CN86106200A - 用油菜甾醇内酯衍生物提高谷物产量 - Google Patents
用油菜甾醇内酯衍生物提高谷物产量 Download PDFInfo
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- 238000000034 method Methods 0.000 claims abstract description 7
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- 229910052739 hydrogen Inorganic materials 0.000 claims abstract 5
- 239000001257 hydrogen Substances 0.000 claims abstract 5
- 150000001875 compounds Chemical class 0.000 claims description 16
- 125000002777 acetyl group Chemical group [H]C([H])([H])C(*)=O 0.000 claims description 9
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- 150000001646 brassinolides Chemical class 0.000 claims description 2
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J73/00—Steroids in which the cyclopenta[a]hydrophenanthrene skeleton has been modified by substitution of one or two carbon atoms by hetero atoms
- C07J73/001—Steroids in which the cyclopenta[a]hydrophenanthrene skeleton has been modified by substitution of one or two carbon atoms by hetero atoms by one hetero atom
- C07J73/003—Steroids in which the cyclopenta[a]hydrophenanthrene skeleton has been modified by substitution of one or two carbon atoms by hetero atoms by one hetero atom by oxygen as hetero atom
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- A—HUMAN NECESSITIES
- A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
- A01N—PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
- A01N49/00—Biocides, pest repellants or attractants, or plant growth regulators, containing compounds containing the group, wherein m+n>=1, both X together may also mean —Y— or a direct carbon-to-carbon bond, and the carbon atoms marked with an asterisk are not part of any ring system other than that which may be formed by the atoms X, the carbon atoms in square brackets being part of any acyclic or cyclic structure, or the group, wherein A means a carbon atom or Y, n>=0, and not more than one of these carbon atoms being a member of the same ring system, e.g. juvenile insect hormones or mimics thereof
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- Agronomy & Crop Science (AREA)
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- Wood Science & Technology (AREA)
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Abstract
本发明为一种提高谷物产量的组合物,其中包括
Description
本发明是关于具有促进植物生长作用的油菜甾醇内酯(brassinolide)衍生物的应用,或更具体地说是,关于含有该衍生物作为活性组份的组合物为提高谷类产量的应用和使用该衍生物提高谷物产量的方法。
事实上,已经知道油菜甾醇内酯衍生物具有促进植物生长的作用,例如,由KAGAKU Vol.39 No2,pp.129-131(1984)和日本专利公开58-90578公布的。也已经知道,在水果开花期,通过喷撒例如植物生长素、赤霉素或细胞激动素类植物激素促进结实和采收无籽葡萄。
由于世界人口的增长,为提高农作物产量,特别是例如水稻,小麦和玉米等主要农作物的产量进行了大力的研究。在这些研究中,包括应用油菜甾醇内酯衍生物(近来的研究结果)和植物激素来提高农作物产量的试验,但是,还没有任何对谷类显著有效的报告。
本发明的目的是有效地提高主要农作物特别是谷类的产量。
本发明的发明人充分地研究了提高谷类产量和被认为是具有植物生长作用的油菜甾醇内酯衍生物的生理活性作用之间的关系。
经研究,发明人发现如果至少一种选自通式(Ⅰ)和(Ⅱ)的油菜甾醇内酯衍生物,应用于种子期、种子刚刚发芽到5叶期,或开花期前后,该谷物的产量会显著提高。因此,发明人实现了本发明的目的。
其中R代表氢原子或乙酰基。
由通式(Ⅰ)和(Ⅱ)表示的本发明的油菜甾醇内酯可由例如日本专利公开No60-139685叙述的方法制备,作为这种化合物的实例可以叙述如下:
(22R,23R,24R)-2α,3α,22,23-四羟基-B-高-7-氧杂-5α-麦角甾烷-6-酮
熔点:256~257℃(文献:256~257℃)
EI-MSm/z:465(M+-15),462(M+-18),447,409,380(M+-101,C22-C23裂解+H,基峰),379,361,350,343,331,325,322,313,307,303,285,177,173,155,131,101,71,43。
发射体CI-MS(异丁烷)m/z:481(M++1,基峰),463,445。
1H-NMR(CDCl3)δ:
0.69(3H,s,18-H3)
1.98(3H,s,乙酰基)
2.02(6H,s,2乙酰基)
2.09(3H,s,乙酰基)
3.00(1H,dd,J=13和6Hz,5α-H)
4.07(2H,m,7-H2)
4.07~5.50(4H,m,2-H,3-H,22-H和23-H)
(试验样品为四乙酸酯)
元素分析:
C(%) H(%)
测定值:70.01 9.92
计算值:70.03 9.85
(C28H48O6)
和它的乙酰衍生物,例如,四乙酸酯。
(22S,23S,24S)-2α,3α,22,23-四羟基-B-高-7-氧杂-5α-麦角甾烷-6-酮
熔点:193~195℃(文献193~195℃)
EL-MSm/z:465(M+-15),465(M+-18),447,409,380,379,361,350,343,331,325,322,313,307,285,177,173,155,131,101,71,43。
发射体-CI-MS(异丁烷)m/z:841(M++1,基峰),463,445。
1H-NMR(CDCl3)δ:
0.67(3H,s,18-H3)
1.93(3H,s,乙酰基)
2.03(9H,s,3乙酰基)
3.00(1H,dd,J=13和6Hz,5α-H)
4.07(2H,m,7-H2)
4.50~5.50(4H,m,2-H,3-H,22-H和23-H)
(试验样品为四乙酸酯)
元素分析:
C(%) H(%)
测定值:69.88 9.87
计算值:70.03 9.85
(C28H48O6)
和它的乙酰衍生物,例如,四乙酸酯。根据本发明,通式(Ⅰ)和通式(Ⅱ)的油菜甾醇内酯衍生物用水稀积成低浓度使用,既可单独使用也可两种或多种这类衍生物混合使用。另一方面,可以用通常的农业化学加工方法,使其与辅剂混合制成制剂,例如粉剂、颗粒剂、可湿性粉剂、可流动悬浮剂和浓乳剂以提高和稳定该衍生物的作用。
这样的辅剂包括载体(稀积剂)和其他辅剂例如展布剂,乳化剂,湿润剂,分散剂,固定剂和分解剂(disintegrator)。
液体载体可以是芳香烃例如甲苯和二甲苯,醇例如甲醇、丁醇和乙二醇,酮例如丙酮,酰胺例如二甲基甲酰胺,亚砜例如二甲基亚砜,甲基萘,环己烷,动物和植物油,脂肪酸及其酯等等。
固体载体有粘土、高岭土、滑石、硅藻土、硅石、碳酸钙、蒙脱土、膨润土、长石、石英、氧化铝、木屑等等。
一般使用的乳化剂或分散剂是表面活性剂,包括阴离子、阳离子、非离子和两性的表面活性剂例如高级烷基硫酸钠,十八烷基三甲基氯化铵,聚氧乙烯烷基苯基醚,十二烷基甜菜碱等等。
在使用这些载体的情况中,仔细地推敲是特别重要的,应采用最适于促进油菜甾醇内酯衍生物效果的那些载体。
这些制剂的任意一种不仅可以单独施用,而且还可以与杀菌剂、杀虫剂、植物生长调节剂、杀螨剂、园艺农药、土壤消毒剂、土壤改良剂或杀线虫剂混合施用,而且还可再与化肥和其他除草剂结合施用。
为提高谷类的产量,油菜甾醇内酯衍生物作为活性成分在组合物中的含量可随制剂种类,施用方法和其他条件而变化,一般地,其含量为0.01-95%(重量),最好为0.01-50%(重量),但是有时可以单独施用活性化合物。
本发明中的术语“谷类”的意思和“乔木科植物”,“粮食作物”等等相同;“谷类”包括水稻,玉米,小麦,大麦,燕麦等等。
本发明中的术语“施用”包括“撒布”,“喷雾”,“喷淋”或“浸泡”。
已明显证明,本发明中应用的油菜甾醇内酯衍生物有提高作物产量的作用,即使用量很少。施用量一般为0.00001到100毫克,最好为0.01到10毫克。当作为水或有机溶剂溶液或分散液施用时,0.0001到10ppm最好。施用时,撒布在茎和叶包括花和穗上特别好。
当施用本发明的组合物提高谷类产量时,在农作物大约开花期进行是重要的。这里使用的短语“大约开花期”是指从再生细胞形成开始到完成受精种子成熟的周期。以水稻为例,该周期是从稻穗灌浆到穗中最后谷粒花完成受精之后。
从再生细胞形成到种子受精完成这段时间,植物体中营养素或能量转移或释放到再生细胞或种子中是非常活跃的。为了调节这一过程,各种各样的物质例如植物激素也直接参与。如果这种转移和释放可以进一步活化并增加成熟种子的话,那么,最终可以提高作物的产量。
而且,从卵细胞和精子细胞的形成到受精的周期是特别适合于对再生细胞直接发生影响的时期。开花和受精期是再生细胞直接暴露于环境的时期,因此它们对甚至极少量的活性化合物的影响都是非常敏感的。
发明人指出,对于收获种子的那些作物来说,例如谷类,这个时期与大大提高产量密切有关,并发现当撒布通式(Ⅰ)和(Ⅱ)的油菜甾醇内酯衍生物时,提高作物产量的作用很大。本发明的油菜甾醇内酯衍生物具有植物激素例如,吲哚-乙酸,赤酶素、细胞激动素等促进细胞扩张的作用。
本发明的另一个特征是在开花期施药,即使极少量的单独施用(撒布),也可大大增加作物产量。
当要提高谷类产量时,种子发芽后到5叶期得到良好的生长是特别重要的,这时期,作物的生长对周围环境条件非常敏感。
业已发现,在此期间用少量油菜甾醇内酯衍生物浸泡种子、处理根部、处理茎等,可大大促进作物生长。
根据本发明,一些作物例如,水稻,小麦和玉米的产量增加可达2-37%。
本发明将由下面的制剂实例进一步详细说明。其中辅剂的种类和混合比例不受限制,而且使用范围很广。实例中的“份”是指重量份。
制剂实例1:乳剂
35份二甲苯和甲基萘(1∶1)的混合物加到25份化合物[Ⅲ]和25份化合物[Ⅳ]的混合物中形成溶液,形成的溶液再同15份聚氧乙烯烷基苯基醚和烷基苯磺酸钙(8∶2)的混合物混合,得到乳剂。
制剂实例2:粉剂
5份化合物[Ⅳ]同95份粘土混合并研磨,得到粉剂。
制剂实例3:可湿性粉剂
1份化合物[Ⅳ]与作为载体的10份硅藻土和71份高岭土混合,再与18份十二烷基硫酸钠和2,2-二萘基甲磺酸钠的混合物均匀混合,然后精细地研磨得到可湿性粉剂。
制剂实例4:颗粒剂
在适当的混合器中,用1.5份聚乙酸乙烯酯的甲醇溶液作粘合剂,把0.01份化合物[Ⅲ]的精细粉剂撒布和涂敷在98.4份硅石粒上(16到32筛目)得到颗粒剂。
试验实例1:
1/5000的瓦格钠盆(Wagner)用农田土填满,施肥以后,在其中播种10粒小麦种子。在2到3叶阶段间苗,每盆各5棵,在开花阶段,用表1所列浓度的溶液以5毫升/盆喷洒处理,这些溶液由含有1%油菜甾醇内酯衍生物的可湿性粉剂制得。
正如表1所示,在0.001到1ppm时,穗重增加是2到33%,这一重量比未处理小麦高得多。
表1 对小麦穗重的影响
试验化合物 浓度 穗重(同未处理地 种子重量(与未处理
(ppm) 块比)克/穗 地块比)克/穗
0.001 1.37(126) 1.07(130)
Ⅲ 0.01 1.43(132) 1.04(127)
0.1 1.39(128) 1.12(137)
1 1.35(125) 1.03(126)
0.001 1.11(102) 0.85(104)
Ⅳ 0.01 1.26(116) 1.00(122)
0.1 1.44(133) 1.12(137)
1 1.31(121) 1.01(123)
未处理 1.08(100) 0.82(100)
试验实例2:对玉米种子的影响
玉米(Honey Bantam)6月7日播种,在它的雌性穗丝长出时,分别用0.01,0.1,和1ppm的化学式[Ⅲ]和[Ⅳ]的化合物按1000升/公顷[各自加展布剂(按1000倍重量)]喷洒处理。
处理后约第43天,收割,测量颗粒穗总长度和不育穗的最长部分。正如表2所示结果,不育穗部分同未处理的玉米相比较减少约一半,因此,果实变得更好。
表2 油菜甾醇内酯衍生物对玉米的影响
(*按单类方差分析法处理数据,5%有效。)
化合物 浓度ppm 总长cm 不育部分cm 不育部分与总长
之比%
0.01 19.2 2.0* 10.5
Ⅲ 0.1 20.1 1.6* 8.2
1 19.6 1.9* 9.9
0.01 20.4 2.4* 11.5
Ⅳ 0.1 19.8 1.6* 8.2
1 18.7 1.2* 6.0
对照 - 19.3 3.2 16.6
试验实例3:
于室温下,按0.01ppm配料浓度,把稻种(品种:Nihonbare)浸于化学式[Ⅲ]的油菜甾醇内酯衍生物和稀积1000倍的Benlate T溶液的混合溶液中约24小时,然后用水洗涤并浸在水中约24小时。发芽后,把种子种到育苗盆里的颗粒土壤中,用相同的土盖上并放在发芽容器内约2天。取出后,使它们变成绿色,然后在12℃~17℃~22℃的空调室内栽培,生长21天后,分别测定植物的高度和茎干、根及稻谷的干重。
结果如表3所示,植物的高度,以及地面上茎干和根的干重都增加了,因此,在12到22℃低温下用化学式[Ⅲ]的油菜甾醇内酯衍生物处理后生长良好。
表3 浸泡稻种对稻谷早期生长的影响
干重(mg)
化合物 浓度ppm 植物高cm 茎干 根 稻谷
[Ⅲ] 0.1 19.6 274.0 9.0 7.0
未处理 - 19.0 228.0 7.4 7.4
试验实例4
稻种(CV:Nihonbare)于室温下在浓度分别为1,1和0.1ppm的化合物(Ⅲ),(Ⅳ)和(Ⅲ)的四乙酸酯与稀释200倍的Benlate溶液的混合液中浸泡约24小时。然后,用水洗涤和浸渍,芽长到1到2毫米时,在室外的每个混凝土盒(50厘米×50厘米)中播种30粒,30天后观察芽的数目(在4月20日排水1厘米,并用水浸没5厘米深以便栽培)。
如表4所示,处理过的发芽情况都优于未处理的。
表4 对水稻直接排水的影响
化合物 浓度(ppm) 发芽率(%)
Ⅲ 1.0 40.0
Ⅳ 1.0 55.0
[Ⅲ]的四乙酸酯 0.1 54.5
未处理 - 18.3
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US6063731A (en) * | 1999-03-30 | 2000-05-16 | Agritope, Inc. | Brassinosteroid analogs useful as plant growth regulators |
US6239073B1 (en) | 1999-03-30 | 2001-05-29 | Exelixis Plant Sciences, Inc. | Brassinosteroid analogs useful as plant growth regulators |
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US4346226A (en) * | 1980-08-28 | 1982-08-24 | The United States Of America As Represented By The Secretary Of The Department Of Agriculture | Plant growth promoting brassinosteroids |
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NO863598L (no) | 1987-03-20 |
US4767442A (en) | 1988-08-30 |
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CA1282976C (en) | 1991-04-16 |
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BR8604476A (pt) | 1987-05-19 |
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