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    • 1. 发明授权
    • 2,3,4-triacylhexoses and mixtures thereof
    • 2,3,4-三酰基己糖及其混合物
    • US4745186A
    • 1988-05-17
    • US828108
    • 1986-02-10
    • John B. MuddBasil A. BurkeJon F. FobesMuraleedharan G. Nair
    • John B. MuddBasil A. BurkeJon F. FobesMuraleedharan G. Nair
    • A21D2/08A21D10/04A23D7/015A23L1/24A23L1/305A61K8/60A61K8/97A61Q1/06A61Q3/02A61Q5/06A61Q9/02A61Q15/00A61Q17/04A61Q19/00A61Q19/10C07H13/06C07H13/02C07H11/00
    • A61Q19/00A21D10/04A21D2/08A23D7/015A23L27/60A23L33/17A61K8/60A61K8/97C07H13/06A61Q1/06A61Q15/00A61Q17/04A61Q19/001A61Q19/002A61Q19/10A61Q3/02A61Q5/06A61Q9/02Y10S514/846Y10S514/847
    • The present invention comprises a new class of 2,3,4-tri-O-acylhexoses and mixtures thereof. Members of the new class of compounds are comprised of a hexose sugar having fatty acids attached at the 2, 3 and 4 positions of the hexose moiety. The fatty acids can be saturated or unsaturated, and can have a relative molecular size of up to C.sub.30. When at least one of the acylating fatty acid groups on the hexose molecule contains more than 7 carbons, the resulting 2,3,4-tri-O-acylhexoses (or mixtures thereof) have a non-bitter taste. On the other hand, when none of the acylating fatty acids have more than 7 carbons, the resulting 2,3,4-tri-O-acylhexoses (and mixtures that contain them) are bitter when tasted.The new 2,3,4-tri-O-acylhexoses can be synthesized using known chemical methods. Alternatively, the new compounds, and especially mixtures thereof, are obtained as the result of selective extraction and purification of the epicuticular exudate from Lycopersicon pennellii plant parts. Mixtures of 2,3,4-tri-O-acylhexoses, especially as found in the Lycopersicon pennellii natural plant extract, or the glucolipid fraction thereof, are useful as evaporation suppressants, antitranspirants and antidesiccants. The Lycopersicon pennellii natural plant extract is also useful as an ingredient in cosmetic and toiletry formulations, while the non-bitter glucolipid subfraction is especially useful as a "low calorie" substitute for fats in foods.
    • 本发明包括一类新的2,3,4-三-O-酰基己糖及其混合物。 新类化合物的成员由在己糖部分的2,3和4位上连接有脂肪酸的己糖组成。 脂肪酸可以是饱和的或不饱和的,并且可以具有高达C30的相对分子大小。 当己糖分子上的至少一个酰化脂肪酸基团含有多于7个碳时,得到的2,3,4-三-O-酰基己糖(或其混合物)具有非苦味。 另一方面,当酰化脂肪酸不超过7个碳时,得到的2,3,4-三-O-酰基己糖(和含有它们的混合物)在品尝时是苦的。 新的2,3,4-三-O-酰基己糖可以使用已知的化学方法合成。 或者,作为从番茄植物部分选择性提取和纯化表皮渗出物的结果,获得新化合物,特别是其混合物。 2,3,4-三-O-酰基己糖的混合物,特别是在番茄番茄植物提取物中发现的,或其糖脂部分,可用作蒸发抑制剂,防转铁剂和防腐剂。 番茄番茄天然植物提取物也可用作化妆品和化妆品配方中的成分,而非苦味的葡萄糖脂亚类特别可用作食品中脂肪的“低热量”替代物。
    • 2. 发明授权
    • Antimicrobial/antifungal compositions
    • 抗微生物/抗真菌组合物
    • US4876277A
    • 1989-10-24
    • US55737
    • 1987-05-29
    • Basil A. BurkeMuraleedharan G. Nair
    • Basil A. BurkeMuraleedharan G. Nair
    • A01N43/30C07D317/64
    • A01N43/30C07D317/64
    • Substituted olefinic (allyl) benzene compounds which exhibit important antimicrobial (antibacterial and antifungal) activity, compositions and methods of delivery against pathovars and pathogens, and methods of synthesis from commonly available reactants. The antifungal composition active ingredient is one or more 4,5-substituted 2,3-alkylidenedioxy-1-olefinic benzenes of the formula: ##STR1## where R.sub.1 and R.sub.2 may be the same or different, and are selected from OH, and C.sub.1 -C.sub.5 alkoxy (--OR) or thioalkyl (--SR) groups. R.sub.3 and R.sub.4 are selected from H and C.sub.1 -C.sub.5 alkyl, alkenyl and alkynyl groups, and R.sub.5 is selected from C.sub.3 -C.sub.7 alkyl, alkenyl and alkynyl groups. The preferred compounds are 4,5-substituted-2,3-methylenedioxy-1-allyl benzenes. Where R.sub.1 =OCH.sub.3, R.sub.2 =OH, R.sub.3 and R.sub.4 =H and R.sub.5 =allyl (2',3' propenyl) the compound may be called nor methyl-pseudo-dillapiole. Where R.sub.1 =R.sub.2 =OCH.sub.3, R.sub.3 and R.sub.4 are again H, and R.sub.5 =allyl, the compound may be called pseudo-dillapiole. Compositions including these compounds exhibit antimicrobial activity against a variety of pathogens and pathovars, e.g., Xanthomonas campestris spp. bacteria, antifungal activity against a variety of fungi and bacteria, and are highly specific, e.g., antifungal activity against wheat powdery mildew, but do not affect seed germination or have herbicidal or insecticial activity. Methods and compositions for delivery of these agents against such pathogens, and methods of chemical synthesis of the compounds are disclosed.
    • 显示出重要的抗微生物(抗菌和抗真菌)活性,组合物和递送针对病原体和病原体的方法的取代的烯丙基(烯丙基)苯化合物,以及通常可得的反应物的合成方法。 抗真菌组合物活性成分是一种或多种下式的4,5-取代的2,3-亚烷基二氧基-1-烯烃苯:其中R 1和R 2可以相同或不同,并且选自OH, 和C 1 -C 5烷氧基(-OR)或硫代烷基(-SR)基团。 R3和R4选自H和C1-C5烷基,烯基和炔基,R5选自C3-C7烷基,烯基和炔基。 优选的化合物是4,5-取代-2,3-亚甲二氧基-1-烯丙基苯。 其中R1 = OCH3,R2 = OH,R3和R4 = H,R5 =烯丙基(2',3'丙烯基),化合物可称为甲基假鞭毛虫。 当R 1 = R 2 = OCH 3时,R 3和R 4再次为H,R 5为烯丙基,该化合物可称为伪鞭毛虫。 包括这些化合物的组合物对各种病原体和病原体表现出抗菌活性,例如野油菜黄单胞菌(Xanthomonas campestris spp。) 细菌,针对各种真菌和细菌的抗真菌活性,并且是高度特异性的,例如抗小麦白粉病的抗真菌活性,但不影响种子发芽或具有除草或昆虫活性。 公开了用于递送这些试剂以抵抗这种病原体的方法和组合物,以及化合物的化学合成方法。
    • 10. 发明授权
    • Anticancer anthraquinones and method of use thereof
    • 抗癌蒽醌类及其使用方法
    • US06875746B1
    • 2005-04-05
    • US10355483
    • 2003-01-31
    • Muraleedharan G. NairRobert H. CichewiczNavindra P. SeeramYanjun Zhang
    • Muraleedharan G. NairRobert H. CichewiczNavindra P. SeeramYanjun Zhang
    • C07H15/244A61K31/122A61K31/21A61K31/70A61K31/704A61P33/10A61P33/12C07C50/34C07C50/38C07C66/02C07C69/157A01N43/04A01N37/00
    • A61K31/70A61K31/21C07C50/38Y02A50/423
    • Anthraquinones are described which have anticancer or antitumor activity and which are useful for inhibiting cancer cells and cells comprising tumors in vitro or in vivo. Preferably, the anthraquinones have the chemical formula: wherein R1 is selected from the group consisting of hydrogen, alkyl, and substituted alkyl; R2 is a group containing 1-12 carbons selected from the group consisting of alkyl, substituted alkyl, aldehyde, hydroxy, hydroxymethyl, acid group, carbohydrate and combinations thereof; and R3 is a group containing 1 to 12 carbons selected from the group consisting of methyl, alkyl, substituted alkyl, aldehyde, hydroxy, hydroxymethyl, acid group, carbohydrate, and combinations thereof. The preferred anthraquinones are 1-hydroxy-2-acetyl-3,6-methyl anthraquinone, 2-acetyl-3,6-methyl anthraquinone monoacetate, 1-hydroxy-2-acetyl-3,7-methyl anthraquinone, 2-acetyl-3,7-methyl anthraquinone monoacetate, 1,2,8-trihydroxy-3-methyl anthraquinone, 1,8-dihydroxy-2-O-β-D-glucopyranoside anthraquinone, 1,2,8-trihydroxy-3-hydroxymethyl anthraquinone, and 1,8-dihydroxy-3-carboxy anthraquinone.
    • 描述了具有抗癌或抗肿瘤活性的蒽醌,其可用于在体外或体内抑制癌细胞和包含肿瘤的细胞。 优选地,蒽醌具有以下化学式:其中R 1选自氢,烷基和取代的烷基; R2是含有选自烷基,取代的烷基,醛,羟基,羟甲基,酸基,碳水化合物及其组合的1-12个碳的基团; 并且R 3是选自甲基,烷基,取代的烷基,醛,羟基,羟甲基,酸基,碳水化合物及其组合中的1至12个碳的基团。 优选的蒽醌是1-羟基-2-乙酰基-3,6-甲基蒽醌,2-乙酰基-3,6-甲基蒽醌单乙酸酯,1-羟基-2-乙酰基-3,7-甲基蒽醌,2-乙酰基 - 3,7-甲基蒽醌单乙酸酯,1,2,8-三羟基-3-甲基蒽醌,1,8-二羟基-2-O-β-D-吡喃葡萄糖苷蒽醌,1,2,8-三羟基-3-羟甲基蒽醌 ,和1,8-二羟基-3-羧基蒽醌。