two of the hit compounds, peonidin-3-glucoside and cyaniding-3-glucoside, are both extracts from black rice. They inhibit the phospho-HER2 and phospho-AKT and were confirmed to induce HER2-psotive breast cancer cells apoptosis both in vitro and in vivo. Peonidin-3-glucoside and cyaniding-3-glucoside treatments significantly reduced the tumor size and volume in vivo compared to the control group. There is no significant difference of antitumorgenic effects between peonidin-3-glucoside and cyaniding-3-glucoside treatments.

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Section: Discussionmentioning

confidence: 99%

Selective Anti-Proliferation of HER2-Positive Breast Cancer Cells by Anthocyanins Identified by High-Throughput Screening

Liu

et al. 2013

PLoS ONE

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“…Iridoid glycosides exist widely in plants of many families and display various biological activities, including purgative, hepatoprotective, anti-microbial, analgesic, antitumor, sedative and anti-inflammatory effects [11]. Several studies have demonstrated a broad range of biological and pharmacological effects of catalpol, an iridoid glucosideisolated from the root of Rehmannia glutinose , such as neuroprotection, anti-tumor [12] and anti-inflammation [13,14,15]. Research on the anti-inflammatory activity of catalpol further suggests that catalpol exerts therapeutic activity through attenuation of NF-κB activity [16,17].…”

Section: Introductionmentioning

confidence: 99%

Catalpol Ameliorates Sodium Taurocholate-Induced Acute Pancreatitis in Rats via Inhibiting Activation of Nuclear Factor Kappa B

Xiao

Yin

Fan

et al. 2014

IJMS

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Catalpol, an iridoid glucoside extracted from the traditional Chinese herbal medicine, Rehmannia glutinosa, is reported to exert neuroprotective, anti-inflammatory, anti-tumor and anti-apoptotic effects. The main aim of the present study was to investigate whether catalpol ameliorates experimental acute pancreatitis (AP) induced by sodium taurocholate (STC). AP was induced in rats via retrograde injection of 4% STC (0.1 mL/100 g) into the biliopancreatic duct. Rats were pre-treated with saline or catalpol (50 mg/kg) 2 h before STC injection. At 12, 24 and 48 h after injection, the severity of AP was evaluated using biochemical and morphological analyses. Pretreatment with catalpol led to a significant reduction in serum amylase and lipase activities, pancreatic histological damage, myeloperoxidase (MPO) activity, interleukin (IL)-1β, IL-6 and TNF-α levels, and activation of nuclear factor kappa B (NF-κB). Moreover, administration of catalpol increased the viability of pancreatic acinar cells and inhibited NF-κB expression in vitro. Our results collectively support the potential of catalpol as a highly effective therapeutic agent for treatment of AP.

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“…Catalpol, an iridoid glucoside found in the root of R. glutinosa Libosch, has been shown to exhibit various biological and pharmacological activities, including anti-tumor [21], anti-inflammation [22], anti-oxidation [23–25] and anti-apoptosis activities [26, 27]. Exposure of ionizing radiation can lead to increased generation of ROS, including hydroxyl radicals (OH), superoxide anions (O2 − ), singlet oxygen ( 1 O 2 ) and hydrogen peroxide (H 2 O 2 ), which are major determinants of cellular damage including apoptosis and necrosis.…”

Section: Discussionmentioning

confidence: 99%

Radio-protective effect of catalpol in cultured cells and mice

Chen

Xu³

et al. 2012

Journal of Radiation Research

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Ionizing radiation can induce DNA damage and cell death by generating reactive oxygen species (ROS). The objective of this study was to investigate the radio-protective effect of catalpol (a main bioactive component in the traditional Chinese Rehmannia) on irradiated cells and mice. We found that treating cells with catalpol (25–100 μg/ml) before irradiation could significantly inhibit ionizing radiation (IR)-induced human lymphocyte AHH-1 cells apoptosis and increase cells viability in vitro. At the same time our study also showed that catalpol (25–100 mg/kg) reduced morphological damage of the gastrointestinal tract by 15.6%, 33.3% and 44.4%, respectively compared with the radiation-induced group, decreased plasma malondialdehyde (MDA) intestinal 8-hydroxydeoxyguanosine (8-OHdG) levels and increased plasma endogenous antioxidants and peripheral white blood cells and platelets in vivo. These results suggest that catalpol possesses notable radio-protective activity, which might be related to its effect of reducing ROS.

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Novel antiproliferative analogs of the Taq DNA polymerase inhibitor catalpol

Cited by 47 publications

References 17 publications

Selective Anti-Proliferation of HER2-Positive Breast Cancer Cells by Anthocyanins Identified by High-Throughput Screening

Selective Anti-Proliferation of HER2-Positive Breast Cancer Cells by Anthocyanins Identified by High-Throughput Screening

Catalpol Ameliorates Sodium Taurocholate-Induced Acute Pancreatitis in Rats via Inhibiting Activation of Nuclear Factor Kappa B

Radio-protective effect of catalpol in cultured cells and mice

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