| Description: |
Corilagin has antitumour, anti-inflammatory, antioxidant, antifibrotics, antiviral, antibacterial, hepatoprotective, antiatherogenic, and antihypertensive activities. Corilagin reduces the cytotoxicity induced by EV71 or CA16 on Vero cells with and IC50 value of 5.6 and 32.33 μg/mL, respectively; it shows the potential to protect against HSV-1-induced encephalitis, and the beneficial effects may be mediated by inhibiting TLR2 signaling pathways. Corilagin attenuates bleomycin-induced epithelial injury and fibrosis via inactivation of oxidative stress, proinflammatory cytokine release and NF-κB and TGF-β1 signaling; it suppresses the activity of beta-lactamase to some extent. |
| Targets: |
TLR | TGF-β/Smad | LDL | HO-1 | HSV | IL Receptor | p65 | NF-kB | IkB | TNF-α | Akt | p53 | p21 | Caspase | Adrenergic Receptor | IKK |
| In vitro: |
| Phytother Res. 2014 May;28(5):781-3. | | Sensitization of Hep3B hepatoma cells to cisplatin and doxorubicin by corilagin.[Pubmed: 23913631] | The anticancer action of gallotannins is a well-developed topic. We have demonstrated the in vivo antitumour activity of Corilagin on Hep3B hepatoma using the xenograft athymic nude mice model.
METHODS AND RESULTS:
Here, we further report the potential sensitization of Hep3B hepatoma cells to cisplatin and doxorubicin by Corilagin. Our results showed that Corilagin is able to enhance the cytotoxicity of both cisplatin and doxorubicin on the Hep3B hepatoma cells.
CONCLUSIONS:
We speculate the possible use of Corilagin in combination with low dosages of the anticancer chemotherapeutic standard drugs like cisplatin and doxorubicin, with the aim of obtaining an increment in the anticancer effect. | | Arch Pharm Res. 2015 Feb;38(2):193-202. | | Antiviral effects of Phyllanthus urinaria containing corilagin against human enterovirus 71 and Coxsackievirus A16 in vitro.[Pubmed: 24752860] | Human enterovirus 71 (EV71) and Coxsackievirus A16 (CA16) are major causative agents of hand, foot, and mouth disease (HFMD) especially in infants and children under 5 years of age. Despite recent outbreaks of HFMD, there are no approved therapeutics against EV71 and CA16 infection. Moreover, in a small percentage of cases, the disease progression can lead to serious complications of the central nervous system.
METHODS AND RESULTS:
In this study, we investigated the antiviral effect of Corilagin and Phyllanthus urinaria extract, which contains Corilagin as a major component, on EV71 and CA16 infection in vitro. Our results indicate that Corilagin reduces the cytotoxicity induced by EV71 or CA16 on Vero cells with and IC50 value of 5.6 and 32.33 μg/mL, respectively. We confirmed the presence of Corilagin in EtOAc and BuOH fractions from P. urinaria extract and this correlated with antiviral activity of the fractions against EV71 or CA16. Future studies will be required to confirm the antiviral activity of Corilagin and P. urinaria extract in vivo. Challenging a model with a lethal dose of viral infection will be required to test this.
CONCLUSIONS:
Collectively, our work provides potential candidates for the development of novel drugs to treat HFMD. | | Microbiol Immunol. 2004;48(1):67-73. | | Mechanisms of action of corilagin and tellimagrandin I that remarkably potentiate the activity of beta-lactams against methicillin-resistant Staphylococcus aureus.[Pubmed: 14734860] | Corilagin and tellimagrandin I are polyphenols isolated from the extract of Arctostaphylos uvaursi and Rosa canina L. (rose red), respectively. We have reported that Corilagin and tellimagrandin I remarkably reduced the minimum inhibitory concentration (MIC) of beta-lactams in methicillin-resistant Staphylococcus aureus(MRSA).
METHODS AND RESULTS:
In this study, we investigated the effect of Corilagin and tellimagrandin I on the penicillin binding protein 2 '(2a) (PBP2 '(PBP2a)) which mainly confers the resistance to beta-lactam antibiotics in MRSA. These compounds when added to the culture medium were found to decrease production of the PBP2 '(PBP2a) slightly. Using BOCILLIN FL, a fluorescent-labeled benzyl penicillin, we found that PBP2 '(PBP2a) in MRSA cells that were grown in medium containing Corilagin or tellimagrandin I almost completely lost the ability to bind BOCILLIN FL. The binding activity of PBP2 and PBP3 were also reduced to some extent by these compounds.
CONCLUSIONS:
These results indicate that inactivation of PBPs, especially of PBP2 '(PBP2a), by Corilagin or tellimagrandin I is the major reason for the remarkable reduction in the resistance level of beta-lactams in MRSA. Corilagin or tellimagrandin I suppressed the activity of beta-lactamase to some extent. | | Biomed Pharmacother . 2018 Mar;99:43-50. | | Corilagin, a promising medicinal herbal agent[Pubmed: 29324311] | | Abstract
Corilagin, a gallotannin, is one of the major active components of many ethnopharmacological plants. It was isolated from Caesalpinia coriaria (Jacq.) Willd. (dividivi) by Schmidt in 1951 for the first time. In the past few decades, Corilagin was reported to exhibit anti-tumor, anti-inflammatory and hepatoprotective activities, etc. However, little attention was paid to its pharmacological properties due to the complicated and inefficient extract method. In recent years, with the development of extraction technology Corilagin was much easier to obtain than before. Thus, people return to pay attention to its anti-tumor, hepatoprotective, and anti-inflammatory activities, particularly as an anti-tumor agent candidate. Our research team had focused on the distribution, preparation and anti-tumor activity of Corilagin since 2005. We found Corilagin showed good anti-tumor activity on hepatocellular carcinoma and ovarian cancer. What's more, Corilagin showed a low level of toxicity toward normal cells and tissues. Due to the extensive attention that Corilagin has received, we present a systematic review of the pharmacological effects of Corilagin. In this review, we summarized all the pharmacological effects of Corilagin with a focus on the molecular mechanism of anti-tumor activity and show you how Corilagin affected the signaling pathways of tumor cells as well as its physicochemical properties, distribution and preparation methods.
Keywords: Anti-inflammation; Anti-tumor; Corilagin; Hepatoprotective; Pharmacological effect; Signaling pathway. |
|
| In vivo: |
| Int J Mol Sci. 2014 May 30;15(6):9762-79. | | Corilagin attenuates aerosol bleomycin-induced experimental lung injury.[Pubmed: 24886817] | Idiopathic pulmonary fibrosis (IPF) is a progressing lethal disease with few clinically effective therapies. Corilagin is a tannin derivative which shows anti-inflammatory and antifibrotics properties and is potentiated in treating IPF.
METHODS AND RESULTS:
Here, we investigated the effect of Corilagin on lung injury following bleomycin exposure in an animal model of pulmonary fibrosis. Corilagin abrogated bleomycin-induced lung fibrosis as assessed by H&E; Masson's trichrome staining and lung hydroxyproline content in lung tissue. Corilagin reduced the number of apoptotic lung cells and prevented lung epithelial cells from membrane breakdown, effluence of lamellar bodies and thickening of the respiratory membrane. Bleomycin exposure induced expression of MDA, IKKα, phosphorylated IKKα (p-IKKα), NF-κB P65, TNF-α and IL-1β, and reduced I-κB expression in mice lung tissue or in BALF. These changes were reversed by high-dose Corilagin (100 mg/kg i.p) more dramatically than by low dose (10 mg/kg i.p). Last, Corilagin inhibits TGF-β1 production and α-SMA expression in lung tissue samples.
CONCLUSIONS:
Taken together, these findings confirmed that Corilagin attenuates bleomycin-induced epithelial injury and fibrosis via inactivation of oxidative stress, proinflammatory cytokine release and NF-κB and TGF-β1 signaling. Corilagin may serve as a promising therapeutic agent for pulmonary fibrosis. | | Phytomedicine. 2007 Nov;14(11):755-62. | | Antioxidant and hepatoprotective actions of medicinal herb, Terminalia catappa L. from Okinawa Island and its tannin corilagin.[Pubmed: 17293097 ] | The antioxidant and hepatoprotective actions of Terminalia catappa L. collected from Okinawa Island were evaluated in vitro and in vivo using leaves extract and isolated antioxidants.
METHODS AND RESULTS:
A water extract of the leaves of T. catappa showed a strong radical scavenging action for 1,1-diphenyl-2-picrylhydrazyl and superoxide (O(2)(.-)) anion. Chebulagic acid and Corilagin were isolated as the active components from T. catappa. Both antioxidants showed a strong scavenging action for O(2)(.-) and peroxyl radicals and also inhibited reactive oxygen species production from leukocytes stimulated by phorbol-12-myristate acetate. Galactosamine (GalN, 600 mg/kg, s.c.,) and lipopolysaccharide (LPS, 0.5 microg/kg, i.p.)-induced hepatotoxicity of rats as seen by an elevation of serum alanine aminotransferase, aspartate aminotransferase and glutathione S-transferase (GST) activities was significantly reduced when the herb extract or Corilagin was given intraperitoneally to rats prior to GalN/LPS treatment. Increase of free radical formation and lipid peroxidation in mitochondria caused by GalN/LPS treatment were also decreased by pretreatment with the herb/Corilagin. In addition, apoptotic events such as DNA fragmentation and the increase in caspase-3 activity in the liver observed with GalN/LPS treatment were prevented by the pretreatment with the herb/Corilagin.
CONCLUSIONS:
These results show that the extract of T. catappa and its antioxidant, Corilagin are protective against GalN/LPS-induced liver injury through suppression of oxidative stress and apoptosis. |
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