Paeonol inhibits tumor growth in gastric cancerin vitroandin vivo

Li, Na; Fan, Lulu; Sun, Guan; Wan, Xinan; Wang, Zhanggui; Wu, Qiang; Wang, Hua

doi:10.3748/wjg.v16.i35.4483

Cited by 58 publications

(36 citation statements)

References 17 publications

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“…2,3) However, paeonol has significant growth-inhibitory and apoptosis-inducing effects in gastric cancer cells in vitro and in vivo. 4) Moreover, studies have shown that paeonol prevents inflammatory diseases of the alimentary canal, such as irritable gastric ulcer, with minimal side effects. 5) However, studies on the ethanol-induced gastric ulcer effect of paeonol are lacking.…”

mentioning

confidence: 99%

Formulation Optimization of Gastro-Retention Tablets of Paeonol and Efficacy in Treatment of Experimental Gastric Ulcer

Zhang

Han

et al. 2017

CHEMICAL & PHARMACEUTICAL BULLETIN

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This study aims to develop a gastroretentive sustained-release drug delivery system of paeonol using floating properties and to investigate its therapeutic effects in rat models. The gastric retention tablets of paeonol (GRT-Ps) were prepared by a direct compression method, and the Box-Behnken design was used to optimize its formulation. The optimized formulation containing 15% NaHCO 3 and a 2 : 1 ratio of paeonol and HPMC-K4M floated within 1 min and remained afloat for more than 8 h in the simulated gastric fluid (200 mL, pH 1.2) and simultaneously showed the desired sustained drug release. Moreover, small tablets (3 mm) were prepared according to the same formulation and the process technology of big tablets (8 mm). A similar drug release behavior was observed between two kinds of tablets ( f 2 52), and then the evaluations of efficacy and retention capacity in vivo were conducted with small tablets. In vivo retention studies showed that the T max (2 h) of GRT-P in rat stomachs was significantly extended compared with the T max (0.5 h) of normal reference preparation. Compared with the model group, low and high doses of GRT-P could significantly inhibit the increase of malondialdehyde (MDA) in serum. Studies showed that the higher MDA content in inflammation tissue increases the inflammatory response. The ulcer inhibition rates of GRT-P in the highdose group were 59.0 and 64.1% in the ranitidine group. Results indicated that GRT-Ps had the potential for a sustained drug release and an enhanced gastric residence time with relatively high drug concentrations in the tissue distribution.Key words paeonol; gastric retention tablet; sustained release; gastric ulcer; efficacy Paeonol, also called peony phenol, is the active component of a traditional Chinese medicine, namely, moutan cortex (Paeonia suffruticosa ANDREWS, Ranunculaceae).1) Paeonol has been extensively studied for its anti-inflammatory, antioxidant, anti-atherosclerosis, anti-diabetic, and anti-mutagenic effects.2,3) However, paeonol has significant growth-inhibitory and apoptosis-inducing effects in gastric cancer cells in vitro and in vivo.4) Moreover, studies have shown that paeonol prevents inflammatory diseases of the alimentary canal, such as irritable gastric ulcer, with minimal side effects.5) However, studies on the ethanol-induced gastric ulcer effect of paeonol are lacking. Currently, the listed paeonol dosages are administered via ordinary oral tablets and injection. However, paeonol has poor water solubility, easy oxidation, and a short biological half-life. [6][7][8] The paeonol products are unable to prolong effective drug concentration in blood to influence the oral bioavailability of a drug. Therefore, the present study, which is based on the properties of paeonol, has been designed to develop gastric retention tablets using modern technology to achieve prolonged presence in the stomach, thereby improving treatment of gastric ulcer. This approach has a profound clinical significance in developing a novel sustained-release delivery syst...

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confidence: 99%

Formulation Optimization of Gastro-Retention Tablets of Paeonol and Efficacy in Treatment of Experimental Gastric Ulcer

Zhang

Han

et al. 2017

CHEMICAL & PHARMACEUTICAL BULLETIN

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“…We found that the increased levels of phosphorylated Akt and caspase-3 cleavage by Pae or Pae-NPs were rescued with NAC pretreatment, especially Although it has been shown that Pae-induced apoptosis is characterized by the activation of caspase-3 and inhibition of surviving, 6 decrease in the Bcl-2/Bax ratio, 5,8,12 and stimulation of interleukin (IL)-2 and tumor necrosis factor (TNF)-α production, 12 the exact mechanism remains unclear. Previous studies have demonstrated that the mechanism of Pae's antitumor effect is via induction of apoptosis, stimulation of IL-2, and TNF-α production.…”

Section: Modulation Of Akt/apoptotic Pathways By Pae-npsmentioning

confidence: 95%

“…[5][6][7][8][9][10][11][12][13] Pae has been reported to induce apoptosis in various cancer cells, including gastric cancer, esophageal cancer, ovarian cancer, and hepatocellular carcinoma. 5,6,8,12 One study reported that Pae had a radiosensitizing effect on lung adenocarcinoma cell both in vitro and in vivo. 9 This radiosensitizing effect is closely related to apoptotic induction, which is caused by the downregulation of the PI3K/Akt signaling pathway.…”

Section: Introductionmentioning

confidence: 99%

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Delivery of paeonol by nanoparticles enhances its in vitro and in vivo antitumor effects

Chen¹,

Feng²,

Hou³

et al. 2017

IJN

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Paeonol (Pae; 2′-hydroxy-4′-methoxyacetophenone) has attracted intense attention as a potential therapeutic agent against various cancers. However, the use of Pae is limited owing to its hydrophobicity. Recently, biodegradable polymeric nanoparticles with amphiphilic copolymers have been used as drug carriers; these have better bioavailability and are promising tumor-targeted drug delivery systems. In the current study, we prepared Pae-loaded nanoparticles (Pae-NPs) with amphiphilic block copolymers using nanoprecipitation. The physiochemical characteristics and antitumor effects of nanoparticles were evaluated in different cancer cells. 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assays showed substantial inhibition of cell growth by Pae-NPs. Moreover, lower doses of Pae-NPs inhibited cell growth more efficiently than the equivalent doses of free Pae. Inhibition was characterized by significant elevation of intracellular reactive oxygen species and subsequent inhibition of Akt and regulation of apoptotic proteins, which could be partly reversed by pretreatment with the antioxidant N-acetylcysteine. In vivo results also demonstrated that Pae-NPs could exert much stronger antitumor effects than free Pae. Therefore, Pae-NPs represent a promising delivery system to overcome the low solubility of Pae and enable its use in treating cancer.

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“…A number of studies have drawn attention to natural products extracted from Chinese medicinal herbs as anticancer agents in cancer therapy (Cragg et al, 1997;Newman and Cragg, 2007;Chen et al, 2012;Li et al, 2010). Among natural products, natural triterpenes represent a structurally diverse group of organic compounds with potent bioactivity including antitumor effects.…”

Section: Introductionmentioning

confidence: 99%

Taraxerone triterpene inhibits cancer cell growth by inducing apoptosis in non-small cell lung cancer cells

Dong

Zhang

et al. 2016

Bangladesh J Pharmacol

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The objective of the present study was to evaluate the anti-cancer effects of taraxerone in non-small cell lung cancer cells (A-549). The effect of this compound on apoptosis and cellular morphology was also studied. MTT (3-(4, 5-dimethylthiazol-2-yl)-2, 5-diphenyltetrazolium bromide) assay was used to evaluate the effect of the compound on cell viability. Cellular morphology after taraxerone treatment was demonstrated by fluorescence microscopy and transmission electron microscopy. The results revealed that taraxerone induced dose-dependent as well as time-dependent growth inhibitory effects on A-549 cell line showing an IC50 value of 53.2 and 61.6 µM at 24 hours and 48 hours time intervals respectively. It also inhibited cancer cell colony formation in a dose-dependent manner and around 90% of the cancer cells were destroyed by the 125 µM dose of taraxerone treatment. Taraxerone also induced cell shrinkage, chromatin condensation and nuclear membrane rupture which are characteristic of apoptosis.

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Paeonol inhibits tumor growth in gastric cancerin vitroandin vivo

Cited by 58 publications

References 17 publications

Formulation Optimization of Gastro-Retention Tablets of Paeonol and Efficacy in Treatment of Experimental Gastric Ulcer

Formulation Optimization of Gastro-Retention Tablets of Paeonol and Efficacy in Treatment of Experimental Gastric Ulcer

Delivery of paeonol by nanoparticles enhances its in vitro and in vivo antitumor effects

Taraxerone triterpene inhibits cancer cell growth by inducing apoptosis in non-small cell lung cancer cells

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