Corilagin

CAS# 23094-69-1

Corilagin

Catalog No. BCN2322----Order now to get a substantial discount!

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Quality Control of Corilagin

Number of papers citing our products

Chemical structure

Corilagin

3D structure

Chemical Properties of Corilagin

Cas No. 23094-69-1 SDF Download SDF
PubChem ID 73568 Appearance White-beige powder
Formula C27H22O18 M.Wt 634.45
Type of Compound Phenols Storage Desiccate at -20°C
Solubility DMSO : 125 mg/mL (197.02 mM; Need ultrasonic)
SMILES C1C2C(C(C(C(O2)OC(=O)C3=CC(=C(C(=C3)O)O)O)O)OC(=O)C4=CC(=C(C(=C4C5=C(C(=C(C=C5C(=O)O1)O)O)O)O)O)O)O
Standard InChIKey TUSDEZXZIZRFGC-XIGLUPEJSA-N
Standard InChI InChI=1S/C27H22O18/c28-9-1-6(2-10(29)16(9)32)24(39)45-27-22(38)23-19(35)13(43-27)5-42-25(40)7-3-11(30)17(33)20(36)14(7)15-8(26(41)44-23)4-12(31)18(34)21(15)37/h1-4,13,19,22-23,27-38H,5H2/t13-,19-,22-,23+,27+/m1/s1
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Source of Corilagin

1 Arctostaphylos sp. 2 Euphorbia sp. 3 Excoecaria sp. 4 Geranium sp. 5 Mallotus sp. 6 Phyllanthus sp. 7 Punica sp. 8 Ricinus sp. 9 Sapium sp. 10 Terminalia sp.

Biological Activity of Corilagin

DescriptionCorilagin 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.
TargetsTLR | TGF-β/Smad | LDL | HO-1 | HSV | IL Receptor | p65 | NF-kB | IkB | TNF-α | Akt | p53 | p21 | Caspase | Adrenergic Receptor | IKK
In vitro

Sensitization of Hep3B hepatoma cells to cisplatin and doxorubicin by corilagin.[Pubmed: 23913631]

Phytother Res. 2014 May;28(5):781-3.

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.

Antiviral effects of Phyllanthus urinaria containing corilagin against human enterovirus 71 and Coxsackievirus A16 in vitro.[Pubmed: 24752860]

Arch Pharm Res. 2015 Feb;38(2):193-202.

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.

Mechanisms of action of corilagin and tellimagrandin I that remarkably potentiate the activity of beta-lactams against methicillin-resistant Staphylococcus aureus.[Pubmed: 14734860]

Microbiol Immunol. 2004;48(1):67-73.

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.

In vivo

Corilagin attenuates aerosol bleomycin-induced experimental lung injury.[Pubmed: 24886817]

Int J Mol Sci. 2014 May 30;15(6):9762-79.

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.

Antioxidant and hepatoprotective actions of medicinal herb, Terminalia catappa L. from Okinawa Island and its tannin corilagin.[Pubmed: 17293097 ]

Phytomedicine. 2007 Nov;14(11):755-62.

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.

Protocol of Corilagin

Kinase Assay

Corilagin Protects Against HSV1 Encephalitis Through Inhibiting the TLR2 Signaling Pathways In Vivo and In Vitro.[Pubmed: 25367881]

Mol Neurobiol. 2014 Nov 4.

In this study, we tried to explore the molecular mechanism that Corilagin protected against herpes simplex virus-1 encephalitis through inhibiting the TLR2 signaling pathways in vivo and in vitro.
METHODS AND RESULTS:
As a result, Corilagin significantly prevented increase in the levels of TLR2 and its downstream mediators following Malp2 or HSV-1 challenge. On the other hand, in spite of TLR2 knockdown, Corilagin could still significantly suppress the expression of P38 and NEMO, phosphor-P38, and nuclear factor kappa B. The mRNA and protein expression of TLR2 and its downstream mediators in the brain tissue were also significantly lowered in mice treated with Corilagin. In addition, Corilagin inhibited expression of tumor necrosis factor-α (TNF-α) and interleukin (IL)-6 protein.
CONCLUSIONS:
In conclusion, Corilagin shows the potential to protect against HSV-1-induced encephalitis, and the beneficial effects may be mediated by inhibiting TLR2 signaling pathways.

Cell Research

Antiatherogenic effects of phyllanthus emblica associated with corilagin and its analogue.[Pubmed: 15997216]

Corilagin inhibits hepatocellular carcinoma cell proliferation by inducing G2/M phase arrest.[Pubmed: 23686743]

Cell Biol Int. 2013 Oct;37(10):1046-54.

Hepatocellular carcinoma (HCC) is one of most common types of malignant tumours. Therefore, it is very important to identify powerful drugs and their antitumour mechanisms. Corilagin has a significant antitumour potential and lower toxicity in normal cells in vitro.
METHODS AND RESULTS:
The IC50 values of Corilagin for normal Chang-liver cells and the HCC cell lines Bel7402 and SMMC7721 were 131.4, 24.5 and 23.4 μM, respectively, in the methyl thiazolyl tetrazolium (MTT) assay. MHCC97-H xenografts in Balb/c mice intraperitoneally injected with 30 mg/kg Corilagin for 5 weeks showed a 47.3% inhibition of tumour growth in vivo. Furthermore, data from flow cytometry and Western blot analyses of cell cycle and cell cycle-related proteins suggest that Corilagin arrests SMMC7721 cells at the G2/M phase by downregulating p-Akt and cyclin B1/cdc2 and upregulating p-p53 and p21(Cip1) .
CONCLUSIONS:
In conclusion, Corilagin is a potential antitumour drug that is effective in retarding the growth of HCC, which is correlated with the activation of p-p53-p21(Cip1) -cdc2/cyclin B1.

Yakugaku Zasshi. 2005 Jul;125(7):587-91.

Oxidized low-density lipoprotein (ox-LDL) is the main etiologic factor in atherogenesis, and antioxidants are accepted as effective treatment of atherosclerosis. The aim of this study was to clarify whether the mechanism of the antiatherogenic effects of the herb Phyllanthus Emblica, which is widely used to treat atherosclerosis-related diseases, is associated with ox-LDL via its compounds of soluble tannin, Corilagin (beta-1-O-galloyl-3,6-(R)-hexahydroxydiphenoyl-d-glucose), and its analogue Dgg16 (1,6-di-O-galloyl-beta-d-glucose).
METHODS AND RESULTS:
Human umbilical vein endothelial cells, ECV-304, were incubated with ox-LDL (50 mg/l), treated with Corilagin or Dgg16 at different doses (0.0001-0.1 mmol/l), and then incubated with monocytes. Malondialdehyde (MDA) in the culture media was determined and the number of monocytes adhering to ECV-304 cells was counted with cytometry. In another experiment, the rat vascular smooth muscular cells (VSMC) were incubated in media with or without ox-LDL (50 mg/l), and with Corilagin or Dgg16 also at different doses (0.0001-0.1 mol/l), the proliferation of which was assayed with MTT. The results showed that both Corilagin and Dgg16 were able to decrease MDA, prevented ECV-304 cells from being adhering to by monocytes, and inhibited VSMC proliferation activated by ox-LDL.
CONCLUSIONS:
The results suggest that the two compounds are effective in inhibiting the progress of atherosclerosis by alleviating oxidation injury or by inhibiting ox-LDL-induced VSMC proliferation, which may be promising mechanisms for treating atherosclerosis.

Animal Research

Antihypertensive effect of corilagin in the rat.[Pubmed: 8748933]

Can J Physiol Pharmacol. 1995 Oct;73(10):1425-9.

The antihypertensive effect of Corilagin, one of the ellagitannins purified from the seeds of Euphoria longana Lam. (Sapindaceae), was investigated in the spontaneously hypertensive rat (SHR).
METHODS AND RESULTS:
Administration of Corilagin into conscious SHR at 5 mg/kg produced an antihypertensive effect equivalent to that induced by 1 mg/kg of guanethidine. This dose-dependent hypotensive effect was comparable with that observed in anesthetized SHR animals. Corilagin did not modify the baroreflex sensitivity in phenylephrine-challenged SHR. Corilagin reduced plasma noradrenaline in a dose-dependent fashion, an effect that was maintained in adrenalectomized rats. Failure of the antagonists for alpha2-adrenoceptors, idazoxan and yohimbine, as well as for dopamine receptors, haloperidol and domperidone, to reverse the antihypertensive actions of Corilagin ruled out the participation of these receptors. Moreover, Corilagin attenuated the pressor effects of methoxamine and Bay K8644 to a similar degree, indicating the direct effect of Corilagin on vascular activity in rats.
CONCLUSIONS:
These results suggest that Corilagin possesses the ability to lower blood pressure through the reduction of noradrenaline release and (or) direct vasorelaxation.

Corilagin Dilution Calculator

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Preparing Stock Solutions of Corilagin

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 1.5762 mL 7.8808 mL 15.7617 mL 31.5234 mL 39.4042 mL
5 mM 0.3152 mL 1.5762 mL 3.1523 mL 6.3047 mL 7.8808 mL
10 mM 0.1576 mL 0.7881 mL 1.5762 mL 3.1523 mL 3.9404 mL
50 mM 0.0315 mL 0.1576 mL 0.3152 mL 0.6305 mL 0.7881 mL
100 mM 0.0158 mL 0.0788 mL 0.1576 mL 0.3152 mL 0.394 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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References on Corilagin

Corilagin Protects Against HSV1 Encephalitis Through Inhibiting the TLR2 Signaling Pathways In Vivo and In Vitro.[Pubmed:25367881]

Mol Neurobiol. 2015 Dec;52(3):1547-1560.

In this study, we tried to explore the molecular mechanism that Corilagin protected against herpes simplex virus-1 encephalitis through inhibiting the TLR2 signaling pathways in vivo and in vitro. As a result, Corilagin significantly prevented increase in the levels of TLR2 and its downstream mediators following Malp2 or HSV-1 challenge. On the other hand, in spite of TLR2 knockdown, Corilagin could still significantly suppress the expression of P38 and NEMO, phosphor-P38, and nuclear factor kappa B. The mRNA and protein expression of TLR2 and its downstream mediators in the brain tissue were also significantly lowered in mice treated with Corilagin. In addition, Corilagin inhibited expression of tumor necrosis factor-alpha (TNF-alpha) and interleukin (IL)-6 protein. In conclusion, Corilagin shows the potential to protect against HSV-1-induced encephalitis, and the beneficial effects may be mediated by inhibiting TLR2 signaling pathways.

Sensitization of Hep3B hepatoma cells to cisplatin and doxorubicin by corilagin.[Pubmed:23913631]

Phytother Res. 2014 May;28(5):781-3.

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. 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. 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.

Antioxidant and hepatoprotective actions of medicinal herb, Terminalia catappa L. from Okinawa Island and its tannin corilagin.[Pubmed:17293097]

Phytomedicine. 2007 Nov;14(11):755-62.

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. 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. 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.

Mechanisms of action of corilagin and tellimagrandin I that remarkably potentiate the activity of beta-lactams against methicillin-resistant Staphylococcus aureus.[Pubmed:14734860]

Microbiol Immunol. 2004;48(1):67-73.

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). 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. 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.

Antihypertensive effect of corilagin in the rat.[Pubmed:8748933]

Can J Physiol Pharmacol. 1995 Oct;73(10):1425-9.

The antihypertensive effect of Corilagin, one of the ellagitannins purified from the seeds of Euphoria longana Lam. (Sapindaceae), was investigated in the spontaneously hypertensive rat (SHR). Administration of Corilagin into conscious SHR at 5 mg/kg produced an antihypertensive effect equivalent to that induced by 1 mg/kg of guanethidine. This dose-dependent hypotensive effect was comparable with that observed in anesthetized SHR animals. Corilagin did not modify the baroreflex sensitivity in phenylephrine-challenged SHR. Corilagin reduced plasma noradrenaline in a dose-dependent fashion, an effect that was maintained in adrenalectomized rats. Failure of the antagonists for alpha2-adrenoceptors, idazoxan and yohimbine, as well as for dopamine receptors, haloperidol and domperidone, to reverse the antihypertensive actions of Corilagin ruled out the participation of these receptors. Moreover, Corilagin attenuated the pressor effects of methoxamine and Bay K8644 to a similar degree, indicating the direct effect of Corilagin on vascular activity in rats. These results suggest that Corilagin possesses the ability to lower blood pressure through the reduction of noradrenaline release and (or) direct vasorelaxation.

Corilagin attenuates aerosol bleomycin-induced experimental lung injury.[Pubmed:24886817]

Int J Mol Sci. 2014 May 30;15(6):9762-79.

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. 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, IKKalpha, phosphorylated IKKalpha (p-IKKalpha), NF-kappaB P65, TNF-alpha and IL-1beta, and reduced I-kappaB 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-beta1 production and alpha-SMA expression in lung tissue samples. Taken together, these findings confirmed that Corilagin attenuates bleomycin-induced epithelial injury and fibrosis via inactivation of oxidative stress, proinflammatory cytokine release and NF-kappaB and TGF-beta1 signaling. Corilagin may serve as a promising therapeutic agent for pulmonary fibrosis.

Antiatherogenic effects of phyllanthus emblica associated with corilagin and its analogue.[Pubmed:15997216]

Yakugaku Zasshi. 2005 Jul;125(7):587-91.

Oxidized low-density lipoprotein (ox-LDL) is the main etiologic factor in atherogenesis, and antioxidants are accepted as effective treatment of atherosclerosis. The aim of this study was to clarify whether the mechanism of the antiatherogenic effects of the herb Phyllanthus Emblica, which is widely used to treat atherosclerosis-related diseases, is associated with ox-LDL via its compounds of soluble tannin, Corilagin (beta-1-O-galloyl-3,6-(R)-hexahydroxydiphenoyl-d-glucose), and its analogue Dgg16 (1,6-di-O-galloyl-beta-d-glucose). Human umbilical vein endothelial cells, ECV-304, were incubated with ox-LDL (50 mg/l), treated with Corilagin or Dgg16 at different doses (0.0001-0.1 mmol/l), and then incubated with monocytes. Malondialdehyde (MDA) in the culture media was determined and the number of monocytes adhering to ECV-304 cells was counted with cytometry. In another experiment, the rat vascular smooth muscular cells (VSMC) were incubated in media with or without ox-LDL (50 mg/l), and with Corilagin or Dgg16 also at different doses (0.0001-0.1 mol/l), the proliferation of which was assayed with MTT. The results showed that both Corilagin and Dgg16 were able to decrease MDA, prevented ECV-304 cells from being adhering to by monocytes, and inhibited VSMC proliferation activated by ox-LDL. The results suggest that the two compounds are effective in inhibiting the progress of atherosclerosis by alleviating oxidation injury or by inhibiting ox-LDL-induced VSMC proliferation, which may be promising mechanisms for treating atherosclerosis.

Corilagin inhibits hepatocellular carcinoma cell proliferation by inducing G2/M phase arrest.[Pubmed:23686743]

Cell Biol Int. 2013 Oct;37(10):1046-54.

Hepatocellular carcinoma (HCC) is one of most common types of malignant tumours. Therefore, it is very important to identify powerful drugs and their antitumour mechanisms. Corilagin has a significant antitumour potential and lower toxicity in normal cells in vitro. The IC50 values of Corilagin for normal Chang-liver cells and the HCC cell lines Bel7402 and SMMC7721 were 131.4, 24.5 and 23.4 microM, respectively, in the methyl thiazolyl tetrazolium (MTT) assay. MHCC97-H xenografts in Balb/c mice intraperitoneally injected with 30 mg/kg Corilagin for 5 weeks showed a 47.3% inhibition of tumour growth in vivo. Furthermore, data from flow cytometry and Western blot analyses of cell cycle and cell cycle-related proteins suggest that Corilagin arrests SMMC7721 cells at the G2/M phase by downregulating p-Akt and cyclin B1/cdc2 and upregulating p-p53 and p21(Cip1) . In conclusion, Corilagin is a potential antitumour drug that is effective in retarding the growth of HCC, which is correlated with the activation of p-p53-p21(Cip1) -cdc2/cyclin B1.

Antiviral effects of Phyllanthus urinaria containing corilagin against human enterovirus 71 and Coxsackievirus A16 in vitro.[Pubmed:24752860]

Arch Pharm Res. 2015 Feb;38(2):193-202.

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. 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 mug/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. Collectively, our work provides potential candidates for the development of novel drugs to treat HFMD.

Description

Corilagin, a gallotannin, is isolated from Caesalpinia coriaria (Jacq.) Willd. Corilagin inhibits activity of reverse transcriptase of RNA tumor viruses. Corilagin inhibits the growth of Staphylococcus aureus with a MIC of 25 μg/mL. Corilagin shows good anti-tumor activity on hepatocellular carcinoma and ovarian cancer. Corilagin shows a low level of toxicity toward normal cells and tissues.

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