CN101518250B - Camptothecin plant molluscacide and preparation and application method thereof - Google Patents
Camptothecin plant molluscacide and preparation and application method thereof Download PDFInfo
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- CN101518250B CN101518250B CN2009100615274A CN200910061527A CN101518250B CN 101518250 B CN101518250 B CN 101518250B CN 2009100615274 A CN2009100615274 A CN 2009100615274A CN 200910061527 A CN200910061527 A CN 200910061527A CN 101518250 B CN101518250 B CN 101518250B
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- molluscacide
- camptothecine
- camptothecin
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Abstract
The invention provides a camptothecin plant molluscacide and a preparation and application method thereof. The crystalline powder of the camptothecin is prepared into 0.05-0.1g/L of molluscacide aqueous solution and molluscacide pelletized granule with camptothecin content of 0.25-0.30 percent. The camptothecin plant molluscacide is pure chemical component and meets the requirement of environmental protection, and the oncomelania control effect of the Camptothecin plant molluscacide can be evaluate in a standardized way; and the invention has good effect of expelling and killing the oncomelania and also has the advantages of simple manufacturing process, lower cost, convenient storage and transportation, no pollution to the environment, no harm to human, animals and fish and obvious economic benefit, social benefit and ecological benefit.
Description
Technical field
The present invention relates to a kind of camptothecin plant molluscacide and methods for making and using same thereof that is used for killing oncomelania.
Background technology
Schistosomiasis is the healthy disease of serious harm human body.Oncomelania is an indispensable link in the schistosomiasis propagation, and the spiral shell that goes out can reduce the propagation of schistosomiasis effectively.At present, snail-killing method roughly has three kinds: the manual work spiral shell that goes out, chemicals spiral shell and the biology spiral shell that goes out that goes out.The manual work time-consuming expense of spiral shell of going out is high, and the chemicals spiral shell that goes out costs an arm and a leg, and the term of validity is of short duration, and is how toxic to people, animal, fish etc., is prone to cause environmental pollution.
For fear of the pollution of chemicals molluscacide to environment, people seek out the pure natural plants snail killing agent always.The plant snail killing agents such as the plain molluscacide of rhizome powder molluscacide, Jatropha curcas of dioscorea zingiberensis wright have been found at present.Above-mentioned plant snail killing agent is mostly with the powder of plant or with the mixture composition of the plant extract spiral shell that goes out, effect can not be carried out the standardization evaluation, is difficult to approved in the world.
Camplotheca acuminata [Camptotheca acuminata Decne.] is a kind of deciduous tree, up to 30m, and leaf alternate, the florescence 7-8 month; The fruit phase 11-12 month.The leaf of this plant, bark, Gen Pi and fruit can be controlled furuncle, sore carbuncle, trichophytosis, also can try to control various cancers, the diseases such as hepatosplenomegaly that acute and chronic leukemia and schistosomiasis cause.Camplotheca acuminata is a kind of special product plant of China.On the south main distribution China Qinling Mountains.Cultivate in the roadside or the flower garden more.China widely cultivates in the schistosomiasis epidemic-stricken area.Resource is very abundant.Find that after deliberation camplotheca acuminata active ingredient has very strong toxic action to oncomelania, confirm that camptothecine wherein is one of the active component of spiral shell that mainly goes out.Utilize this new purposes of plant camptotheca acuminata alkali not appear in the newspapers always.
Summary of the invention
The objective of the invention is to utilize the toxic action of plant camptotheca acuminata alkali to oncomelania, proposing a kind of is plant molluscacide and preparation technology's and methods for using them thereof of raw material with the camptothecine.
The camptothecine that the present invention uses is a kind of camplotheca acuminata fresh leaf before full-bloom stage, adopts pulverizing--alcohol immersion--ethanol to reclaim the camptothecine that an organic solvent chloroform extraction crystallisation extracts.Perhaps use commercially available (content＞95%) camptothecine.
Camptothecine is a light yellow crystalline powder, mp 264-266 ℃, little have draw moistly, see that light is perishable, water insoluble, dissolve in ethanol, chloroform, meet the concentrated sulfuric acid and promptly show yellow green, thin up then produces green fluorescence.Be dissolved in the ethanol and can show hyacinthine fluorescence.
One, the preparation of the camptothecin plant molluscacide aqueous solution:
Weighing camptothecine crystalline powder, the dissolve with ethanol with 1-1.5 times of 75% concentration adds entry again, is mixed with the aqueous solution of 0.05-0.1g/L concentration.
Two, the camptothecin plant preparation of spiral shell granule of going out:
1, weighing camptothecine crystalline powder 0.1-0.15kg,
2, with the 1-1.5 dissolve with ethanol of 75% concentration doubly,
3, be 4.5: 40.8: 4.5 Icing Sugar by weight proportion: flour: the fine powder of gum Arabic mixes into mixed powder,
4, with camptothecine crystalline powder ethanolic solution and mixed powder by weight 0.2-0.3% mixing stirring, the clear water that adds 3-5% again stirs,
5, grow into 0.8-1cm with the oodle maker compacting of the transformation of the way then, the footpath is the oval cylindrical particle of 0.2-0.4cm, to 70-90 ℃, is incubated 10-15 minute with heating using microwave, and being drying to obtain camptothecine content is the camptothecine particle molluscacide of 0.25-0.30% specification.
The camptothecine molluscacide has very strong killing action to oncomelania, and concentration is the aqueous solution processing time of 0.05g/L-0.8g/L to reach 3～5 days, and its dead spiral shell rate can reach 95.5%～100%; Toxic action increases with the increase of treatment fluid concentration and the prolongation in processing time, and has obvious seasonal difference; Summer, toxic action was the strongest, and spring, autumn take second place, and toxic action is little during winter oncomelania dormancy; Its toxic action mechanism is that oncomelania is caused oncomelania head, neck, foot and hepar damnification, and liver function is reduced; Responsive to the reaction of oncomelania esterase: enzymic activity changes the Changing Pattern that is " strengthening-weaken-disappear ".Oncomelania is poisoned early stage, the expression of medicine irritation EST, and the detoxification ability of enhancing oncomelania liver, enzyme is lived and is raise; Oncomelania is poisoned the middle and later periods, because drug treating time or intensity surpass its physiology threshold, the synthetic of enzyme is suppressed, and enzyme is lived and descended, until complete obiteration.
The present invention in the schistosomiasis epidemic-stricken area oncomelania multiply the go out application of spiral shell of region.
1) soak method extremely: be applicable to the shallow water area that can control water level, multiply the place like oncomelanias such as irrigation canals and ditches, small reservoir, rice fields, camptothecine particle molluscacide spreading is soaked oncomelania extremely in water, concentration is controlled at the 0.05g/L-0.8g/L scope.
2) broadcast sowing method: by per hectare 100kg amount spreading, mortality of snails can reach 100% after 3 days with camptothecine particle molluscacide.
In sum, utilize the camptothecine particle molluscacide spiral shell that goes out, have following advantage:
1, aboundresources: camplotheca acuminata is a kind of special product plant of China, and subtropical zone on the south China Qinling Mountains mainly distributes.Cultivate in the roadside more, Jiang Tan or flower garden.China widely cultivates in the schistosomiasis epidemic-stricken area.Resource is very abundant.Resource is very abundant; Seminal propagation, growth is fast, and output is high, can scale cultivate, and camptothecine content is higher, and dry product content can reach more than 0.07%, does not have the problem of product development raw material difficulty; Be the famous Chinese herbal medicine of China, can control furuncle, sore carbuncle, trichophytosis, also can try to control various cancers, the diseases such as hepatosplenomegaly that acute and chronic leukemia and schistosomiasis cause, economic worth is big, also has to view and admire, afforest, conserve water and soil and other comprehensive benefits.
2, production equipment is simple and easy: the camptothecine production technology is easy, and production equipment and operation all do not have specific (special) requirements, production process environmentally safe; Be fit to the commercialization running, be particularly suitable for the various places medium-sized and small enterprises and utilize plant resources production on the spot.
3, easy to use: this product is convenient to store, transportation, according to actual sight, can spread, and also can soak and kill, and is extremely easy to use.Pure Phytochemistry composition, sn ail control effect are easy to carry out the standardization evaluation.
4, compliance with environmental protection requirements: this product sn ail control effect is continual and steady, and environmentally safe is to people and animals and fish nonhazardous, compliance with environmental protection requirements.
5, with low cost: this product integrated cost is lower than the chemistry spiral shell preparation that goes out, and economic benefit, social benefit, ecological benefits are obvious.
Embodiment
Embodiment 1
Get the camplotheca acuminata fresh leaf 150kg before the full-bloom stage, adopt and pulverize--alcohol immersion--ethanol recovery--the camptothecine 0.11kg that organic solvent chloroform extraction crystallisation extracts, through prepare camptothecine particle molluscacide 55.5kg.
Embodiment 2
Get the camplotheca acuminata fresh leaf 1000kg before the full-bloom stage, adopt and pulverize--alcohol immersion--ethanol recovery--the camptothecine 0.7kg that organic solvent chloroform extraction crystallisation extracts, through prepare camptothecine particle molluscacide 345.7kg.
The application implementation example is referring to annex 1, to the influences of fish referring to annex 2.
Annex 1: the test report of snail killing test of the present invention (retrial)
Infusion method is adopted in experiment.Experiment is controlled under 23 ± 1 ℃ of conditions in temperature to be carried out.Getting 100 on oncomelania alive is one group, in per 20 nylon net bags of packing into, respectively each group (5 bags every group) oncomelania is immersed in the glass jar of the camptothecine aqueous solution that fills the 1000g variable concentrations, and other establishes the niclosamidum aqueous solution and no chlorine clear water contrast.Behind processing 1,2,3,4,5d, the oncomelania in each processing is taken out 1 bag at random, use no chlorine water flushing for several times, put into clear water again and leave standstill 1d, work is survived and checked then: open the operculum scrambler and be the spiral shell of living, the method for unloading thorn is broken and dissected to the usefulness of remainder into pieces, discriminating life or death.Experiment repetition 3 times is got its mean value as experimental result (seeing table 1-4).
1 camplotheca acuminata total alkali activity against snails
Table 1 sn ail control effect of the present invention
2 significance analysis
Significance analysis: analyze between the variable concentrations variance between the different time, degree of freedom, equal sides, significance. with the statistica of statistical software analysis result such as table 2:
Table 2 concentration and time statistic analysis result
Can know that by the result significance of concentration and time is respectively 0.000001 and 0.000018, and is remarkable for extremely, explain between variable concentrations and the different time to have significant difference.Test the back average relatively:
3 test back average check analysis result
Know by significance analysis, have significant difference between concentration and the concentration, test back average check as concentration, like table 3:
Table 3 concentration is tested back average check
In like manner, also there is significant difference between time and time, tests back average check as the time, like table 4:
Table 4 time is tested back average check
The back average of testing through between concentration relatively draws, the concentration of 50mg/L and no chlorine water, and chlorine nitre willow ammonia, there is significant difference in 400mg/L between 800mg/L; 100mg/L concentration and no chlorine water, there is significant difference in chlorine nitre willow ammonia between 800mg/L concentration; There are significant difference in 200mg/L concentration and no chlorine water between chlorine nitre willow ammonia.
The back average of testing through the time relatively draws, and handles 24h and handles 72h, has significant difference between the 96h, handles 48h and handle between 96h to have significant difference.
The aqueous solution of the present invention with variable concentrations is handled oncomelania, and under the processing of different time, mortality of snails there are differences.Its rule is that mortality of snails is in rising trend with the increase of handling concentration.0.05g/L-0.8g/L the above camptothecine aqueous solution has 100% obvious poisoning oncomelania lethal effect, even under very low concentration (0.05g/L-0.10g/L) is handled, also can reach the effect of poisoning with poison more than 30%; The camptothecine aqueous solution with the above concentration of 1.0g/L is handled oncomelania 2d, just can reach 100% killing effect.
Niclosamidum is the chemical molluscacide that generally uses.Sn ail control effect of the present invention is contrasted with it, can know that the aqueous solution of the present invention of 0.80g/L is suitable with the sn ail control effect of 0.0005g/L niclosamidum solution approximately.Drug effect but of the present invention is slightly slow than niclosamidum.2-3d can reach 100% lethality with 0.0005g/L niclosamidum solution-treated oncomelania, needs 4-5d just can reach same effect with the aqueous solution processing of the present invention of 0.80g/L.
Annex 2: toxicity test of fishes of the present invention
1, the acute toxicity testing of fish
Fry (crucian and carp) is put into the aqueous solution of the present invention of four concentration (0.05g/L, 0.10g/L, 0.20g/L, 0.40g/L); Observe the reaction of fry every day; No abnormal phenomenon takes place, and it is also very brisk to move about, and the statistics fry does not have death after 72 hours; After observing 48 hours again, the still no abnormal and phenomena of mortality.
2, the long term toxicity test of fish
Two kinds of fries of buy (carp and crucian) are put into four concentration of the present invention (0.05g/L, 0.10g/L, 0.20g/L, 0.40g/L) and the processing that clear water contrasts, measure the body length of fish, the body weight of title fish after 30 days respectively, carry out statistical analysis.Gained data and statistical analysis see the following form:
Table 5 young crucian is raised the body
after 30 days
The variance analysis of the young crucian body weight of table 6 control group and processed group
Can know F＜F from above variance analysis
0.05, F＜F
0.01, the body weight of control group and each concentration group feeding fish does not have significant difference, and the visible aqueous solution of the present invention does not make significant difference to the body weight gain of crucian.
Table 7 young crucian is raised the body long (cm) after 30 days
The variance analysis that table 4 control group and processed group young crucian body are long
Above variance analysis can be known, F＜F
0.05, F＜F
0.01, the long no significant difference of the young crucian body of processed group and control group, the aqueous solution of the present invention that is to say four concentration does not make significant difference to the growth of young crucian yet.
Raising to the carp fry in the aqueous solution of the present invention of above-mentioned four concentration does not make significant difference yet.
Through experimental data and variance analysis, the result shows: in the variable concentrations the present invention who oncomelania is had strong killing effect, raise crucian and carp after one month, growing of carp and young crucian all do not made significant difference.
Claims (3)
1. a camptothecin plant molluscacide it is characterized in that molluscacide is that camptothecine concentration is the aqueous solution of 0.05-0.1g/L, or camptothecine content is the camptothecine particle molluscacide of 0.25-0.30% specification.
2. the compound method of a camptothecin plant molluscacide aqueous solution is characterized in that, weighing camptothecine crystalline powder, and the dissolve with ethanol with 1-1.5 times of 75% concentration adds entry again, is mixed with the aqueous solution of 0.05-0.1g/L concentration.
3. the camptothecin plant compound method of spiral shell granule of going out is characterized in that preparation steps is:
1), weighing camptothecine crystalline powder 0.1-0.15kg,
2), with the 1-1.5 dissolve with ethanol of 75% concentration doubly,
3) be 4.5: 40.8: 4.5 Icing Sugar, by weight proportion: flour: the fine powder of gum Arabic mixes into mixed powder,
4), with camptothecine crystalline powder ethanolic solution and mixed powder by weight 0.2-0.3% mixing stirring, the clear water that adds 3-5% again stirs,
5) suppress with the oodle maker of the transformation of the way, then and grow into 0.8-1cm, the footpath is the oval cylindrical particle of 0.2-0.4cm, to 70-90 ℃, is incubated 10-15 minute with heating using microwave, and being drying to obtain camptothecine content is the camptothecine particle molluscacide of 0.25-0.30% specification.
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| CN101518250B true CN101518250B (en) | 2012-03-28 |
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Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1373131A (en) * | 2002-03-18 | 2002-10-09 | 浙江大学 | Process and apparatus for extracting and separating high-purity monomolecular camptothecine |
| WO2007110637A1 (en) * | 2006-03-28 | 2007-10-04 | Bioniqs Limited | Method for extracting target alkaloid using an ionic liquid as extracting solvent |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1373131A (en) * | 2002-03-18 | 2002-10-09 | 浙江大学 | Process and apparatus for extracting and separating high-purity monomolecular camptothecine |
| WO2007110637A1 (en) * | 2006-03-28 | 2007-10-04 | Bioniqs Limited | Method for extracting target alkaloid using an ionic liquid as extracting solvent |
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