• YAKHAK HOEJI
• /
• v.45 no.6
• /
• pp.565-569
• /
• 2001

Five novel cinmetacin amide derivatives as potential nonsteroidal antiinflammatory and analgesic compounds were prepared and their antiinflammatory-analgesic activity was compared with cinmetacin. Cinmetacin and hydroxysuccinimide were reacted with dicyclohexyl carbodiimide to give cinmetacin active ester (4), which was treated with amines to yield cinmetacin amides (5-9). Compounds (5) and (9) gave stronger analgesic activity than cinmetacin and compounds (5), (6), (9) showed comparable antiinflammatory activity to cinmetacin.

• YAKHAK HOEJI
• /
• v.45 no.1
• /
• pp.1-6
• /
• 2001

Nine cinmetacin derivatives as potential nonsteroidal analgesic and antiinflammatory compounds were prepared and their analgesic-antiinflammatory activity was compared with cinmetacin. Salicylic acid and phenols were reacted with dicyclohexyl carbodiimide (DCC) to give phenol salicylates (1-4). Cinmetacin was treated with DCC and phenol derivatives to yield cinmetacin esters (5-13). Compounds (5, 7, 8, 10, 12, and 13) showed stronger analgesic activity than cinmetacin, but only compound (5) showed comparable antiinflammatory activity to cinmetacin.

• Korean Journal of Pharmacognosy
• /
• v.17 no.2
• /
• pp.107-112
• /
• 1986

The investigation aimed to study the effects of methanol fraction of licorice (FM 100) and glycyrrhizin on prostaglandin synthetase activity, in relation to their analgesic effects. Effects of FM 100 and glycyrrhizin on the activity of prostaglandin synthetase extracted from bull seminal vesicles were examined by the modified method of Takeguchi et al. The analgesic effect of FM 100 was tested in mice by the acetic acid writhing method. FM 100 was administered orally to mice. BSV prostaglandin synthetase activity was inhibited significantly by FM 100 in a dose-dependent manner, whereas the activity was slightly inhibited by glycyrrhizin. Statistically significant analgesic effects were also observed with FM 100. The results suggest that analgesic effect of licorice may be due to the inhibition of prostaglandin synthesis.

• Biomolecules & Therapeutics
• /
• v.5 no.1
• /
• pp.67-73
• /
• 1997

Analgesic effect of DA-5018, a new capsaicin derivative, was evaluated in various rat models of experimentally induced acute pain. DA-5018(0.2∼10.0 mg/kg, p.o.) prevented the writhing syndromes induced by acetic acid or phenol-p-benzoquinone(PBQ). It increased the pain threshold of inflamed paw when tested by the Randall-Selitto method at the dose of 2.0∼20.0 mg/kg by oral administration. And also it showed antinociceptive activities in tail-pinch(1.0∼20.0 mg/kg, p.o.) and tail-flick test(5.0∼50.0 mg/kg, p.o.). the potency and efficacy of DA-5018 were comparable to morphine · HCI in all the models mentioned above. Acetaminophen exhibited the inhibition of acetic acid-induced writhing syndromes and also analgesic activity in Randall-Selitto test, but it showed the limited efficacy in tail-pinch and tail-flick test. These results mean that DA-5018 has a broader analgesic activity profile than acetaminophen. And we found out that the analgesic activity of DA-5018 was 100 times more potent when administered centrally than administered orally in tail-flick test. These results suggest that DA-5018 has an orally active analgesic activity, and central nervous system may be involved in the action of DA-5018.

• Archives of Pharmacal Research
• /
• v.19 no.3
• /
• pp.246-247
• /
• 1996

In the previous reports (Park et al., 1991, and 1993), we described the synthesis and analgesic effects of various homovanillic amides as analogs of capsaicin. In the study, we tried to enhance the analgesic actvity of capsaicin by structural modification. Our study has been performed in three directions. First, the amide bond of capsaicin was transposed. Second, a phenyl ring was introduced to replace a double bond of capsaicin. Finally, aminoethylation was performed on 4-hydroxy group of capsaicin to improve oral bioavailability. These studies have led to N-(3-phenylpropyl)homovanillic amide 2 which has high analgesic activity. Our continuing efforts in this area have focused on the introduction of various substituents on the phenyl ring of 2 as well as their pharmacological studies. We report herein the synthesis of homovanillic amide derivatives and their analgesic activity.

• Korean Journal of Pharmacognosy
• /
• v.38 no.4
• /
• pp.334-338
• /
• 2007

Roots of Rumex crispus (Rc) (Polygonaceae) has been used as therapeutic agents of acute and chronic cutaneous diseases, cathartics, fever and jaundice in folk medicines. Recently, Seeds of Rc has known as a digestive, an anticancer agent and a remedy of acute hepatitis, among many traditional folk medicines. So far it isn't reported about pharmacological effects of Rumecis Semen. The present study describes the preliminary evaluations of biological activities, anti-inflammatory activity (AA, Carrageenan) analgesic activity (writhing test), and hepatoprotective activities ($CCl_4$), of its methanol extract, ethyl acetate fraction and butanol fraction. Among them butanol fraction showed the highest activity in analgesic acivity.

• Advances in Traditional Medicine
• /
• v.5 no.2
• /
• pp.124-136
• /
• 2005

Two popular ethnomedicines of the Onge, a Negrito tribe of Andaman Islands, were evaluated for analgesic and antiinflammatory activity. The methanol extract as well as the different fractions of methanol extract of both Alstonia macrophylla and Mallotus peltatus leaves were studied using Swiss albino mice and Wistar albino rats. Acetic acid induced writhing, Tail flick and Tail immersion; Carrageenin- and Dextran-induced paw oedema tests were used. Dose-dependent analgesic and antiinflammatory activity were demonstrated for both methanol leaf extracts as well as fractions. Results were highly comparable with that of the standard drug pethidine.

• Natural Product Sciences
• /
• v.9 no.3
• /
• pp.154-157
• /
• 2003

In the present study, the roots of Sesbania grandiflora L. Poiret (Papilionaceae) were successively extracted with petroleum ether (PE), chloroform (CE), methanol (ME) and water (AE) by soxhlet extraction. The extracts were vacuum dried and screened for analgesic, antidiarrhoeal, antibacterial (Staphylococcus epidermidis, Staphylococcus aureus, Micrococcus luteus, Bacillus cereus, and Klebsiella pneumonia) and antifungal (Candida albicans and Aspergillus niger) activity. All the extracts exhibited potent, dose dependant (40 and 80 mg/kg) and significant analgesic and antidiarrhoeal activity in the order of AE>PE>CE>ME and ME>PE>AE>CE respectively. AE at the experimental dose was found to exhibit more potent analgesic activity than standard drug. All the extracts exhibited significant antibacterial $(100\;{\mu}g/ml)$ and antifungal activity $(50\;and\;100\;{\mu}g/ml)$. ME exhibited the most potent antibacterial activity.

• Natural Product Sciences
• /
• v.12 no.1
• /
• pp.24-28
• /
• 2006

The analgesic and the antipyretic activity of the methanol, chloroform, hexane and acetonitrile extracts of the aerial parts of Stachys schimperi Vatke were investigated in mice. The nociceptive response was tested using acetic acid-induced writhing and tail flick method; while hypothermia affect was examined via yeast-induced fever test. The chloroform extract at 500 mg and hexane and acetonitrile extracts at 250 mg produced significant analgesic and antipyretic activity.

• Archives of Pharmacal Research
• /
• v.18 no.1
• /
• pp.38-40
• /
• 1995

melandrin exhibited an analgesic activity as assessed by inhibition of writhing syndromein mice and by pressure method of inflamed paws of arts and inflamed tails of mmice, and showed a hypothermic effect. However, no anti-inflammatory activity was shown.