• Advances in Traditional Medicine
• /
• v.8 no.1
• /
• pp.24-31
• /
• 2008

In the present investigation, we studied the effect of alcoholic extract of Moringa oleifera (M. oleifera) seed kernels on various experimental models of bronchial asthma. Significant (P < 0. 05) increase in preconvulsion time was observed due to pretreatment with M. oleifera when the guinea pigs were exposed to either acetylcholine (Ach) or histamine aerosol. This bronchodilating effect of M. oleifera was comparable to ketotifen fumarate. Spasmolytic effect of M. oleifera was also observed by dose dependent inhibition of ideal contractions induced by Ach, 5HT, histamine and $BaCl_2$. Alcoholic extract of M. oleifera produced significant dose dependent protection by egg albumin and compound 48/80 induced mast cell degranulation. Pretreatment with alcoholic extract of M. oleifera also decreased carrageenan induced rat paw edema, which was comparable to that of standard diclofenac sodium. Minimum inhibitory concentration for alcoholic extract of M. oleifera was low as compared to cold-water extract and hot water extract when antimicrobial activity was tested against various respiratory pathogens like Escherichia coli (E. coli), Staphylococus aureus (S. aureus) and pseudomonas aeruginosa (P. aeruginosa). Our data suggest that antiasthmatic activity of M. oleifera seed kernels may be due to its bronchodilator, anti-inflammatory, mast cell stabilization and antimicrobial activity.

• Korean Journal of Food Science and Technology
• /
• v.48 no.1
• /
• pp.86-91
• /
• 2016

Oxidative stress caused by reactive oxygen species is ascribed to many neurodegenerative diseases like Alzheimer's disease. Phenolic antioxidants can reduce the oxidative stress. In this study, ripe fruits of Opuntia ficus-indica var. saboten (OFS) were extracted using 80% (v/v) aqueous ethanol. Total phenolic and flavonoid contents of the OFS fruits (100 g) were 409.9 mg gallic acid equivalents and 72.2 mg catechin equivalents, respectively. The OFS fruits had antioxidant capacity at 381.2, 298.2, and 3,219.9 mg vitamin C equivalents/100 g in ABTS, DPPH, and ORAC assays, respectively. The OFS fruits showed protective effects on PC-12 cells against oxidative stress in a dose-dependent manner, partly due to decrease of intracellular oxidative stress. Furthermore, the OFS fruits inhibited both acetylcholinesterase and butyrylcholinesterase. Consequently, these results suggest that the OFS fruits might be served as a source of functional materials to reduce oxidative stress in neuronal cells and to inhibit cholinesterases.

• Journal of Food Hygiene and Safety
• /
• v.16 no.1
• /
• pp.21-26
• /
• 2001

Risk assessment traditionally are conducted on individual chemicals; however, humans are exposed to multiple chemicals in daily life. The organophosphorus (OP) pesticides are considered in a single risk assessment because they act by a common mechanism of toxicity, and there is likely to be expose to multiple OP pesticides simultaneously or sequentially. The OP pesticides act by inhibiting the enzyme acetylcholinesterasc (AChE) and have available extensive database. AChE is widely distributed throughout the body, most importantly in the nervous system. Inhibition of AChE results in accumulation of acetylcholine in the nervous system that results in clinical signs of cholinergic toxicity, including increased salivation and lacrimation, nausea and vomiting, muscle fasciculation, lethargy and fatigue, among others. To conduct an exposure assessment for pesticides in the diet, we need to know the food consumption patterns of the populations, and the pesticide residue levels in the foods that are consumed. This study was conducted to identify cumulative dietary risk due to multiple OP pesticides that can be exposed through various foods. Total 22 food samples including cereals, vegetables and fruits were collected randomly two times from food markets in several sites (4 cities). The subjected foods were selected by regarding of highly consumed foods to general Korean people. The 12 OP pesticides including Acephate, Azinphos-methyl, Chlorpyrifos, and Diazinon were monitored. For the exposure assessment, general adult group of 60 kg body weight was regarded as target population and food consumption data suggested by Lee et al. (2000) were used as consumed value of individual food. Analyses of samples for OP pesticides have been carried out according to the multiclass multiresidue analysis method and acephate and methamidophos analysis method of Korea Food Code. In general the levels of OP pesticides found in the food samples were very low or not detected.

• Natural Product Sciences
• /
• v.24 no.2
• /
• pp.88-92
• /
• 2018

The present study was undertaken to investigate the isolated compounds from the stem bark of Garcinia atroviridis as potential cholinesterase inhibitors and the ligand-enzyme interactions of selected bioactive compounds in silico. The in vitro cholinesterase results showed that quercetin (3) was the most active AChE inhibitor ($12.65{\pm}1.57{\mu}g/ml$) while garcinexanthone G (6) was the most active BChE inhibitor ($18.86{\pm}2.41{\mu}g/ml$). It is noteworthy to note that compound 6 was a selective inhibitor with the selectivity index of 11.82. Molecular insight from docking interaction further substantiate that orientation of compound 6 in the catalytic site which enhanced its binding affinity as compared to other xanthones. The nature of protein-ligand interactions of compound 6 is mainly hydrogen bonding, and the hydroxyl group of compound 6 at C-10 is vital in BChE inhibition activity. Therefore, compound 6 is a notable lead for further drug design and development of BChE selective inhibitor.

• Molecules and Cells
• /
• v.27 no.5
• /
• pp.591-599
• /
• 2009

Nicotinic acetylcholine receptors (nAChRs) play important roles in nervous system functions and are involved in a variety of diseases. We previously demonstrated that ginsenosides, the active ingredients of Panax ginseng, inhibit subsets of nAChR channel currents, but not ${\alpha}7$, expressed in Xenopus laevis oocytes. Mutation of the highly conserved Leu247 to Thr247 in the transmembrane domain 2 (TM2) channel pore region of ${\alpha}7$ nAChR induces alterations in channel gating properties and converts ${\alpha}7$ nAChR antagonists into agonists. In the present study, we assessed how point mutations in the Leu247 residue leading to various amino acids affect 20(S)-ginsenoside $Rg_3$ ($Rg_3$) activity against the ${\alpha}7$ nAChR. Mutation of L247 to L247A, L247D, L247E, L247I, L247S, and L247T, but not L247K, rendered mutant receptors sensitive to $Rg_3$. We further characterized $Rg_3$ regulation of L247T receptors. We found that $Rg_3$ inhibition of mutant ${\alpha}7$ nAChR channel currents was reversible and concentration-dependent. $Rg_3$ inhibition was strongly voltage-dependent and noncompetitive manner. These results indicate that the interaction between $Rg_3$ and mutant receptors might differ from its interaction with the wild-type receptor. To identify differences in $Rg_3$ interactions between wild-type and L247T receptors, we utilized docked modeling. This modeling revealed that $Rg_3$ forms hydrogen bonds with amino acids, such as Ser240 of subunit I and Thr244 of subunit II and V at the channel pore, whereas $Rg_3$ localizes at the interface of the two wild-type receptor subunits. These results indicate that mutation of Leu247 to Thr247 induces conformational changes in the wild-type receptor and provides a binding pocket for $Rg_3$ at the channel pore.

• Food Science and Biotechnology
• /
• v.17 no.3
• /
• pp.594-597
• /
• 2008

Natural products have been used to treat many neurological illnesses such as Alzheimer's disease. In the present study, the effects of the water extract of smoke-dried skipjack tuna (WSST), which is used as a traditional seasoning in Japan, as well as its fractions on acetylcholinesterase (AChE) inhibition in vitro and on memory in scopolamine-induced amnesia mice in vivo were evaluated. Bio-Rad P-2 gel permeation chromatography revealed the presence of 7 peaks and AChE significantly inhibited peak 3 and 5. When in vivo behavioral studies were conducted, a passive avoidance test revealed that treatment with 50 and 100 mg/kg WSST as well as with fraction 3 and 5 improved the loss in memory retention induced by scopolamine. These results suggest that skipjack tuna extract and its fractions improve memory deficits and that these substances are suitable for use in healthy foods designed to improve memory deficits induced by aging and Alzheimer's disease.

• The Korean Journal of Physiology and Pharmacology
• /
• v.9 no.1
• /
• pp.29-35
• /
• 2005

To prove the buffering contribution of mitochondria to the increase of intracellular $Ca^{2+}$ level ($[Ca^{2+}]_i$) via background nonselective cation channel (background NSCC), we examined whether inhibition of mitochondria by protonophore carbonylcyanide m-chlorophenylhydrazone (CCCP) affects endothelial $Ca^{2+}$ entry and $Ca^{2+}$ buffering in freshly isolated rabbit aortic endothelial cells (RAECs). The ratio of fluorescence by fura-2 AM ($R_{340/380}$) was measured in RAECs. Biological state was checked by application of acetylcholine (ACh) and ACh ($10{\mu}M$) increased $R_{340/380}$ by $1.1{\pm}0.15$ ($mean{\pm}S.E.$, n=6). When the external $Na^+$ was totally replaced by $NMDG^+$, $R_{340/380}$ was increased by $1.19{\pm}0.17$ in a reversible manner (n=27). $NMDG^+$-induced $[Ca^{2+}]_i$ increase was followed by oscillatory decay after $[Ca^{2+}]_i$ reached the peak level. The increase of $[Ca^{2+}]_i$ by $NMDG^+$ was completely suppressed by replacement with $Cs^+$. When $1{\mu}M$ CCCP was applied to bath solution, the ratio of $[Ca^{2+}]_i$ was increased by $0.4{\pm}0.06$ (n=31). When $1{\mu}M$ CCCP was used for pretreatment before application of $NMDG^+$, oscillatory decay of $[Ca^{2+}]_i$ by $NMDG^+$ was significantly inhibited compared to the control (p＜0.05). In addition, $NMDG^+-induced$ increase of $[Ca^{2+}]_i$ was highly enhanced by pretreatment with $2{\mu}M$ CCCP by $320{\pm}93.7$%, compared to the control ($mean{\pm}S.E.$, n=12). From these results, it is concluded that mitochondria might have buffering contribution to the $[Ca^{2+}]_i$ increase through regulation of the background NSCC in RAECs.

• The Korean Journal of Pesticide Science
• /
• v.16 no.1
• /
• pp.69-77
• /
• 2012

To evaluate the effect of endocrine disruption chemicals (EDCs) to aquatic organisms, muddy loach (Misgurnus anguillicaudatus) was exposed to low concentration methomyl for 21 days in order to identify the effect of biomarkers and endocrine. Vitellogenin (VTG) in blood plasma, which used widely as validated biomarker for endocrine disruption, was significantly greater in male fish exposed to 0.4 mg/L and 2 mg/L methomyl, and in female fish exposed to 0.08 mg/L, 0.4 mg/L, and 2 mg/L methomyl for 21 days (p<0.05). This results suggest that methomyl have probability of endocrine disruption to organism on aquatic system. While inhibition of Acetylcholinesterase (AChE) activity and increase of DNA damage in comet assay were verified by fish exposed to methomyl, change of ethoxyresorufin-O-deethylase (EROD) activity was not occurred, comparing the control group (p<0.05). Indicators at the level of organism such as condition factor (CF), hepato-somatic index (HSI), and gonado-somatic index (GSI) were not influenced by exposure of methomyl. In conclusion, these results showed the possibility of methomyl in regard to not only endocrine disruption but also impacts on biochemical biomarkers to aquatic organisms.

• Journal of Acupuncture Research
• /
• v.23 no.3
• /
• pp.117-127
• /
• 2006

Alzheimer's disease (AD) is the most prevalent form of neurodegenerative disease associated with aging in the human population. This disease is characterized by the following 4 structural changes : Atrophy of the Cortex, Parasympathetic, and other neural cells, the existence of Neurofibrillary tangles (NFTs), and the accumulation of Senile plaques. NFTs and Senile plaques is known to be the index of this disease. Senile plaques disturbs the neutro transmission and depletes of Acetylcholine. So, Recovery of Acetylcholine is the primal objective for treating Alzheimer's disease. So, Inhibiting the activity of Acetylcholine Esterase (AChE), which causes the hydrolysus of acetylcholine into choline and acetate, can be seen as a key role for treating Alzheimer's disease. Increasing body of evidence has been demonstrated that Bee Venom Acupuncture (BV) could compete with complex protein involving in multiple step of $NF-_{\kappa}B$ activation and exert the anti-inflammatory potential of combined inhibition of the prostanoid and nitric oxide synthesis systems by inhibition of IKK and $NF-_{\kappa}B$. BV dose-dependently attenuated Scopolamine-induced Acetylcholine esterase activities in cerebral cortex and hippocampus of the mice brain. This study therefore suggests that BV acupuncture method may be useful for prevention of development or progression of AD.

• Food Science and Biotechnology
• /
• v.17 no.1
• /
• pp.95-101
• /
• 2008

Some biological activities of Beauveria bassiana were studied to elucidate pharmacological function of B. bassiana-infected larva of the silkworm. The mycelium consisted mainly of carbohydrate (65.8%), followed by protein (15.9%) and fat (8.3%). Glucose (68.8%), mannose (7.1%), and galactose (6.1%) were major components in carbohydrates. Ten amino acids including glutamine, threonine, valine, aspartic acid, alanine, leucine, serine, glycine, arginine, and isoleucine were found in protein as major amino acids. Various extracts were prepared from the freeze-dried mycelium of B. bassiana by systemic extraction and their biological activities were investigated. Among tested fractions, the hot-water extract (HW) contributed significantly to the anti-coagulant activity, anti-complementary activity, and stimulation of intestinal immune system. The methanol extract (ME) increased acetylcholinesterase (AChE) inhibition activity and reactive oxygen species (ROS) scavenging activity.