Baicalein inhibits pulmonary carcinogenesis-associated inflammation and interferes with COX-2, MMP-2 and MMP-9 expressions in-vivo

Naveenkumar, Chandrashekar; Asokkumar, Selvamani; Raghunandhakumar, Subramanian; Anandakumar, Pandi; Devaki, Thiruvengadam

doi:10.1016/j.taap.2012.02.004

Cited by 68 publications

(43 citation statements)

References 52 publications

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“…It has been reported that COX-2 and ICAM-1 play an important role in the precursor lesions of human lung adenocarcinoma and lung epithelium inflammation [20][21][22][23]. CS increases inflammatory responses which result in the changes of lung function, morphology and gene expression [24,25].…”

Section: Discussionmentioning

confidence: 99%

Wedelolactone protects human bronchial epithelial cell injury against cigarette smoke extract-induced oxidant stress and inflammation responses through Nrf2 pathway

Ding

Hou

Yuan

et al. 2015

International Immunopharmacology

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Section: Discussionmentioning

confidence: 99%

Wedelolactone protects human bronchial epithelial cell injury against cigarette smoke extract-induced oxidant stress and inflammation responses through Nrf2 pathway

Ding

Hou

Yuan

et al. 2015

International Immunopharmacology

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“…In the past decade, there has been great progress in exploring the target mechanisms and signaling pathways of baicalein’s anti-cancer potential. The main molecular mechanisms of the anti-tumor effects of baicalein include inhibiting several cyclins or cyclin-dependent kinases (CDKs) to regulate the cell cycle [9], scavenging oxidative radicals, attenuating MAPK, Akt or mTOR activities [15], inducing apoptosis through activating caspase-9/-3 [11] and inhibiting tumor invasion and metastasis by reducing the expression of MMP-2/-9 [14]. As shown in Figure 2, we summarized the relevant biological mechanisms of baicalein involved in inhibiting various types of cancer (e.g., bladder cancer, breast cancer, cervical cancer, colorectal cancer, gastric cancer, hepatocellular carcinoma, osteosarcoma, multiple myeloma, melanoma/skin cancer, ovarian cancer, pancreatic cancer, prostate cancer, and lung cancer).…”

Section: The Property and Antitumor Effect Of Baicaleinmentioning

confidence: 99%

“…Baicalein is a flavone and an active ingredient in the traditional herb, Huang Qin. There is an accumulating amount of evidence that demonstrates baicalein’s role in treating and preventing various types of cancer [9,10,11,12,13,14,15]. In this review, we explored its chemical structure, properties, and possible biological mechanisms through which it acts.…”

Section: Introductionmentioning

confidence: 99%

The Fascinating Effects of Baicalein on Cancer: A Review

Liu

Dong

Gao

et al. 2016

IJMS

191

133

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Cancer is one of the leading causes of death worldwide and a major global health problem. In recent decades, the rates of both mortality and morbidity of cancer have rapidly increased for a variety of reasons. Despite treatment options, there are serious side effects associated with chemotherapy drugs and multiple forms of drug resistance that significantly reduce their effects. There is an accumulating amount of evidence on the pharmacological activities of baicalein (e.g., anti-inflammatory, antioxidant, antiviral, and antitumor effects). Furthermore, there has been great progress in elucidating the target mechanisms and signaling pathways of baicalein’s anti-cancer potential. The anti-tumor functions of baicalein are mainly due to its capacities to inhibit complexes of cyclins to regulate the cell cycle, to scavenge oxidative radicals, to attenuate mitogen activated protein kinase (MAPK), protein kinase B (Akt) or mammalian target of rapamycin (mTOR) activities, to induce apoptosis by activating caspase-9/-3 and to inhibit tumorinvasion and metastasis by reducing the expression of matrix metalloproteinase-2/-9 (MMP-2/-9). In this review, we focused on the relevant biological mechanisms of baicalein involved in inhibiting various cancers, such as bladder cancer, breast cancer, and ovarian cancer. Moreover, we also summarized the specific mechanisms by which baicalein inhibited the growth of various tumors in vivo. Taken together, baicalein may be developed as a potential, novel anticancer drug to treat tumors.

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“…Baicalein (3,4,5-trihyroxyfurane), a flavonoid with well-established anti-inflammatory and antioxidant properties, is extracted from the root of Scutellaria baicalensis [6][7][8][9][10][11]. Furthermore, baicalein has an inhibitory effect on several cancers including colorectal, lung, breast and prostate carcinomas.…”

Section: Introductionmentioning

confidence: 99%

Baicalein induces autophagic cell death through AMPK/ULK1 activation and downregulation of mTORC1 complex components in human cancer cells

et al. 2014

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Baicalein, a flavonoid and aglycon hydrolyzed from baicalin, has anticancer properties in several human carcinomas, but its molecular mechanisms of action remain unclear. Here, we show that baicalein leads to human cancer cell death by inducing autophagy rather than apoptosis, because cell death induced by baicalein was completely reversed by suppressing the expression levels of key molecules in autophagy such as Beclin 1, vacuolar protein sorting 34 (Vps34), autophagy-related (Atg)5 and Atg7, but not by pan-caspase inhibitor. Our data revealed that baicalein significantly increased the number of green fluorescence protein-cytosol-associated protein light chain 3 (GFP-LC3)-containing puncta and LC3B-II expression levels, which were further enhanced by chloroquine treatment. Furthermore, a luciferase-based reporter assay showed that the ratio of RLuc-LC3wt/RLuc-LC3G120A was greatly reduced. The data suggested that baicalein induced not only autophagosome formation, but also autophagic flux. Experiments using short interfering RNAs and pharmacological inhibitors revealed that Beclin 1, Vps34, Atg5, Atg7 and UNC-51 (Caenorhabditis elegans)-like kinase 1 (ULK1) play pivotal roles in mediating baicalein-induced autophagy. Moreover, baicalein activated AMP-activated protein kinase (AMPK)a, leading to ULK1 activation through phosphorylation at Ser555, whereas both protein and mRNA levels of mammalian target of rapamycin (mTOR) and Raptor, upstream inhibitors of ULK1 and autophagy, were markedly downregulated by baicalein. Our data suggest that the anticancer effects of baicalein are mainly due to autophagic cell death through activation of the AMPK/ULK1 pathway and inhibition of mTOR/Raptor complex 1 expression. These results provide new mechanistic insights into the anticancer functions of autophagy inducers, such as baicalein, which may be used as potential therapeutics for cancer treatment.Abbreviations Δwmt, mitochondrial membrane potential; 3-MA, 3-methyladenine; AMPK, AMP-activated protein kinase; Atg, autophagy-related; cdk, cyclindependent kinase; CQ, chloroquine; DMEM, Dulbecco's modified Eagle's medium; FLICA, fluorescent-labeled inhibitor of caspases; GFP, green fluorescent protein; LC3, microtubule-associated protein light chain 3; mTORC1, mammalian target of kanamycin complex 1; PARP, poly(ADP-ribose) polymerase; PtdIns3K, phosphoinositide 3-kinase; PtIns3P, phosphatidylinositol-3-phosphate; Raptor, regulatory-associated protein of mTOR; siRNA, small interfering RNA; ULK1, UNC-51 (C. elegans)-like kinase 1; Vps34, vacuolar protein sorting 34; wt, wild-type.

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Baicalein inhibits pulmonary carcinogenesis-associated inflammation and interferes with COX-2, MMP-2 and MMP-9 expressions in-vivo

Cited by 68 publications

References 52 publications

Wedelolactone protects human bronchial epithelial cell injury against cigarette smoke extract-induced oxidant stress and inflammation responses through Nrf2 pathway

Wedelolactone protects human bronchial epithelial cell injury against cigarette smoke extract-induced oxidant stress and inflammation responses through Nrf2 pathway

The Fascinating Effects of Baicalein on Cancer: A Review

Baicalein induces autophagic cell death through AMPK/ULK1 activation and downregulation of mTORC1 complex components in human cancer cells

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