海桐果壳和种子脂肪酸成分研究

目的:分析并比较海桐果壳和种子的脂肪酸成分。方法:采用有机溶剂抽提海桐果壳和种子的挥发油,用KOH-NaOH溶液进行甲酯化,采用气相色谱-质谱联用法分离并确认二者的化学成分。结果:从2种样品中共鉴定出了13种脂肪酸,主要成分均为棕榈酸和油酸。结论:海桐果壳和种子均可作为保健型食用油而开发利用。     

Identification of chemical compounds from the leaves of Leea indica

Twenty-three known chemical compounds were identified in the leaves of Leea indica (Burm. f.) Merr. (Leeaceae) by GC-MS analysis, spectroscopic techniques and co-TLC with authentic samples. The identified compounds include eleven hydrocarbons, phthalic acid, palmitic acid, 1-eicosanol, solanesol, farnesol, three phthalic acid esters, gallic acid, lupeol, beta-sitosterol and ursolic acid. Gallic acid was isolated as n-butyl gallate and identified by co-TLC. This seems to be the first report of the presence of gallic acid in the leaves of L. indica.     

Protective effect of Coccinia indica on changes in the fatty acid composition in streptozotocin induced diabetic rats

The present study was undertaken to investigate the effect of Coccinia indica, an indigenous plant used in Ayurvedic Medicine in India, on blood glucose, plasma insulin, cholesterol, triglycerides, free fatty acids and phospholipids and fatty acid composition of total lipids in liver, kidney and brain of normal and streptozotocin (STZ) diabetic rats. Oral administration of the ethanolic extract of Coccinia indica leaves (200 mg/kg body weight, CLEt) for 45 days to diabetic rats decreased the concentrations of blood glucose, lipids and fatty acids, viz., palmitic, stearic, and oleic acid whereas linolenic and arachidonic acid and plasma insulin were elevated. These results suggest that CLEt exhibits hypoglycaemic and hypolipidaemic effects in STZ induced diabetic rats. It also prevents the fatty acid changes produced during diabetes. The effect of CLEt at 200 mg/kg body weight was better than that of glibenclamide.     

Ion exchange interactions on silica gel layers. III. Salts of organic bases with organic acids. Organic acids and sodium salts

By thin-layer chromatographic and spectroscopic (UV, IR) methods it has been proved that bass and acid are formed from salts of organic bases with organic acids during primary interaction because of the ion exchange behaviour of the silica gel layer. The organic acids formed have interacted with metals on the layer during secondary ion exchange and they migrate further as salts again. It has also been established that the extent of secondary ion exchange between metal silanate groups and acids depends on pKS values of acids. On the basis of investigations it can be ascertained with great probability that organic acids of pKS greater than 7 do not interact with metal silanate groups of silica gel layer. Sodium salts of organic acids of pKS less than 3 values similarly do not interact on the other hand sodium salts of organic acids of pKS greater than 3 values are able to interact with silanol groups. It has been established by flame atomic emission method that salicylic acid interacts with sodium ion and 86% of it migrates further as sodium salicylate.     

Phenolic acids in neem (Azadirachta indica): a major pre-existing secondary metabolites

High Performance Liquid Chromatographic (HPLC) analyses of various parts (fresh and dry bark of stem, mature and tender leaves, flower and different parts of fruit, i.e., raw and ripe fruit epicarp, mesocarp and seed) of neem (Azadirachta indica), which occupies an important place in socio-cultural-religious life in Indian communities, indicate that neem is rich in pre-existing secondary metabolites (phenolic acids). Dry bark showed only tannic acid but in fresh bark three phenolic acids were observed, i.e., gallic, tannic, and ferulic acids. In tender leaves only gallic and ferulic acids were detected, but the levels of these phenolic acids in mature leaves were about three times and fifty times greater, respectively. Flowers had only two phenolic acids in which gallic acid was maximum followed by chlorogenic acid. The level of phenolic acid was maximum in seeds followed by epicarp and pulp. In raw and ripe fruit seeds four phenolic acids were detected. Raw fruit seeds were rich in phenolic acids than ripe fruit seeds. Fruit epicarp was relatively richer than seed, seed pulp and flowers of the plants. Neem flowers were also rich in gallic and chlorogenic acids.     

Acidity constants of sparingly water-soluble drugs from potentiometric determinations in aqueous dimethyl sulfoxide

A brief analysis of the acid-base equilibria in pure organic solvents and/or in their aqueous mixtures is reported with the aim of determining dissociation constants of acidic drugs that are sparingly soluble in water. Among aqueous organic mixtures, aqueous Me2SO (80% w/w) presents properties particularly suitable for acid-base studies, and thermodynamically meaningful acidity constants can be obtained by a potentiometric technique, provided that the glass electrode is properly calibrated. Thermodynamic acidity constants of more than 100 acids have been potentiometrically determined at 25 degrees C in this mixed solvent, and the selected series of acids has been divided into four classes according to the nature of the acidic group (COOH, OH, SH) and the structure of the acid (aliphatic, aromatic, heterocyclic). A linear relationship between the experimental pKa values in water and pKa values in aqueous Me2SO (80% w/w) has been found within the single classes and a group of equations has been derived (the asterisk denotes pKa values in which infinite dilution in the mixed solvent is taken as a standard state). For the carboxylic acid class, the following "common" equation has been found: pKa(H2O) = -0.80 + 0.67 pKa (Me2SO; 80% w/w). As an application, pKa values in water are reported for a representative number of sparingly soluble acids. These values have been calculated by means of the "common" equation, using pKa values experimentally determined in aqueous Me2SO (80% w/w). The calculated values are in good agreement with those expected from the acid structures.     

Activity-guided isolation and identification of Azadirachta indica bark extract constituents which specifically inhibit chemiluminescence production by activated human polymorphonuclear leukocytes

The A. indica crude aqueous bark extract inhibits the generation of chemiluminescence by activated human polymorphonuclear leukocytes (PMN). Guided by this activity the responsible compounds were purified by extraction with different organic solvents and HPLC. Gallic acid, (+)-gallocatechin, (-)-epicatechin, and (as a 2:1 mixture) (+)-catechin and epigallocatechin were isolated and identified by means of HPLC, TLC, MS, 1H-NMR, UV, and CD data. Commercial samples of gallic acid, (+)-catechin and (-)-epicatechin showed the same effects. To our knowledge the identified catechins have never been described as constituents of A. indica.     

Cassava cyanogens and free amino acids in raw and cooked leaves.

Cassava leaves (Manihot esculenta Crantz) constitute the main daily source of protein as supplement to the major staple food, the processed cassava roots in remote rural areas of Africa. Konzo, an upper motoneurone disease with permanent spastic paralysis of both legs, has been reported among populations consuming this unbalanced diet. In commercial pounded cassava leaves residual cyanogens and the presence of inherent potentially toxic non-protein amino acids were analysed to check their safety. The initial total cyanogens before cooking ranged from 35.9+/-0.4 to 107.5+/-0.8 mg HCN (hydrogen cyanide) equivalent kg(-1) dry weight. After cooking, the residual cyanogens were significantly reduced (P<0.05) ranging from 0.30+/-0.04 to 1.9+/-0.2 mg HCN equivalent kg(-1) dry weight, and were below the recommended FAO/WHO safe limit set at 10 mg HCN equivalent kg(-1) dry weight. The total free amino acids and trigonelline (N-methyl-nicotinic acid) detected varied from 10.8 g kg(-1) dry weight to 38.2 g kg(-1) dry weight in the raw and from 7.4 g kg(-1) dry weight to 25.6 g kg(-1) dry weight in the cooked cassava leaves. The non-protein amino acids gamma-amino butyric acid (GABA) and alpha-amino butyric acid (alpha-ABA) were detected. No known potentially toxic non-protein amino acid was found. In konzo-affected areas, cassava leaves with inadequate preparation and cooking can be a non-negligible source of dietary exposure to cyanogens apart from the cassava roots that are suggested to be involved in the aetiology of konzo.     

柱前衍生RP-HPLC法测定桑叶中16种游离氨基酸的含量

目的:建立柱前衍生法测定桑叶中游离氨基酸的含量。方法:以水超声提取桑叶中的氨基酸,以异硫氰酸苯酯柱前衍生,采用反相高效液相色谱法测定氨基酸的含量。结果:桑叶中含有苏氨酸、缬氨酸、脯氨酸、蛋氨酸、谷氨酸、甘氨酸、亮氨酸、苯丙氨酸、酪氨酸、天门冬氨酸、γ-氨基丁酸、丙氨酸、组氨酸、胱氨酸、色氨酸、异亮氨酸等16种游离氨基酸;其中人体必需氨基酸有7种,人体半必需氨基酸有1种,含量占氨基酸总量的20%左右。结论:本法不需要专门的氨基酸分析仪,操作简便、灵敏度高,结果准确、可靠。桑叶中氨基酸的种类齐全、含量丰富,具有很高的开发利用价值。     

Targeted metabolite analysis of Catharanthus roseus and its biological potential

Catharanthus roseus is nowadays one of the most studied medicinal plants. In this work, further knowledge on different parts of this species (leaves, stems, seeds and petals) was achieved, namely phenolics by HPLC-DAD and organic acids and amino acids by HPLC-UV. Also, the biological potential, expressed as acetylcholinesterase inhibitory activity was accessed and, in some parts, an acetylcholinesterase inhibitory capacity higher than 85% was found (IC₅₀ at 422, 442 and 2683 μg/mL in leaves, stems and petals, respectively). C. roseus aqueous extract revealed to be a rich source of phenolics, namely caffeoylquinic acids and flavonoids derivatives (up to 4127 mg/kg in stems, 4484 mg/kg in seeds, 8688 mg/kg in leaves and 41125 mg/kg in petals), organic acids (962, 6678, 25972 and 12463 mg/kg in seeds, petals, stems and leaves, respectively), such as citric acid (over 85% in some plant parts), and amino acids (31557, 39327, 50540 and 159697 mg/kg in stems, petals, seeds and leaves, respectively), of which arginine was a major compound.     

Resin glycosides from the leaves and stems of <Emphasis Type="Italic">Ipomoea digitata</Emphasis>

Alkaline hydrolysis of the ether-soluble resin glycoside (jalapin) fraction of the leaves and stems of Ipomoea digitata L. (Convolvulaceae) gave six organic acids, isobutyric, (S)-2-methylbutyric, tiglic, n-decanoic, n-dodecanoic, and cinnamic acids, and two glycosidic acids, quamoclinic acid A and operculinic acid A. Further, a new genuine resin glycoside, named digitatajalapin I, was isolated from the jalapin fraction, along with three known resin glycosides. Their structures have been determined on the basis of chemical and spectroscopic data.     

银杏酸的高效液相色谱法测定

目的建立银杏酸的简便预净化处理和HPLC含量测定方法。方法用LC/DAD/ESI/MS对银杏酸进行定性鉴定。银杏叶经正己烷提取、硅胶柱色谱净化处理,HPLC测定。色谱分析条件:色谱柱为Inertsil ODS-2,流动相为甲醇-3% HAc溶液(92∶8),流速1.0 mL·min^-1,柱温40℃,紫外检测波长310 nm。结果银杏叶中存在5种银杏酸C13∶0,C15∶0,C15∶1,C17∶1和C17∶2,其中C15∶1和C17∶1约占银杏酸的85%,C17∶2银杏酸未见国内文献报道。银杏叶提取物经硅胶柱色谱处理后,其HPLC谱中除银杏酸峰外,几无其他杂质峰。平均回收率97.0%,RSD为1.7%(N=6)。结论该方法准确、简便、可靠,可用于银杏酸的定量分析。     

In vitro metabolism of 8-2 fluorotelomer alcohol: interspecies comparisons and metabolic pathway refinement.

The detection of perfluorinated organic compounds in the environment has generated interest in their biological fate. 8-2 Fluorotelomer alcohol (8-2 FTOH, C(7)F(15)CF(2)CH(2)CH(2)OH), a raw material used in the manufacture of fluorotelomer-based products, has been identified in the environment and has been implicated as a potential source for perfluorooctanoic acid (PFOA) in the environment. In this study, the in vitro metabolism of [3-(14)C] 8-2 FTOH and selected acid metabolites by rat, mouse, trout, and human hepatocytes and by rat, mouse, and human liver microsomes and cytosol were investigated. Clearance rates of 8-2 FTOH in hepatocytes indicated rat > mouse > human >/= trout. A number of metabolites not previously reported were identified, adding further understanding to the pathway for 8-2 FTOH metabolism. Neither perfluorooctanoate nor perfluorononanoate was detected from incubations with human microsomes. To further elucidate the steps in the metabolic pathway, hepatocytes were incubated with 8-2 fluorotelomer acid, 8-2 fluorotelomer unsaturated acid, 7-3 acid, 7-3 unsaturated acid, and 7-2 secondary fluorotelomer alcohol. Shorter chain perfluorinated acids were only observed in hepatocyte and microsome incubations of the 8-2 acids but not from the 7-3 acids. Overall, the results indicate that 8-2 FTOH is extensively metabolized in rats and mice and to a lesser extent in humans and trout. Metabolism of 8-2 FTOH to perfluorinated acids was extremely small and likely mediated by enzymes in the microsomal fraction. These results suggest that human exposure to 8-2 FTOH is not expected to be a significant source of PFOA or any other perfluorocarboxylic acids.     

Fatty acid composition and antibacterial potential of Cassia tora (leaves and stem) collected from different geographic areas of India

The comparative analysis of the fatty acid composition of Cassia tora (leaves and stem) was determined using gas chromatography–mass spectrometry. Twenty-seven fatty acids were identified in C. tora (leaves and stem) which was collected from three different geographical areas of India: Lucknow (Uttar Pradesh), Nainital (Uttarakhand), and Bhavnagar (Gujarat), coded as CT-1, CT-2, and CT-3, respectively. The gas chromatography–mass spectrometry analysis showed the presence of various saturated and unsaturated fatty acids. The major fatty acids found were palmitic acid, linoleic acid, linolenic acid, margaric acid, melissic acid, and behenic acid. The highest amounts of saturated fatty acids were found in leaves of C. tora collected from Bhavnagar (Gujarat) (60.7% ± 0.5%). Thus, the study reveals that C. tora has a major amount of nutritionally important fatty acids, along with significant antimicrobial potential. Fatty acids play a significant role in the development of fat products with enhanced nutritional value and clinical application. Remarkable differences were found in the present study between fatty acid profiles of C. tora collected from different locations in India. To the best of our knowledge there is no previously reported comparative study of the fatty acids of C. tora.     

Inhibitory effect of cholephilic anions on fatty acid uptake by the perfused rat liver

The mechanisms of uptake and intracellular transport of plasma free fatty acids by the liver cell are poorly known. A cytosolic protein, termed Z protein, has been identified in the liver, intestine and other tissues; in vitro studies show a high affinity of fatty acid and organic anions for this protein and suggest that it could be involved in the cellular transport of fatty acids in vivo. The present experiments demonstrate an inhibitory effect of various organic cholephilic anions (B.S.P., D.B.S.P., flavaspidic acid, bilirubin, etc) on fatty acid uptake by the isolated perfused rat liver. This inhibition is rapidly reversible when the liver is perfused with a medium lacking cholephilic anions, which together with the absence of any functional or ultrastructural damage to the organ, excludes any hepatotoxic effect. Such an inhibition of fatty acid uptake could be due to a competition for binding either to membrane sites and/or to intracellular carriers common to both fatty acids and cholephilic anions. These data are consistent with the involvement of carrier-mediated processes in fatty acid transport in the liver. Finally, simultaneous uptake of radioactive fatty acid and cholephilic anions does not interfere with further fatty acid utilization by the cell.     

Chemical constituents of Hainan Syzygium myrsinifolium (Hance) Merr. et Perry based on ultra-high performance liquid chromatography-time-of-flight tandem mass spectrometry

Syzygium myrsinifolium (Hance) Merr. et Perry is a unique plant resource on Hainan Island, and there are few reports on its chemical constituents. In the present study, we identified the major chemical constituents in the leaves of Syzygium myrsinifolium (Hance) Merr. et Perry using ultra-high performance liquid chromatography coupled with electrospray ionization quadrupole time-of-flight tandem mass spectrometry (UPLC-Q-TOF-MS/MS). The chemical constituents in Syzygium myrsinifolium (Hance) Merr. et Perry were identified rapidly based on the accurate relative molecular mass and combined with literature data and reference substances. A total of 20 compounds, including organic acids, phenolic acids, and flavonoids, were identified. Among these 20 compounds, four organic acids, eight phenolic acids, seven flavonoids, and one coumarin were reported from the leaves of Syzygium myrsinifolium (Hance) Merr. et Perry for the first time. The established method was rapid and accurate, and some chemical constituents in the leaves of Syzygium myrsinifolium (Hance) Merr. et Perry have been identified. This research provided an experimental reference for the study of the constituents and utilization of Syzygium myrsinifolium (Hance) Merr. et Perry.     

基于气相色谱质谱联用法对金黄色葡萄球菌中6种有机酸的测定

目的 采用气相色谱质谱联用法(GC-MS)建立临床耐药金黄色葡萄球菌中琥珀酸、延胡索酸、苹果酸、草酰乙酸、α-酮戊二酸及柠檬酸的测定方法。方法 6种有机酸由硅烷化试剂N,O-双(三甲基硅烷基)三氟乙酰胺(含1%三甲基氯硅烷)(BSTFA-TMCS)衍生化后,采用选择离子扫描模式(SIR)以外标法进行定量测定。结果 6种有机酸在0.31～300μg/mL范围内线性良好,相关系数大于0.99,回收率在83.02%～109.28%之间。同时,利用该方法对乳酸左氧氟沙星处理后的金黄色葡萄球菌胞内6种有机酸含量进行测定,与未经乳酸左氧氟沙星处理的SA相比6种有机酸代谢含量均表达下调。结论 该方法受基质影响小,重现性好,适合于复杂生物基质样本中有机酸含量的测定,同时发现乳酸左氧氟沙星是通过柠檬酸循环途径抑制金黄色葡萄球菌生长。     

Mercapturic acids (N-acetylcysteine S-conjugates) as endogenous substrates for the renal organic anion transporter-1

Mercapturic acids are N-acetyl-L-cysteine S-conjugates that are formed from a range of endogenous and exogenous chemicals. Although the kidney is a major site for elimination of mercapturic acids, the transport mechanisms involved have not been identified. The present study examined whether mercapturic acids are substrates for the renal basolateral organic anion transporter-1 (Oat1) from rat kidney. This carrier mediates uptake of organic anions from the bloodstream in exchange for intracellular alpha-ketoglutarate. Uptake of [(3)H]p-aminohippuric acid (PAH) in Oat1-expressing Xenopus laevis oocytes was strongly inhibited by S-(2,4-dinitrophenyl)-N-acetyl-L-cysteine (DNP-NAC) and by all other mercapturic acids tested, including the endogenous mercapturic acid N-acetyl-leukotriene E(4). Inhibition by the mercapturic acids was competitive, which is consistent with the hypothesis that these compounds are substrates for Oat1. This conclusion was supported by the direct demonstration of saturable [(35)S]DNP-NAC uptake in Oat1-expressing oocytes. [(35)S]DNP-NAC uptake was inhibited by PAH and other mercapturic acids and was stimulated in oocytes preloaded with glutarate. The apparent K(m) value for DNP-NAC uptake was only 2 microM, indicating that this mercapturic acid is a high affinity substrate for Oat1. Together, these data indicate that clearance of endogenous mercapturic acids is an important function of the renal organic anion transporter.     

芒果叶提取物体外抗菌作用研究

目的研究芒果叶提取物的体外抗菌效果。方法采用琼脂二倍稀释法，观察芒果叶提取物对，临床常见呼吸道感染菌的抑制作用。结果芒果叶提取物对6种常见的呼吸道感染菌（铜绿假单胞菌、大肠埃希菌、肺炎克雷伯杆菌、鲍氏不动杆菌、金黄色葡萄球菌和表皮葡萄球菌）有较强的体外抑制作用，其最低抑菌浓度（MIC）0．107—0．320mg／mL；细菌接种量增加和培养基pH值降低均可使芒果叶提取物的MIC增加1—3倍。结论芒果叶提取物对6种常见呼吸道感染菌具有较强的体外抗菌作用。     

Ficus carica L.: Metabolic and biological screening

Ficus carica L. is one of the earliest cultivated fruit trees. In this work, metabolite profiling was performed on the leaves, pulps and peels of two Portuguese white varieties of F. carica (Pingo de Mel and Branca Tradicional). Phenolics and organic acids profiles were determined by HPLC/DAD and HPLC/UV, respectively. All samples presented a similar phenolic profile composed by 3-O- and 5-O-caffeoylquinic acids, ferulic acid, quercetin-3-O-glucoside, quercetin-3-O-rutinoside, psoralen and bergapten. 3-O-Caffeoylquinic acid and quercetin-3-O-glucoside are described for the first time in this species. Leaves’ organic acids profile presented oxalic, citric, malic, quinic, shikimic and fumaric acids, while in pulps and peels quinic acid was absent. The antioxidant potential of the different plant parts was checked. All materials exhibited activity against DPPH and nitric oxide radicals in a concentration-dependent way. However, only the leaves presented capacity to scavenge superoxide radical. Leaves were always the most effective part, which seems to be related with phenolics compounds. Additionally, acetylcholinesterase inhibitory capacity was evaluated, but no effect was observed. Antimicrobial potential was also assessed against several bacterial species, although no activity was noticed. This is the first study comparing the chemical composition and biological potential of F. carica pulps, peels and leaves.