• Proceedings of the Korean Society of Applied Pharmacology
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• 1993.11a
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• pp.1-6
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• 1993

Capsaicin [N-(4-hydroxy-3-methoxybenzyl)-trans-8-methyl -6-nonenamide], a pungent principle of red pepper. is known to induce analgesia. Though it has shown remarkable pharmacological activity, the toxicity and side effects inhibited its wider application. The interest has been renewed by the emergence of its agonists, resineferatoxin and ruthenium red. Recently, few successful capsaicinoids including 01vanil (NE-19550), NE-28345, and NE-21610 were reported.

• Proceedings of the PSK Conference
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• 2001.04a
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• pp.159.1-159.1
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• 2001

• Archives of Pharmacal Research
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• v.15 no.1
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• pp.104-108
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• 1992

2, 3-Diphenyl-6-formyl-5-methoxyindole reacts with ethyl cyano acetate to yield the arylidene derivative which forms with urea and thiourea the corresponding pyrimidine derivatives. The arylidene derivatives react with hydrazines and with active methylenes to form the respective pyrazole derivatives and the $\alpha, \;\beta$-disubstituted acrylonitriles. Seven new compounds were tested for their effects on the arterial blood pressure of rats and analgesic activity.

• Preventive Nutrition and Food Science
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• v.22 no.3
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• pp.157-165
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• 2017

Fruits of Sonneratia apetala (Buch.-Ham.), (English: mangrove apple, Bengali: keora) both seeds and pericarps, are largely consumed as food besides their enormous medicinal application. The fruit seeds have high content of nutrients and bioactive components. The seeds powder of S. apetala was successively fractionated using n-hexane, diethyl ether, chloroform, ethyl acetate, and methanol. The fractions were used to evaluate antibacterial, anti-diarrhoeal, analgesic, and cytotoxic activities. Methanol fraction of seeds (MeS) stronly inhibited Escherichia coli strains, Salmonella Paratyphi A, Salmonella Typhi, Shigella dysenteriae, and Staphylococcus aureus except Vibrio cholerae at $500{\mu}g/disc$. All the fractions strongly inhibited castor oil induced diarrhoeal episodes and onset time in mice at 500 mg extract/kg body weight (P<0.001). At the same concentration, MeS had the strongest inhibitory activity on diarrhoeal episodes, whereas the n-hexane fraction (HS) significantly (P<0.05) prolonged diarrhoeal onset time as compared to positive control. Similarly, HS (P<0.005) inhibited acetic acid induced writhing in mice at 500 mg extract/kg, more than any other fraction. HS and diethyl ether fractions of seed strongly increased reaction time of mice in hot plate test at 500 mg extract/kg. All the fractions showed strong cytotoxic effects in brine shrimp lethality tests. Gas chromatography-mass spectrometry analysis of HS led to the identification of 23 compounds. Linoleic acid (29.9%), palmitic acid (23.2%), ascorbyl palmitate (21.2%), and stearic acid (10.5%) were the major compounds in HS. These results suggest that seeds of S. apetala could be of great use as nutraceuticals.

• Proceedings of the Korean Society of Applied Pharmacology
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• 1998.11a
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• pp.178-178
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• 1998

We reported that the hexane fraction of Torilis Fructus have an anti-inflammatory and analgesic effect. Therefore, in order to isolate the active compound, the hexan fraction of Torilis Fructus was chromatographed on silica gel column. The subfraction of hexane fraction was crystallized as colorless stout needles. The chemical structure of this compound was verified to be torilin through m.p., UV, IR, GC-MS, and NMR spectral data. In pharmacological tests, torilin exhibited strong anticarrageenan activity at the dose of 90 and 270 mg/kg, p.o. in rats, and it had inhibitory effect on the vascular permeability at the dose of 30 and 90 mg/kg, p.o. in mice. Torilin showed potent inhibition of leucocyte emigration in CMC-pouch at the dose of 3 and 9 mg/rat, s.c. Torilin have the analgesic effect at the dose of 30, 90 and 270 mg/kg, p.o. in both of the acetic acid- and phenyl-p-benzoquinone-induced writhing syndrome. It also increased the pain threshold at the dose of 30, 90 and 270 mg/kg, p.o. in the tail pressure method and the Randall-Selitto method. Torilin did not show a hypothermic action at the dose of 30 and 90 mg/kg, p.o. in mice. The acute toxicity of torilin was very weak: the LD$\_$50/ value was more than 5000 mg/kg, p.o. and 2000 mg/kg, Lp. in mice. From the above mentioned results, it was suggested that torilin had potent anti-inflammatory and analgesic activities in animals.

• The Korean Journal of Pain
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• v.24 no.4
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• pp.179-184
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• 2011

Background: The analgesic mechanisms of cyclooxygenase (COX)-2 inhibitors have been explained mainly on the basis of the inhibition of prostaglandin biosynthesis. However, several lines of evidence suggest that their analgesic effects are mediated through serotonergic or adrenergic transmissions. We investigated the roles of these neurotransmitters in the antinociception of a selective COX-2 inhibitor at the spinal level. Methods: DUP-697, a selective COX-2 inhibitor, was delivered through an intrathecal catheter to male Sprague-Dawley rats to examine its effect on the flinching responses evoked by formalin injection into the hindpaw. Subsequently, the effects of intrathecal pretreatment with dihydroergocristine, prazosin, and yohimbine, which are serotonergic, ${\alpha}1$ adrenergic and ${\alpha}2$ adrenergic receptor antagonists, respectively, on the analgesia induced by DUP-697 were assessed. Results: Intrathecal DUP-697 reduced the flinching response evoked by formalin injection during phase 1 and 2. But, intrathecal dihydroergocristine, prazosin, and yohimbine had little effect on the antinociception of intrathecal DUP-697 during both phases of the formalin test. Conclusions: Intrathecal DUP-697, a selective COX-2 inhibitor, effectively relieved inflammatory pain in rats. Either the serotonergic or adrenergic transmissions might not be involved in the analgesic activity of COX-2 inhibitors at the spinal level.

• CELLMED
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• v.8 no.3
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• pp.14.1-14.6
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• 2018

Santalum album Linn. [Family: Santalaceae] is commonly known as white sandalwood, sandal safaid and safed chandan. It is one of the most valuable trees and second costliest wood in the world. Sandalwood and its oil is extensively used in the Unani and other traditional systems of medicine as it has blood purifier, anti-inflammatory, analgesic, exhilarant, cardiotonic, antiseptic, nervine tonic and expectorant properties. It is used in skin, cardiac, liver, gastrointestinal, respiratory, integument and urogenital disorders. These uses are supported and proven by many in vitro or in vivo studies. The proven pharmacological activities of S. album are antimicrobial, anti-oxidant, anti-inflammatory, antimutagenic and anti-fatigue. The research has proven that sandal oil or its constituents have anti-microbial activity. Sandalwood oil showed skin cancer preventive effect in mice and its constituent alpha santalol showed the anticancer property. The methanolic extract of wood was confirmed for antioxidant, free radical scavenging, analgesic and anti-inflammatory activities. ${\alpha}$ and ${\beta}$ santalols present in sandal oil showed sedative effects. Sandalwood tea had a significant effect on heart muscles of frog and showed increased myocardial contractility. Its oil showed significant changes in hepatic xenobiotic metabolizing enzymes. Sandalwood oil and its major constituents showed less acute oral and dermal toxicity in laboratory animals. Hence, the aforementioned studies justify the uses of sandalwood and its oil mentioned in the classical Unani literature. However, further clinical trials are suggested to confirm its efficacy and safety in humans.

• Korean Journal of Pharmacognosy
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• v.32 no.4 s.127
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• pp.330-337
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• 2001

Prickly pear(Opuntia ficus-indica var. saboten Makino, Cactaceae) is a tropical or subtropical plant, which is widely used as folk medicine for burned wound, edema and indigestion. Screening on the biological properties of the fruits(OFS-Fr) and stems(OFS-St) of the plant was carried out to prove the pharmacological significance. By hot plate and acetic acid-inducing writhing methods, significant analgesic effects of OFS-Fr and OFS-St were found in mice and anti-edemic effect was observed in carrageenin-induced inflammatory rats. However, the extracts showed no significant actions on central and autonomic nervous system and blood circulatory system, which imply no toxic effects to animal.

• The Korean Journal of Pain
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• v.18 no.2
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• pp.181-186
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• 2005

Background: Hydromorphone has an intermediate lipid solubility range that falls between morphine and fentanyl. Lipophilic activity during opioid epidural administration is important in relation to both the side effects and analgesic efficacy. The purpose of this study was to compare epidural hydromorphone and fentanyl when concomitantly infused with bupivacaine in patients undergoing a thoracotomy. Methods: Seventy-seven thoracotomy patients, with patient-controlled epidural analgesia (PCEA), were blindly allocated into two groups [group F (n = 34); 0.1% bupivacaine and fentanyl $5{\mu}g/ml$, group H (n = 34); 0.1% bupivacaine and hydromorphone $16{\mu}g/ml$)]. The basal PCEA rate and demand dose were 4 ml/hr and 3 ml, respectively. The visual analogue scale (VAS) for pain, and pruritus, sedation and nausea were measured at 6, 12 and 24 hours after the operation. Results: There were no significant differences in the VAS pain scores and the incidences of pruritus, nausea and sedation between the two groups. The total infused volume after 24 hours was lower in H compared to that of F group (P < 0.05). Conclusions: We conclude that epidural hydromorphone or fentanyl administration has a similar analgesic efficacy and shows similar incidences of side effects, when concomitantly infused with bupivacaine, in the management of acute pain following a thoracotomy.

• Natural Product Sciences
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• v.19 no.4
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• pp.311-315
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• 2013

Ribes fasciculatum (Saxifragaceae) has been widely used as a traditional medicine for the treatment of cough, antidote, cold, lacquer poison, and sore throat. In the present study, we evaluated the anti-nociceptive effects of ethyl acetate fraction of Ribes fasciculatum (ERF) in mice. Test results of tail-immersion test and hot plate test revealed that the ERF had strong anti-nociceptive activities on thermal nociception in a dose dependent manner, indicating ERF's anti-nociception on the central pain. Moreover, the acetic acid-induced chemical nociception was also significantly reduced by ERF treatment. This result shows that ERF may also work on the peripheral pain. We further performed formalin test to confirm ERF's anti-nociceptive properties and found that pain responses were significantly decreased by ERF treatment. Interestingly, in the combination test with naloxone, the analgesic activity of ERF was not changed, indicating that the opioid receptor was not involved in the ERF-mediated anti-nociception. These results indicate that ERF might be possibly used as a painkiller for the treatment of nociceptive pains.