• YAKHAK HOEJI
• /
• v.45 no.6
• /
• pp.694-700
• /
• 2001

Synthetic pyrethroids are analysis of a natural chemical moiety, pyrethrin derived from the pyrethrum plant Chrysanthemum. The natural pyrethrin structure has been modified to be highly lipophilic and photostable, creating an effective pesticide and resulting in an increased presence in the environment. Worldwide, they are commonly used insecticides against ticks, mites, mosquitoes, and as treatment for human head lice and scabies. Therefore, human exposure to their compounds in extensive. Several studies on the effects of pyrethroids on thyroid hormone regulation, estrogen and androgen function have been reported and yet little has been done try assess their potential hormonal activities. Among humans, a pyrethroid compound was suggested to be the causal agent for gynecomastia in a group of Haitian men. The reports suggest that some pyrethroid compounds are capable of disrupting endocrine function. Therefore, we examined estrogenic/antiestrogenic potential of three pyrethroid insecticides, that is permethrin, allethrin and fenvalerate in human breast cancer cell and action mechanism mediated by the estrogen receptor. Fenvalerate showed weak estrogenic activity but aallethrin and permethrin showed no effect. In combination with high levels (10$^{-10}$ M, 10$^{-11}$ M) of 17$\beta$-estradiol and three synthetic pyrethroids inhibited cert proliferations in MCF7-BUS cell by 17$\beta$-estradiol. Whereas, fenvalerate increased cell proliferative activity at lower level of estradiol (10$^{-12}$ M, 10$^{-13}$ M). The relative affinities to the estrogen receptor were observed by allethrin and permethrin treatment, but not by fenvalerate. These results indicated that some of pyrethroid insecticides may modulate estrogen functions in human breast cancer cell. The action mechanisms of estrogen receptor mediated antiestrogenicity by allethrin and permethrin were postulated.

• Clinical Pain
• /
• v.18 no.2
• /
• pp.70-75
• /
• 2019

Objective: The purpose of this study is to evaluate the usefulness of infrared thermography in patients with carpal tunnel syndrome by comparing with electrodiagnostic and ultrasonographic findings. Method: From January 2014 to October 2017, electrodiagnosis, ultrasound, and digital infrared thermal image (DITI) of unilateral carpal tunnel syndrome diagnosed in a single hospital were retrospectively analyzed. The subjects with bilateral symptoms of carpal tunnel syndrome, peripheral vascular disease, diabetes, thyroid disease, fibromyalgia, rheumatic disease, systemic infection, inflammation, malignant tumor, and other musculoskeletal disorders such as finger osteoarthritis, peripheral neuropathy, cervical radiculopathy, and the previous history of surgery were excluded. Results: Of 53 patients diagnosed with carpal tunnel syndrome, 11 were male and 42 were female. The visual analogue scale was 4.9 ± 1.9, and the duration of symptom was 11.8 ± 12.5 months. There was no statistically significant difference in the body surface temperature between the unaffected and affected sides. The severity of symptoms, electrodiagnostic findings, and cross-sectional area of the median nerve significantly correlates to each other. The temperature difference between the second fingers of the affected and unaffected sides showed a weak correlation with the amplitude of sensory nerve action potential and onset latency of compound muscle action potential, when there was no significant correlation with the other parameters. Conclusion: The difference in temperature on the surface of the body, which can be confirmed by DITI, is little diagnostic value when DITI is performed in unilateral carpal tunnel syndrome patients, especially when compared with ultrasonography.

• Archives of Pharmacal Research
• /
• v.17 no.5
• /
• pp.331-336
• /
• 1994

The ether extract from the roots of angelica clahurica was found to inhibit bovine lens aldose reductase (BLAR0 activity in vitro by 100% at 100.mu.g/ml. Systematic fractionation of the ether soluble fraction and subsequent active frctions monitorede by bioassy led to isolation of four furanocoumarins, isoimperatorin (I0, imperatorin (II), ter-O-methyl byakangelicin (III) and byakangelicin (IV), among which compound III and IV were identified as potential AR inhibitors, their $IC_{50}$ values being $2.8{\mu}M{\;}and{\;}6.2{\mu}M$, respectively. Galactosemic cataract formation tors, in rats treated with 40 g/kg/day of galactose was blocked almost completely throughout the exeprimental periods up to 44 days by i.p. administrations of byakangelicin (IV) at 50 mg/kg/day. In coincidence with the inhibitory action on cataract formation, the galactitol accumulation in rats treated with byakangelicin (IV) was found to be markedly prevented by approximately 80.5% compared to those of the contro. These results indicate that byakangelicin (IV), as a main principle of this plant, possesses high potential for a clinically useful drug of the future which prevents and/or improves sugar cataract as well as diabetic complications.

• Animal cells and systems
• /
• v.13 no.4
• /
• pp.357-362
• /
• 2009

Hesperidin, the most abundant polyphenolic compound found in citrus fruits, has been known to possess neuroprotective, sedative, and anticonvulsive effects on the nervous system. In a recent electrophysiological study, it was reported that hesperidin induced biphasic change in population spike amplitude in hippocampal CA1 neurons in response to both single spike stimuli and theta-burst stimulation depending on its concentration. However, the precise mechanism by which hesperidin acts on neuronal functions has not been fully elucidated. Here, using whole-cell patch-clamp recording, we revealed that hesperidin did not affect excitatory synaptic activities such as basal synaptic transmission and theta-burst LTP. Moreover, in a current injection experiment, spike number, resting membrane potential and action potential threshold also remained unchanged. Taken together, these results indicate that the effects of hesperidin on the neuronal functions such as spiking activity might not be attributable to either modification of excitatory synaptic transmissions or changes in membrane excitability in hippocampal CA1 neuron.

• Natural Product Sciences
• /
• v.26 no.4
• /
• pp.295-302
• /
• 2020

Cudrania tricuspidata (C. tricuspidata) is a deciduous tree found in Japan, China and Korea. The root, stems, bark and fruit of C. tricuspidata has been used as traditional herbal remedies such as eczema, mumps, acute arthritis and tuberculosis. In this study, we investigated the potential efficacies of this natural compound by focusing on the inhibitory effect of cudraxanthone L (CXL) isolated from the roots of C. tricuspidata on human platelet aggregation. Our study focused on the action of CXL on collagen-stimulated human platelet aggregation, inhibition of platelet signaling molecules such as fibrinogen binding, intracellular calcium mobilization, fibronectin adhesion, dense granule secretion, and thromboxane A2 secretion. In addition, we investigated the inhibitory effect of CXL on thrombin-induced clot retraction. Our results showed that CXL inhibited collagen-induced human platelet aggregation, intracellular calcium mobilization, fibrinogen binding, fibronectin adhesion and clot retraction without cytotoxicity. Therefore, we confirmed that CXL has inhibitory effects on human platelet activities and has potential value as a natural substance for preventing thrombosis.

• Journal of Applied Biological Chemistry
• /
• v.63 no.4
• /
• pp.365-373
• /
• 2020

We previously reported the potential of Senna tora L. seeds fermented by Lactobacillus casei (FSL) as a laxative agent in a loperamide-induced constipation rat model. Here, we examine the mechanism of action of FSL and its bioactive compound, revealed herein, on loperamide-induced constipation Sprague Dawley rat model. We identified the compound aurantio-obtusin (AO) using HPLC quantitative analysis. Rats were randomly assigned to six experimental groups (eight rats each)-normal and constipated groups (loperamide, FSL [100, 300, 500 mg/kg], and AO [1 mg/kg]). The FSL and AO-treated group showed an increase in the frequency, amount, and water content of feces in the constipated rat. Moreover, FSL and AO increased the intestinal transit speed in the constipated rat. Histological analysis revealed that FSL and AO recovered the intestinal mucus, the number of goblet cells, as well as thickness of the mucosa layer and muscle. Furthermore, the protein levels of the muscarinic acetylcholine receptor M3, which is involved in intestine contraction, were recovered in the FSL and AO-treated group. Its downstream signaling pathway (p-protein kinase C) was recovered by FSL and AO treatment. In conclusion, fermentation of S. tora L. seeds increases AO, which improves intestinal function, indicating that FSL is effective for treating constipation.

• Annals of Clinical Neurophysiology
• /
• v.13 no.1
• /
• pp.31-37
• /
• 2011

Background: Carpal tunnel syndrome (CTS) and tarsal tunnel syndrome (TTS) are thought to share a similar pathophysiology, compression of the median and plantar nerve by the carpal tunnel and flexor retinaculum. A few reports introduced the relationship between idiopathic CTS and TTS without definite evidence of coexistence. The current study was designed to analyze the electrophysiologic characteristics of combined idiopathic CTS and TTS by comparing with each idiopathic CTS or TTS. Methods: We retrospectively collected patients with combined idiopathic CTS and TTS (CTS-TTS group) from June 2001 to February 2009. Patients with each idiopathic CTS or TTS were collected as controls. Electrophysiologic data of median and plantar nerves were compared between CTS-TTS group and controls. Results: CTS-TTS group was composed of 31 patients. Control group of each CTS or TTS were 50 CTS and 49 TTS patients. In comparison of median nerve conduction study between CTS-TTS group and CTS control group, decreased compound muscle action potential amplitude (p<0.001), decreased median sensory nerve action potential amplitude (p<0.001) and sensory nerve conduction velocity at finger stimulation (p=0.013) were prominent in CTS-TTS group. Decreased medial plantar sensory nerve action potential amplitude (p=0.034) was indicated when CTS-TTS groups and TTS control group were compared. Conclusions: If the electrophysiology study of patients with CTS or TTS was suggestive of severe degree of nerve injury, concerns about the possibility of combined CTS and TTS would be helpful.

• The Korean Journal of Physiology
• /
• v.15 no.2
• /
• pp.73-81
• /
• 1981

Experiments were conducted in ischemic decerebrate cats to study the effects of electroacupuncture and electrical stimulation of peripheral nerve on pain reaction. Flexion reflex was used as an index of pain. The reflex was elicited by stimulating the sural nerve(20 V, 0.5 msec duration) and recorded as a compound action potential from the nerve innervated to the semitendinosus muscle. Electroacupuncture was performed, using a 23-gauge hyperdermic needle, on the tsusanli point in the lateral upper tibia of the ipsilateral hindlimb. The common peroneal nerve was selected as a peripheral nerve which may be associated with electroacupuncture action, as it runs through the tissue portion under the tsusanli point. Both for electroacupuncture and the stimulation of common peroneal nerve a stimulus of 20 V-intensity, 2 msec-duration and 2 Hz-frequency was applied for 60 min. The results are summerized as follows: 1) The electroacupuncture markedly depressed the flexion reflex; this effect was eliminated by systemic application of naloxone $(0.02{\sim}0.12\;mg/kg)$, a specific narcotic antagonist. 2) Similarly, the electrical stimulation of the common peroneal nerve significantly depressed the flexion reflex, the effect being reversed by naloxone. 3) When most of the afferent nerves excluding sural nerve in the ipsilateral hindlimb were cut, the effect of electroacupuncture on the flexion reflex was not observed. Whereas direct stimulation of the common peroneal nerve at the proximal end from the cut resulted in a significant reduction of the flexion reflex, again the effect was reversible by naloxone application. 4) Transection of the spinal cord at the thoracic 12 did not eliminate the effect of peripheral nerve stimulation on the flexion reflex and its reversal by naloxone, although the effect was significantly less than that in the animal with spinal cord intact. These results suggest that: 1) the analgesic effect of an electroacupuncture is directly mediated by the nervous system and involves morphine-like substances in CNS, 2) the site of analgesic action of electroacupuncture resides mainly in the brainstem and in part in the spinal cord.

• The Korean Journal of Pain
• /
• v.12 no.2
• /
• pp.177-182
• /
• 1999

Background: Clonidine, an ${\alpha}_2$ adrenergic agonist blocks nerve conduction. However, in our previous experiment we found that adrenaline neither blocks nerve conduction by itself nor augment nerve conduction blockade by lidocaine near clinical concentrations. Possible explanations are: 1) there may be antagonism between some of adrenergic receptors, 2) clonidine may block nerve conduction via non-adrenergic mechanism. The purpose of this study is to obtain dose-response curves of several different forms of adrenergic receptor agonist to see the relative potencies of each adrenergic receptors to block nerve conduction. Methods: Recordings of compound action potentials of A-fiber components (A-CAPs) were obtained from isolated sciatic nerves of adult male Sprague-Dawley rats. Nerve sheath of the sciatic nerve was removed and desheathed nerve bundle was mounted on a recording chamber. Single pulse stimuli (0.5 msec, supramaximal stimuli) were repeatedly applied (2Hz) to one end of the nerve and recordings of A-CAPs were made on the other end of the nerve. Dose-response curves of epinephrine, phenylephrine, isoproterenol, clonidine were obtained. Results: $ED_{50}$ of each adrenergic agonist was: $4.51\times10^{-2}$ M for epinephrine; phenylephrine, $7.74\times10^{-2}$ M; isoproterenol, $9.61\times10^{-2}$ M; clonidine, $1.57\times10^{-3}$ M. Conclusion: This study showed that only clonidine, ${\alpha}_2$ adrenergic agonist, showed some nerve blocking action while other adrenergic agonists showed similar poor degree of nerve blockade. This data suggest that non-effectiveness of epinephrine in blocking nerve conduction is not from the antagonism between adrenergic receptors.

• Archives of Pharmacal Research
• /
• v.29 no.10
• /
• pp.859-865
• /
• 2006

With an approach to study the anti-tumor effects and mechanism of selenium compound, we investigated the anti-tumor activity and mechanism of $Na_5SeV_5O_{18}{\cdot}3H_2O$ (NaSeVO) in K562 cells. The results showed that $0.625{\sim}20\;mg/L$ NaSeVO could significantly inhibit the proliferation of K562 cells in vitro in a time- and concentration-dependent manner as determined by microculture tetrazolium (MTT) assay, the IC50 values were 14.41 (4.45-46.60) and 3.45 (2.29-5.22) mg/L after 48 hand 72 h treatment with NaSeVO respectively. In vivo experiments demonstrated that i.p. administration of 5, 10 mg/kg NaSeVO exhibited an significant inhibitory effect on the growth of transplantation tumor sarcoma 180 (S180) and hepatoma 22 (H22) in mice, with inhibition rate 26.8% and 58.4% on S180 and 31.3% and 47.4% on H22, respectively. Cell cycle studies indicated that the proportion of G0/G1 phase was increased at 2.5 mg/L while decreased at 10 mg/L after treatment for 24, 48 h. Whereas S phase was decreased at 2.5-5 mg/L and markedly increased at 10 mg/L after treatment for 48 h. After treatment for 24 h, 10 mg/L NaSeVO also markedly increased S and G2/M phases. Take together, the result clearly showed that NaSeVO markedly increased S and G2/M phases at 10 mg/L. The study of immunocytochemistry showed that the expression bcl-2 is significantly inhibited by 10 mg/L NaSeVO, and bax increased. Morphology observation also revealed typical apoptotic features. NaSeVO also significantly caused the accumulation of $Ca^{2+}$ and $Mg^{2+}$, reactive oxygen species (ROS) and the reduction of pH value and mitochondrial membrane potential in K562 cells as compared with control by confocal laser scanning microscope. These results suggest that NaSeVO has anti-tumor effects and its mechanism is attributed partially to apoptosis induced by the elevation of intracellular $Ca^{2+}$, $Mg^{2+}$ and ROS concentration, and a reduction of pH value and mitochondria membrane potential (MMP).