Therapeutic Effects of Apamin as a Bee Venom Component for Non-Neoplastic Disease

Gu, Hyemin; Han, Sang‐Mi; Park, Kwan‐Kyu

doi:10.3390/toxins12030195

Cited by 54 publications

(53 citation statements)

References 142 publications

(205 reference statements)

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“…These effects were attributed to inhibition of oxidative stress, apoptosis, and inflammation. Although previous studies have shown the beneficial effect of apamin against several inflammatory diseases [13][14][15][16][17][18], our study is the first to demonstrate the therapeutic action of apamin on LPS-induced AKI.…”

Section: Discussionmentioning

confidence: 65%

“…Much research has focused on the biological effects and clinical potential of bee venom and its main component, melittin [10][11][12]. However, accumulating evidence also has highlighted the importance of apamin as a drug candidate [13]. Apamin has been shown to exert anti-inflammatory, antioxidative, and antiapoptotic activities in animal models of several inflammatory diseases, including gouty arthritis [14], multiple sclerosis [15], chronic liver disease [16], acute pancreatitis [17], and atherosclerosis [18].…”

Section: Introductionmentioning

confidence: 99%

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Antioxidative, Antiapoptotic, and Anti-Inflammatory Effects of Apamin in a Murine Model of Lipopolysaccharide-Induced Acute Kidney Injury

2020

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Sepsis is the major cause of acute kidney injury (AKI) in severely ill patients, but only limited therapeutic options are available. During sepsis, lipopolysaccharide (LPS), an endotoxin derived from bacteria, activates signaling cascades involved in inflammatory responses and tissue injury. Apamin is a component of bee venom and has been shown to exert antioxidative, antiapoptotic, and anti-inflammatory activities. However, the effect of apamin on LPS-induced AKI has not been elucidated. Here, we show that apamin treatment significantly ameliorated renal dysfunction and histological injury, especially tubular injury, in LPS-injected mice. Apamin also suppressed LPS-induced oxidative stress through modulating the expression of nicotinamide adenine dinucleotide phosphate oxidase 4 and heme oxygenase-1. Moreover, tubular cell apoptosis with caspase-3 activation in LPS-injected mice was significantly attenuated by apamin. Apamin also inhibited cytokine production and immune cell accumulation, suppressed toll-like receptor 4 pathway, and downregulated vascular adhesion molecules. Taken together, these results suggest that apamin ameliorates LPS-induced renal injury through inhibiting oxidative stress, apoptosis of tubular epithelial cells, and inflammation. Apamin might be a potential therapeutic option for septic AKI.

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Section: Discussionmentioning

confidence: 65%

Section: Introductionmentioning

confidence: 99%

Antioxidative, Antiapoptotic, and Anti-Inflammatory Effects of Apamin in a Murine Model of Lipopolysaccharide-Induced Acute Kidney Injury

2020

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“…APM has long been known as a specifically selective blocker of SK2 channels [ 27 ]. Ca 2+ /calmodulin-dependent protein kinase II (CaMKII), one of the main downstream targets of Ca 2+ and CaM, is activated by Ca 2+ /CaM [ 29 ].…”

Section: Resultsmentioning

confidence: 99%

“…Our previous studies have confirmed that APM is an anti-inflammatory and antiapoptotic agent that acts through vascular smooth muscle cell migration [ 22 ], biliary fibrosis and activation of hepatic stellate cells [ 23 ], TNFα/interferon (IFN)γ-induced keratinocytes [ 24 ], LPS/fat-induced atherosclerotic mice [ 25 ], and macrophage activation [ 26 ]. In addition, we recently investigated and reported the effect of APM on nonneoplastic disease [ 27 ]. Although studies have investigated the physiological function of APM, including anti-inflammatory and antiapoptotic functions, the effectiveness of APM related to LPS-induced microglial neuroinflammation has not been evaluated.…”

Section: Introductionmentioning

confidence: 99%

Apamin Suppresses LPS-Induced Neuroinflammatory Responses by Regulating SK Channels and TLR4-Mediated Signaling Pathways

Park

Jang

Park

2020

IJMS

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Neuroinflammation plays a vital role in neurodegenerative conditions. Microglia are a key component of the neuroinflammatory response. There is a growing interest in developing drugs to target microglia and thereby control neuroinflammatory processes. Apamin (APM) is a specifically selective antagonist of small conductance calcium-activated potassium (SK) channels. However, its effect on neuroinflammation is largely unknown. We examine the effects of APM on lipopolysaccharide (LPS)-stimulated BV2 and rat primary microglial cells. Regarding the molecular mechanism by which APM significantly inhibits proinflammatory cytokine production and microglial cell activation, we found that APM does so by reducing the expression of phosphorylated CaMKII and toll-like receptor (TLR4). In particular, APM potently suppressed the translocation of nuclear factor kappa-light-chain-enhancer of activated B cells (NF-κB)/signal transducer and activator of transcription (STAT)3 and phosphorylated mitogen-activated protein kinases (MAPK)-extracellular signal-regulated kinase (ERK). In addition, the correlation of NF-κB/STAT3 and MAPK-ERK in the neuroinflammatory response was verified through inhibitors. The literature and our findings suggest that APM is a promising candidate for an anti-neuroinflammatory agent and can potentially be used for the prevention and treatment of various neurological disorders.

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“…Moreover, apamin can activate the inhibitory muscarinic M2 receptors in motor nerve terminals reducing the neuromuscular transmission [78]. Therefore, this capacity gives apamin the potential to be a part of the treatment of different CNS diseases [79].…”

Section: Apaminmentioning

confidence: 99%

Bee Venom: An Updating Review of Its Bioactive Molecules and Its Health Applications

2020

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Bee venom (BV) is usually associated with pain since, when humans are stung by bees, local inflammation and even an allergic reaction can be produced. BV has been traditionally used in ancient medicine and in acupuncture. It consists of a mixture of substances, principally of proteins and peptides, including enzymes as well as other types of molecules in a very low concentration. Melittin and phospholipase A2 (PLA2) are the most abundant and studied compounds of BV. Literature of the main biological activities exerted by BV shows that most studies focuses on the comprehension and test of anti-inflammatory effects and its mechanisms of action. Other properties such as antioxidant, antimicrobial, neuroprotective or antitumor effects have also been assessed, both in vitro and in vivo. Moreover, human trials are necessary to confirm those clinical applications. However, notwithstanding the therapeutic potential of BV, there are certain problems regarding its safety and the possible appearance of adverse effects. On this perspective, new approaches have been developed to avoid these complications. This manuscript is aimed at reviewing the actual knowledge on BV components and its associated biological activities as well as the latest advances on this subject.

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Therapeutic Effects of Apamin as a Bee Venom Component for Non-Neoplastic Disease

Cited by 54 publications

References 142 publications

Antioxidative, Antiapoptotic, and Anti-Inflammatory Effects of Apamin in a Murine Model of Lipopolysaccharide-Induced Acute Kidney Injury

Antioxidative, Antiapoptotic, and Anti-Inflammatory Effects of Apamin in a Murine Model of Lipopolysaccharide-Induced Acute Kidney Injury

Apamin Suppresses LPS-Induced Neuroinflammatory Responses by Regulating SK Channels and TLR4-Mediated Signaling Pathways

Bee Venom: An Updating Review of Its Bioactive Molecules and Its Health Applications

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