Shikonin inhibits IgE-mediated histamine release by human basophils and Syk kinase activity

Takano‐Ohmuro, Hiromi; Yoshida, Lucia S.; Yuda, Yasukatsu; Morioka, Kazuyuki; Kitani, Seiichi

doi:10.1007/s00011-008-8067-9

Cited by 19 publications

(19 citation statements)

References 37 publications

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“…The presence of shikonin caused a small increase in the average fiber diameter, but it did not affect their morphology, since their surface was also smooth as previously described (Taepaiboon et al, 2007;Tungprapa et al, 2007). Additionally, increasing the drug loading did not cause a significant effect on the mean fiber size, although it is a common effect of the drug loading, as reported elsewhere (Deitzel et al, 2001;Puppi et al, 2010;Takano-Ohmuro et al, 2008).…”

Section: Shikonin-loaded Fiberssupporting

confidence: 64%

Electrospun fiber mats containing shikonin and derivatives with potential biomedical applications

Kontogiannopoulos

Assimopoulou

Tsivintzelis

et al. 2011

International Journal of Pharmaceutics

147

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Section: Shikonin-loaded Fiberssupporting

confidence: 64%

Electrospun fiber mats containing shikonin and derivatives with potential biomedical applications

Kontogiannopoulos

Assimopoulou

Tsivintzelis

et al. 2011

International Journal of Pharmaceutics

147

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“…Shikonin might be used in the treatment of asthma. Takano-Ohmuro et al (2008) has explored the use of shikonin in asthma by focusing on its anti-inflammatory activity (Takano-Ohmuro et al, 2008). Other investigators have used a mouse asthma model to demonstrate that shikonin inhibits bone marrow-derived dendritic cell maturation in vitro , and allergic action as well as tracheal hyperresponsiveness in vivo (Lee et al, 2010).…”

Section: Discussionmentioning

confidence: 99%

Shikonin Inhibits Intestinal Calcium-Activated Chloride Channels and Prevents Rotaviral Diarrhea

Jiang

Yang

et al. 2016

Front. Pharmacol.

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Secretory diarrhea remains a global health burden and causes major mortality in children. There have been some focuses on antidiarrheal therapies that may reduce fluid losses and intestinal motility in diarrheal diseases. In the present study, we identified shikonin as an inhibitor of TMEM16A chloride channel activity using cellbased fluorescent-quenching assay. The IC 50 value of shikonin was 6.5 µM. Shortcircuit current measurements demonstrated that shikonin inhibited E act -induced Cl − current in a dose-dependent manner, with IC 50 value of 1.5 µM. Short-circuit current measurement showed that shikonin exhibited inhibitory effect against CChinduced Cl − currents in mouse colonic epithelia but did not affect cytoplasmic Ca 2+ concentration as well as the other major enterocyte chloride channel conductance regulator. Characterization study found that shikonin inhibited basolateral K + channel activity without affecting Na + /K + -ATPase activities. In vivo studies revealed that shikonin significantly delayed intestinal motility in mice and reduced stool water content in a neonatal mice model of rotaviral diarrhea without affecting the viral infection process in vivo. Taken together, the results suggested that shikonin inhibited enterocyte calciumactivated chloride channels, the inhibitory effect was partially through inhbition of basolateral K + channel activity, and shikonin could be a lead compound in the treatment of rotaviral secretory diarrhea.

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“…Shikonin, one of the main active components of Zi Cao, has been shown to exert anti-inflammatory and anti-cancer effects both in vitro and in vivo (Wang et al, 1994; Yang et al, 2009a). Several molecular targets of shikonin have also been proposed (Wang et al, 1994; Staniforth et al, 2004; Nam et al, 2008; Su et al, 2008; Takano-Ohmuro et al, 2008; Yang et al, 2009a). We also reported that the proteasome is one of the important molecular targets of shikonin (Yang et al, 2009a).…”

Section: Introductionmentioning

confidence: 99%

Shikonin extracted from medicinal Chinese herbs exerts anti-inflammatory effect via proteasome inhibition

Lu¹,

Qin²,

Huang³

et al. 2011

European Journal of Pharmacology

139

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Shikonin, extracted from medicinal Chinese herb (Lithospermum erythrorhizo), was reported to exert anti-inflammatory and anti-cancer effects both in vitro and in vivo. We have found that proteasome was a molecular target of shikonin in tumor cells, but whether shikonin targets macrophage proteasome needs to be investigated. In the current study, we report that shikonin inhibited inflammation in mouse models as efficiently as dexamethasone. Shikonin at 4 μM reduced the Lipopolysaccharides (LPS)-mediated TNFα release in rat primary macrophage cultures, and blocked the translocation of p65-NF-κB from the cytoplasm to the nucleus, associated with decreased proteasomal activity. Consistently, shikonin accumulated IκB-α, an inhibitor of NF-κB, and ubiquitinated proteins in rat primary macrophage cultures, demonstrating that the proteasome is a target of shikonin under inflammatory conditions. Shikonin also induced macrophage cell apoptosis and cell death. These results demonstrate for the first time that proteasome inhibition by shikonin contributes to its anti-inflammatory effect. The novel finding about macrophage proteasome as a target of shikonin suggests that this medicinal compound has great potential to be developed into an anti-inflammatory agent.

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Shikonin inhibits IgE-mediated histamine release by human basophils and Syk kinase activity

Abstract: These results indicate that the inhibition of Syk-dependent phosphorylation events might underlie the blocked histamine release from human basophils, thus contributing to the anti-inflammatory effects of shikonin.

Cited by 19 publications

References 37 publications

Electrospun fiber mats containing shikonin and derivatives with potential biomedical applications

Electrospun fiber mats containing shikonin and derivatives with potential biomedical applications

Shikonin Inhibits Intestinal Calcium-Activated Chloride Channels and Prevents Rotaviral Diarrhea

Shikonin extracted from medicinal Chinese herbs exerts anti-inflammatory effect via proteasome inhibition

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