• The Korean Journal of Pharmacology
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• v.31 no.3
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• pp.299-311
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• 1995

Platelets resemble monoaminergic neurons in several respects, i.e. the uptake of 5-HT and its inhibition, the subcellular storage and release of 5-HT, and the metabolism of aromatic amines brought about by monoamine oxidase. And the 5-HT content of rabbit platelets is well known to be about 40 times higher than that of human platelets. Therefore, this study was carried out to investigate the influences of amitriptyline (AMT) and sertraline (SRT) on the aggregation, contents of signaling second messengers, and protein phosphorylations of rabbit platelets in response to thrombin, 0.25 unit/ml, comparing with those of chlorpromazine (CPZ). Thrombin-induced aggregation was inhibited by SRT $(IC50:4.37{\times}10^{-5}\;M)$, CPZ $(IC50:5.76{\times}10^{-5}\;M)$, and AMT $(IC50:1.15{\times}10^{-4}\;M)$, respectively, and the aggregation by A23187 $(1.0\;{\mu}M)$ or PMA (320 nM) was also inhibited by SRT, CPZ, and AMT. AMT, SRT, and CPZ had little affects on basal contents of platelet $TXB_2$ and $PGE_2$, but all of them inhibited the thrombin-induced increase of $TXB_2$. Thrombin did not change the platelet contents of cAMP and cGMP. CPZ, AMT, and SRT produced the slight decrease of basal cAMP content, and their effects were not affected by thrombin-treatment. But SRT and AMT moderately increased the basal cGMP content, and the cGMP content of thrombin-stimulated platelets was gradually increased by the pretreatment with SRT, AMT, and CPZ. Particularly, the SRT-dependent increase of the cGMP content was notable. Platelet $Ins(1,4,5)P_3$ content was rapidly increased up to a plateau within 10 sec after thrombin-stimulation, AMT, SRT, and CPZ increased the basal $Ins(1,4,5)P_3$ content, and the thrombin-dependent increase was enhanced by pretreatment with CPZ and AMT, but was blunted by SRT. Platelet $[Ca^{2+}]_i$, was rapidly increased up to a peak level within 20 sec after thrombin-stimulation. The increase of $[Ca^{2+}]_i$ was sisnificantly inhibited by AMT, SRT, and CPZ. Thrombin- or PMA-induced phosphorylations of platelet $41{\sim}43\;kDa$ and 20 kDa proteins were significantly inhibited by AMT, SRT, and CPZ. These results suggest that the antiplatelet activities of AMT and CPZ may be considerably attributed to the inhibition of protein kinase C activity, and the activity of SRT may be associated with the inhibitory effect on the thrombin-induced increase of $Ins(1,4,5)P_3$ and the increasing effect on the cGMP content of ptatelets. Therefore, it seems to be evident that AMT and SRT may produce their antidepressant activity, at least, partly through the inhibition of protein kinase C activity or the increase of resting $Ins(1,4,5)P_3$, content and in case of SRT, to a lesser extent, via the increase of cGMP in the brain.

• Applied Biological Chemistry
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• v.17 no.3
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• pp.149-176
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• 1974

Eight substituted diphenyl ether herbicides and some of their photoproducts were studied in terms of solution phase photolysis under simulated environmental conditions by using a Rayonet photochemical reactor. The test compounds absorbed sufficient light energy at the wavelength of 300 nm to undergo various photoreactions. All the photoproducts were confirmed by means of tlc, glc, ir, ms, and/or nmr spectrometry. The results obtained are summarized as follows: Solution phase photolysis of C-6989: An exceedingly large amount of p-nitrophenol formed strongly indicates the readiness of the ether linkage cleavage of this compound as the main reaction in all solvents used. Photoreduction of nitro to amino group(s) and photooxidation of trifluoromethyl to carboxyl group were recognized as minor reactions. Aqueous photolysis of p-nitrophenol: Quinone(0.28%), hydroquinone (0.66%), and p-aminophenol (0.42%) were confirmed as photoproducts, in addition to a relatively small amount of an unknown compound. The mechanisms of formation of these products were proposed to be the nitro-nitrite rearrangement via $n{\rightarrow}{\pi}^*$ excitation and the photoreduction through hydrogen abstractions by radicals, respectively. Solution phase photolysis of Nitrofen: Photochemical reduction leading to the p-amino derivative was the main reaction in n-hexane. In aqueous solution, the photoreduction of nitro to amino group and hydroxylation predominated over the ether linkage cleavage. Nucleophilic displacement of the nitro group by hydroxide ion and replacement of chlorine substituents by hydroxyl group or, to a lesser extent, hydrogen were also observed as minor reactoins. Solution phase photolysis of MO-338: Photoreduction of the nitro to amino group was marked in the n-hexane solution photolysis. In the aqueous solution, photoreduction of the nitro substituent and hydroxylation were the main reactions with replacement of chlorine substituents by the hydroxyl group and hydrogen, and cleavage of the ether linkage as minor reactions. Photolyses of MC-4379, MC-3761, MC-5127, MC-6063, and MC-7181 in n-hexane and cyclohexane: Photoreduction of the nitro group leading to the corresponding amino derivative and replacement of one of the halogen substituents by hydrogen from the solvent used were the key reactions in each compound. Aqueous photolysis of MC-4379: Cleavage of the ether linkage, replacement of the carboxymethyl by hydroxyl group, hydroxylation, and replacement of the nitro by hydroxy group were prominent with photoreduction and dechlorination as minor reactions. Aqueous photolysis of MC-3761: Cleavage of the ether linkage, replacement of the carboxymethyl by hydroxyl group, and photoreduction followed by hydroxylation were the main reactions. Aqueous photolysis of MC-5127: Replacement of carboxyethyl by hydrogen was predominant with ether linkage cleavage, photoreduction, and dechlorination as minor reactions. It was obvious that the decarboxyethylation proceeded more readily than decarboxymethylation occurring in the other compounds. Aqueous photolysis of MC-6063: Cleavage of the ether linkage and photodechlorination were the main reactions. Aqueous photolysis of MC-7181: Replacement of the carboxymethyl group by hydrogen and monodechlorination were the remarkable reactions. Cleavage of the ether linkage and hydroxylation were thought to be the minor reactions. Aqueous photolysis of 3-carboxymethyl-4-nitrophenol: The photo-induced Fries rearrangement common to aromatic esters did not appear to occur in the carboxymethyl group of this type of compound. Conversion of nitro to nitroso group was the main reaction.

• KOREAN JOURNAL OF CROP SCIENCE
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• v.47
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• pp.15-32
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• 2002

The endeavors enhancing the grain quality of high-yielding japonica rice were steadily continued during 1980s-1990s along with the self-sufficiency of rice production and the increasing demands of high-quality rices. During this time, considerably great progress and success was obtained in development of high-quality japonica cultivars and quality evaluation techniques including the elucidation of interrelationship between the physicochemical properties of rice grain and the physical or palatability components of cooked rice. In 1990s, some high-quality japonica rice cultivars and special rices adaptable for food processing such as large kernel, chalky endosperm, aromatic and colored rices were developed and its objective preference and utility was also examined by a palatability meter, rapid-visco analyzer and texture analyzer, Recently, new special rices such as extremely low-amylose dull or opaque non-glutinous endosperm mutants were developed. Also, a high-lysine rice variety was developed for higher nutritional utility. The water uptake rate and the maximum water absorption ratio showed significantly negative correlations with the K/Mg ratio and alkali digestion value(ADV) of milled rice. The rice materials showing the higher amount of hot water absorption exhibited the larger volume expansion of cooked rice. The harder rices with lower moisture content revealed the higher rate of water uptake at twenty minutes after soaking and the higher ratio of maximum water uptake under the room temperature condition. These water uptake characteristics were not associated with the protein and amylose contents of milled rice and the palatability of cooked rice. The water/rice ratio (in w/w basis) for optimum cooking was averaged to 1.52 in dry milled rices (12% wet basis) with varietal range from 1.45 to 1.61 and the expansion ratio of milled rice after proper boiling was average to 2.63(in v/v basis). The major physicochemical components of rice grain associated with the palatability of cooked rice were examined using japonica rice materials showing narrow varietal variation in grain size and shape, alkali digestibility, gel consistency, amylose and protein contents, but considerable difference in appearance and texture of cooked rice. The glossiness or gross palatability score of cooked rice were closely associated with the peak, hot paste and consistency viscosities of viscosities with year difference. The high-quality rice variety "IIpumbyeo" showed less portion of amylose on the outer layer of milled rice grain and less and slower change in iodine blue value of extracted paste during twenty minutes of boiling. This highly palatable rice also exhibited very fine net structure in outer layer and fine-spongy and well-swollen shape of gelatinized starch granules in inner layer and core of cooked rice kernel compared with the poor palatable rice through image of scanning electronic microscope. Gross sensory score of cooked rice could be estimated by multiple linear regression formula, deduced from relationship between rice quality components mentioned above and eating quality of cooked rice, with high probability of determination. The $\alpha$-amylose-iodine method was adopted for checking the varietal difference in retrogradation of cooked rice. The rice cultivars revealing the relatively slow retrogradation in aged cooked rice were IIpumbyeo, Chucheongyeo, Sasanishiki, Jinbubyeo and Koshihikari. A Tonsil-type rice, Taebaegbyeo, and a japonica cultivar, Seomjinbyeo, showed the relatively fast deterioration of cooked rice. Generally, the better rice cultivars in eating quality of cooked rice showed less retrogradation and much sponginess in cooled cooked rice. Also, the rice varieties exhibiting less retrogradation in cooled cooked rice revealed higher hot viscosity and lower cool viscosity of rice flour in amylogram. The sponginess of cooled cooked rice was closely associated with magnesium content and volume expansion of cooked rice. The hardness-changed ratio of cooked rice by cooling was negatively correlated with solids amount extracted during boiling and volume expansion of cooked rice. The major physicochemical properties of rice grain closely related to the palatability of cooked rice may be directly or indirectly associated with the retrogradation characteristics of cooked rice. The softer gel consistency and lower amylose content in milled rice revealed the higher ratio of popped rice and larger bulk density of popping. The stronger hardness of rice grain showed relatively higher ratio of popping and the more chalky or less translucent rice exhibited the lower ratio of intact popped brown rice. The potassium and magnesium contents of milled rice were negatively associated with gross score of noodle making mixed with wheat flour in half and the better rice for noodle making revealed relatively less amount of solid extraction during boiling. The more volume expansion of batters for making brown rice bread resulted the better loaf formation and more springiness in rice breed. The higher protein rices produced relatively the more moist white rice bread. The springiness of rice bread was also significantly correlated with high amylose content and hard gel consistency. The completely chalky and large grain rices showed better suitability far fermentation and brewing. The glutinous rice were classified into nine different varietal groups based on various physicochemical and structural characteristics of endosperm. There was some close associations among these grain properties and large varietal difference in suitability to various traditional food processing. Our breeding efforts on improvement of rice quality for high palatability and processing utility or value-adding products in the future should focus on not only continuous enhancement of marketing and eating qualities but also the diversification in morphological, physicochemical and nutritional characteristics of rice grain suitable for processing various value-added rice foods.ice foods.