求高手翻译一篇农药化学文章(重奖)
Furofuranlignanscomprisealargegroupofnaturalproductscharacterizedbycouplingoftwopheny...
Furofuran lignans comprise a large group of natural
products characterized by coupling of two phenylpropane
(C6-C3) units. They are among the largest subclass of
lignans with a wide range of biological activities such as
antitumor, antimitotic, antimicrobial, and antioxidative.1
The majority of furofuran lignans have 2,6-diaryl substituents
on the exo face of the bicyclic skeleton (e.g., sesamin
1), although those with endo, exo aryl substitution (e.g.,
asarinin 2) and others with endo, endo substitution are also
known.2 Sesamin (1), which can be extracted exclusively
from sesame in large quantities, is intriguing due to its
highly efficient antioxidant activity.3 It was also reported
that sesamin is a specific inhibitor of ¢5-desaturase, which
catalyzes the conversion of dihomo-ç-linolenic acid to
arachidonic acid, in both microorganisms and animals,4 and
sesamin also exerts hypocholesterolemic activity through
the inhibition of cholesterol absorption and synthesis.5 The
other report indicated that sesamin prevented liver damage
caused by alcohol or carbon tetrachloride and showed a
suppressive effect against 7,12-dimethylbenz[a]anthraceneinduced
rat mammary carcinogenesis and antihypertensive
effects.6 Asarinin has also been shown to have several
significant biological activities, including antitumor promotion,
antiallergic activity, and enhancement of the toxicity
of certain insecticides.7,8
The radix of Asarum heterotropoides Fr. var. mandshuricum
Kitag. (Xixin) is a traditional herbal medicine listed
officially in the Chinese Pharmacopoeia and used as an
analgesic, antitussive agent, and expectorant for treatment
of influenza, headache, rheumatic pain, and asthma. It is
also used as a drug for invigorating blood circulation and
eliminating blood stasis.9 Furofuran lignans have been
reported to be widely contained in this plant.10 In our
processes of the isolation of sesamin and asarinin previously,
different amounts of 1 and 2 were obtained due to
different extraction methods, e.g., soaking at room temperature
or vacuum distillation. Several reports also
indicated that sesamin epimerized to asarinin during acidcatalyzed
conditions. Given the varied biological activities
displayed by these two furofuran lignans and their interesting
conformational behavior, a more in-depth study on
the epimerization process was undertaken.
Both sesamin (1) and asarinin (2) have a furofuran
backbone, which is similar to those of norbornane and
bicyclo[3.3.0]octane. It is well-known that the exo isomer
is more stable than the endo isomer. Sesamin has two
substituents in exo positions, and asarinin has one substituent
in exo and the other in endo position (Figure 1).
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products characterized by coupling of two phenylpropane
(C6-C3) units. They are among the largest subclass of
lignans with a wide range of biological activities such as
antitumor, antimitotic, antimicrobial, and antioxidative.1
The majority of furofuran lignans have 2,6-diaryl substituents
on the exo face of the bicyclic skeleton (e.g., sesamin
1), although those with endo, exo aryl substitution (e.g.,
asarinin 2) and others with endo, endo substitution are also
known.2 Sesamin (1), which can be extracted exclusively
from sesame in large quantities, is intriguing due to its
highly efficient antioxidant activity.3 It was also reported
that sesamin is a specific inhibitor of ¢5-desaturase, which
catalyzes the conversion of dihomo-ç-linolenic acid to
arachidonic acid, in both microorganisms and animals,4 and
sesamin also exerts hypocholesterolemic activity through
the inhibition of cholesterol absorption and synthesis.5 The
other report indicated that sesamin prevented liver damage
caused by alcohol or carbon tetrachloride and showed a
suppressive effect against 7,12-dimethylbenz[a]anthraceneinduced
rat mammary carcinogenesis and antihypertensive
effects.6 Asarinin has also been shown to have several
significant biological activities, including antitumor promotion,
antiallergic activity, and enhancement of the toxicity
of certain insecticides.7,8
The radix of Asarum heterotropoides Fr. var. mandshuricum
Kitag. (Xixin) is a traditional herbal medicine listed
officially in the Chinese Pharmacopoeia and used as an
analgesic, antitussive agent, and expectorant for treatment
of influenza, headache, rheumatic pain, and asthma. It is
also used as a drug for invigorating blood circulation and
eliminating blood stasis.9 Furofuran lignans have been
reported to be widely contained in this plant.10 In our
processes of the isolation of sesamin and asarinin previously,
different amounts of 1 and 2 were obtained due to
different extraction methods, e.g., soaking at room temperature
or vacuum distillation. Several reports also
indicated that sesamin epimerized to asarinin during acidcatalyzed
conditions. Given the varied biological activities
displayed by these two furofuran lignans and their interesting
conformational behavior, a more in-depth study on
the epimerization process was undertaken.
Both sesamin (1) and asarinin (2) have a furofuran
backbone, which is similar to those of norbornane and
bicyclo[3.3.0]octane. It is well-known that the exo isomer
is more stable than the endo isomer. Sesamin has two
substituents in exo positions, and asarinin has one substituent
in exo and the other in endo position (Figure 1).
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蜂胶天然木脂包含了一大批具有两个耦合苯基丙烷(C6-C3)单位的产品. 它们在最大的多种生物学活性木脂的亚纲之间,如抗癌、抗有丝分裂、抗菌和抗氧化.
1、有多数蜂胶木脂在挂式外观上的双环骨骼有取代2,6-二芳基,(如芝麻素1),虽然那些芳香挂式置换(例如 细辛素2)与其他置换,也是大家知道的。
2、芝麻素(1),可从大量芝麻中提取,它耐人寻味是因为它是高效活性抗氧剂.
3、另据报道,芝麻素食一种5-脱氢酶的特效抑制剂, 它能催化转化亚麻酸-ç-亚麻酸生成烯酸,备有微生物和动物都具备。
4、芝麻素也起到抑制胆固醇的吸收与合成从而降低胆固醇活性的作用.
5、其它报告表明芝麻素阻止肝脏因酒精或四氯化碳受损并且伴演抑制7.12甲蒽引起老鼠乳腺肿瘤和降压的效果.
6、细辛素也有几项生物学意义的活动,包括增强抗癌性,增强抗过敏活性、增强抗毒性。
7、8 细辛的根显效于.Fr. var. mandshuricum 碱蓬.
(欣)是一种传统草药正式列在在中国药典并且用作镇痛、镇咳剂、祛痰治疗、感、头痛、风湿痛、哮喘和活血化淤。
9、据报道,蜂胶已被广泛的栽培。
10 以前我们的过程孤立了芝麻与细辛,不同数量的1和2取决于提取方法的不同,例如,在室温下浸泡或真空蒸馏. 一些报告指出在酸性催化的条件下,芝麻素与细辛素可以形成(立体)异构体。由于不同的生物活性,这两个木脂蜂胶有趣的构像行为显示,要进行更为深入的异构研究.
(1)、细辛两芝麻(2)有蜂胶骨干,是类似于降莰烷和双环辛烷[3.3.0]. 这是众所周知的,外型异构比内异构体更为稳定. 芝麻素有两种外型取代的形式,而细辛素是一种在外型取代另一种在内位置取代(图1).
蜂胶天然木脂包含了一大批具有两个耦合苯基丙烷(C6-C3)单位的产品. 它们在最大的多种生物学活性木脂的亚纲之间,如抗癌、抗有丝分裂、抗菌和抗氧化.
1、有多数蜂胶木脂在挂式外观上的双环骨骼有取代2,6-二芳基,(如芝麻素1),虽然那些芳香挂式置换(例如 细辛素2)与其他置换,也是大家知道的。
2、芝麻素(1),可从大量芝麻中提取,它耐人寻味是因为它是高效活性抗氧剂.
3、另据报道,芝麻素食一种5-脱氢酶的特效抑制剂, 它能催化转化亚麻酸-ç-亚麻酸生成烯酸,备有微生物和动物都具备。
4、芝麻素也起到抑制胆固醇的吸收与合成从而降低胆固醇活性的作用.
5、其它报告表明芝麻素阻止肝脏因酒精或四氯化碳受损并且伴演抑制7.12甲蒽引起老鼠乳腺肿瘤和降压的效果.
6、细辛素也有几项生物学意义的活动,包括增强抗癌性,增强抗过敏活性、增强抗毒性。
7、8 细辛的根显效于.Fr. var. mandshuricum 碱蓬.
(欣)是一种传统草药正式列在在中国药典并且用作镇痛、镇咳剂、祛痰治疗、感、头痛、风湿痛、哮喘和活血化淤。
9、据报道,蜂胶已被广泛的栽培。
10 以前我们的过程孤立了芝麻与细辛,不同数量的1和2取决于提取方法的不同,例如,在室温下浸泡或真空蒸馏. 一些报告指出在酸性催化的条件下,芝麻素与细辛素可以形成(立体)异构体。由于不同的生物活性,这两个木脂蜂胶有趣的构像行为显示,要进行更为深入的异构研究.
(1)、细辛两芝麻(2)有蜂胶骨干,是类似于降莰烷和双环辛烷[3.3.0]. 这是众所周知的,外型异构比内异构体更为稳定. 芝麻素有两种外型取代的形式,而细辛素是一种在外型取代另一种在内位置取代(图1).
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