This study investigated the potential antinociceptive efficacy of a novel synthetic curcuminoid analogue, 2,6-bis-(4-hydroxy-3-methoxybenzylidene)cyclohexanone (BHMC), using chemical-and thermal-induced nociception test models in mice. BHMC (0.03, 0.1, 0.3 and 1.0 mg ⁄ kg) administered via intraperitoneal route (i.p.) produced significant dose-related inhibition in the acetic acid-induced abdominal constriction test in mice with an ID 50 of 0.15 (0.13-0.18) mg ⁄ kg. It was also demonstrated that BHMC produced significant inhibition in both neurogenic (first phase) and inflammatory phases (second phase) of the formalin-induced paw licking test with an ID 50 of 0.35 (0.27-0.46) mg ⁄ kg and 0.07 (0.06-0.08) mg ⁄ kg, respectively. Similarly, BHMC also exerted significant increase in the response latency period in the hot-plate test. Moreover, the antinociceptive effect of the BHMC in the formalin-induced paw licking test and the hot-plate test was antagonized by pre-treatment with the non-selective opioid receptor antagonist, naloxone. Together, these results indicate that the compound acts both centrally and peripherally. In addition, administration of BHMC exhibited significant inhibition of the neurogenic nociception induced by intraplantar injections of glutamate and capsaicin with ID 50 of 0.66 (0.41-1.07) mg ⁄ kg and 0.42 (0.38-0.51) mg ⁄ kg, respectively. Finally, it was also shown that BHMC-induced antinociception was devoid of toxic effects and its antinociceptive effect was associated with neither muscle relaxant nor sedative action. In conclusion, BHMC at all doses investigated did not cause any toxic and sedative effects and produced pronounced central and peripheral antinociceptive activities. The central antinociceptive activity of BHMC was possibly mediated through activation of the opioid system as well as inhibition of the glutamatergic system and TRPV1 receptors, while the peripheral antinociceptive activity was perhaps mediated through inhibition of various inflammatory mediators.

The possible mechanisms of action in the antinociceptive activity induced by systemic administration (intraperitoneal, i.p.) of flavokawin B (FKB) were analysed using chemical models of nociception in mice. It was demonstrated that i.p. administration of FKB to the mice at 0.3, 1.0, 3.0 and 10 mg ⁄ kg produced significant dose-related reduction in the number of abdominal constrictions. The antinociception induced by FKB in the acetic acid test was significantly attenuated by i.p. pretreatment of mice with L-arginine, the substrate for nitric oxide synthase or glibenclamide, the ATP-sensitive K + channel inhibitor, but was enhanced by methylene blue, the non-specific guanylyl cyclase inhibitor. FKB also produced dose-dependent inhibition of licking response caused by intraplantar injection of phorbol 12-myristate 13-acetate, a protein kinase C activator (PKC). Together, these data indicate that the NO ⁄ cyclic guanosine monophosphate ⁄ PKC ⁄ ATP-sensitive K + channel pathway possibly participated in the antinociceptive action induced by FKB.Chalcones or 1,3-diaryl-2-propen-1-ones are a well-known class of flavonoids that have been reported to possess both in vitro and in vivo biological activities including antimicrobial, anticancer, antiprotozoal, antiplatelet, antinociceptive and anti-inflammatory [1][2][3][4][5][6]. It has been reported elsewhere that chalcones and their derivatives inhibited the synthesis of nitric oxide (NO), lipoxygenase as well as cyclo-oxygenase activities which constitute the major pro-inflammatory pathways and remain most targeted for anti-inflammatory and antinociceptive drug development [7][8][9][10].In attempts to obtain active derivatives from chalcone that possesses anti-inflammatory and antinociceptive activities, our group previously isolated 6¢-hydroxy-2¢,4¢-dimethoxychalcone or flavokawin B (FKB) from Alpinia nutans Rosc. along with other chalcones such as cardamonin (6), 5,6-dehydrokawain, (-)-pinocembrin, (-)-pinostrobin and 2¢,3¢,4¢,6¢-tetrahydroxychalcone [11]. Recently, we chemically synthesized FKB and demonstrated that systemic administration of FKB exerted potent dose-dependent antinociceptive activity when assessed in the chemical and thermal models of nociception in mice, indicating involvement of the peripheral and central antinociceptive activities [12]. Moreover, in the same study, we demonstrated that the central antinociceptive activity of FKB was not mediated by the activation of opioid receptors. Besides, we also demonstrated that FKB produced marked inhibition of the nociceptive response caused by intraplantar injection of glutamate into mouse hind paw in the glutamate-induced nociception test and perhaps the inhibition of peripheral N-Methyl-D-aspartic acid (NMDA) receptors contributes to the antinociceptive effect of FKB [12]. As activation of the NO cascade is known to take place secondary to NMDA receptor activation and a great deal of evidence has demonstrated the role of NO in various models of nociception [13][14][15][16], this has led to the ...

Polyethyleneglycol bound sulfonic acid (PEG-OSO3H), a chlorosulphonic acid-modified polyethylene glycol was successfully used as an efficient and eco-friendly polymeric catalyst in the synthesis of 14-aryl/heteroaryl-14H-dibenzo[a,j]xanthenes obtained from the reaction of 2-naphthol and carbonyl compounds under solvent-free conditions with short reaction times and excellent yields. The biological properties of these synthesized title compounds revealed that compounds 3b, 3c, 3f and 3i showed highly significant anti-viral activity against tobacco mosaic virus.

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In conclusion, methanol leaves extract of C. nutans exhibited the highest cytotoxic activity against liver cancer cells (Hep-G2). There is a possibility that herb-drug interaction could occur with C. nutans through inhibitory effects on CYP3A4. Additionally, inhibition of C. nutans on CYP2E1 could show anti-carcinogenesis effects in human liver microsomes.

A New Prenylated Isoflavone from Tephrosia tinctoria. -The title compound (I) is isolated from the roots of Tephrosia tinctoria and represents the rare occurrence of an O-geranylated isoflavone from a natural source. -(REDDY, B. A. K.; KHALIVULLA, S. I.; GUNASEKAR*, D.; Indian J.

Residual liming is one of the measures of the efficacy of liming materials. Ca2+-amendments such as calcium hydroxide (Ca(OH)2), calcium oxide (CaO) and calcium carbonate (CaCO3) in soils may contribute to plant growth response in plant height and total dry matter yield of oil palm seedlings. The increasing of other essential elements such as nitrogen (N), phosphorus (P) and ions of potassium (K+) also play a great role in the plant growth and crop yield, conversely, the soil pH and ions of aluminium (Al3+) will inhibit the plant growth and crop yield. This main aim this experiment is to determine the residual liming effect of Ca2+-amendments to highly acidic soils collected from Jeram and Bungor series, Malaysia, which also contains 2 times of Al3+. The highly acidic soils of previously planted with oil palm seedlings initially incubated with selected Ca2+-amendments along with Mg2+-amendments such as, dolomite (CaMg.CO3) for 360 days and, kept for additional 180 days before planting for a total of 540 days in a greenhouse environment. In this experiment, the soil chemical analysis, plant growth response, and the possible mechanisms responsible for the Ca2+-amendment liming effects were measured. The results of the soil chemical analysis showed that Ca2+-amendment residues potentially reduced the soil acidity than Mg2+-amendments. Ca(OH)2 was the most prominent Ca2+-amendment to increase soil-water pH, soil solution pH, and concentrations of soluble Ca2+ and K+. While, concentration of soil solution and exchangeable Al were effectively reduced 540 days after the application of Ca-amendments. The dry shoot weight of the oil palm seedlings improved about 1.67 g/pot and 16.87 g/pot in control and Ca2+-amendment treatments, respectively. In this study, it has showed that the root dry weight of oil palm seedlings increased from 0.18 g/pot to 4.49 g/pot in pot and Ca2+-amended soil, respectively. Increased plant height and total dry matter yield of oil palm seedlings grown on the Ca-amended soils may be attributed to increased soil pH which resulted in lowered concentration and activity of soluble AI, and increased concentrations of soil solution Ca and K which were released of Ca. This finding concluded that the possible mechanisms of Ca2+-amendments from residual liming might be: a) complexation interaction between Al3+ and Ca2+; (b) capacity of Ca-amendments to increase the concentration of Ca to maintain soil desired pH; (c) alleviation effect of Ca-amendments to reduce Al toxicity concentration in the soil. Last but not least, this finding showed that dry matter yield and plant height positively associated with the presence of Al3 + in both soil conditions.