CN1879660A - A method for preparing novel chemical substance with anti-fertility and pain relieving activity - Google Patents

Abstract

The invention relates to a chemical component method, which uses the soluble (soluble protein) of ant as base material; uses alcohol extraction, to react via cotton cellulose, isatin, and acetate, to obtain new function. And the invention is characterized in that: said chemical solid is obtained by several chemicals, belonging to the organic composite chemical technique. And the traditional contraceptive drug is steroidal matter, to be used in women usually, with large side effect; and the analgesic has dependency and side effect on stomach and intestine system. And the invention is the contraceptive drug used by men, with less side effect and wider application.

Description

A kind of preparation method with antifertility and analgesic activity novel chemical substance

One, technical field

The organic chemicals of the new function that preparation method of the present invention obtained.Be with the insects toy, Polyhachis vicina Roger belongs to water solublity (hot water) material of Formica fusca, be basic material, after introducing special chemical group and carrying out structure of modification and modify, the macromolecular compound of the novel active that obtains, be protein-based organic chemicals, belong to the new innovation and creation of organic assembling chemical field.

Two, technical background

1, antifertility active function: antifertility is the topmost technical measures of fertility that realize a plan.Family planning is a fundamental state policy of China, although some countries in the world do not carry out the policy of family planning,, along with The development in society and economy, the minimizing day by day of nature of depending on for existence and development and social resources, the cost of surviving are constantly strengthening.Bear child less, become people's common recognition.Regulation and control fertilities is all kinsfolks' of society a side (bridegroom's or husband's side or the wife's side) thing that all must experience almost in the world.The existing method that obtains the family planning effect clinically is a lot, the art of pricking the hand extremely of medical contraception, semen deposition (ovum) pipe, last ring, condom etc., the method of each contraception or birth control, all exist some shortcoming and defect, medical contraception, with its contraceptive effect height, easy to use, simple, form the first-selection that adopts contraceptive device for people.Yet contraceptive brings damage to user.Mainly be very limited because of being used for male contraception medicine and method at present.Therefore, male contraception medicine and vaccine that research and development can be oral will obtain people's generally acceptance.

Women commonly used clinically now uses contraceptive, is steroidal substances and constitutes (property is paid plain and the progestogen compound recipe), all exists such problem, the side effect of fugitive contraceptive is less, use trouble, at the appointed time, must every day pills, if easily cause unexpected gestation (unwillingly gestation) after missing, life brings very big influence to physical and mental health, and long acting contraceptive, although can address this problem preferably, but long lasting women is bigger with the side effect of contraceptive.This is to use medicine to obtain contraceptive effect, need most the problem of solution, under the prerequisite that does not influence sexual function, resolve problem on the family planning technology aspect, only place in the development and application of male contraception medicine, could ideally resolve this problem, develop easy to use, side effect is little, definite effect, be easy to carry, the male contraceptive agent thing is pressing for of broad masses.

2, analgesic activities effect: analgesic is most widely used clinically general, the class common drug that use amount is huge.Pain is in clinical common a kind of disease.Result according to the statistics of the Department Of Health Services of various countries shows have the patient of history of pain to account for 35% of world's total population sum, and pain is divided into nerve centre pain and periphery pain by mechanism of action.By the strong and weak procedure division of pain, sharp pain, severe pain, dull pain, dull pain.Cause the slow property division of urgency of pain, be divided into acute pain and chronic pain or the like.Although pain is the early warning signal of numerous disease, can help people to find the state of an illness and the cause of disease, to etiological treatment,, when pain is serious, might cause temporary shock.Cause physiology operation disorder to suffering from pain person, anxious state of mind is having a strong impact on orthobiosis of pain patients.To treatment of pain sometimes also is very necessary.Moreover, some disease (such as: cancer, arthritis etc.) medically not finding effective medicine and method as yet, can only come relief of symptoms with medicine.Chang Yong analgesic can be divided into clinically: be representative and synthetic product thereof, opioid receptor agonist with the morphine and be the non-steroidal anti-inflammatory clearing away heat and alleviating pain medicine of representative with aspirin, be epoxidase (SOX), inhibitor, the opioid recdptor agonist, central pain had fine therapeutical effect, this type of medicine easily produces dependency and addiction, with causing abuse, brings serious harm to patient and society for a long time.Non-steroidal anti-inflammatory pain medicine, various chronic pains (periphery, pain) have better mitigation.This type of medicine, to the intestines and stomach and kidney, heart effectively is serious toxic and side effects, easily causes shortcomings such as gastric ulcer, gastrorrhagia.

Addiction, the dependency of the analgesic of its synthetic product of opiates, and the serious gastrointestinal side-effect of inhibitors of cyclooxygenases class analgesic, this is a kind of worldwide difficult medical problem.Thus, keeping on curative effect and the active basis, can not produce dependency, addiction, do not cause gastrointestinal tract, the toxic and side effects of kidney, cardiovascular aspect,, will produce the huge social benefit being subjected to the welcome of vast pain patients.

Three, summary of the invention

A kind of preparation method introduction with antifertility and analgesic activity novel substance has the prescription prescription and the preparation technology of the novel organic assembling chemical substance of special medicinal function, and synthesis step is introduced respectively:

Chemical substance prescription and proportioning:

1., clean dried Polyhachis vicina Roger belongs to 1 part of Formica fusca (calculating by unit mass) prescription: free from admixture, nothing are gone mouldy, drying, without the raw material of processing.2., 10 part 80% ethanol; 3., 10 part of 95% special solvent, be dissolved with cotton (gossypin) alcoholic solution.4. 5. 2 parts of byssuss of 0.01 part of magenta (being the alkali electroless synthetic dyestuffs), wherein 1 part as the reaction raw materials that extracts cotton ethanol soluble substance, in addition 1 part of conduct filter cloth that removes slag.6. 0.5 part of 20% acetic acid.7. 3 parts of fresh quicklime.

The preparation utensil

1. non iron heating container; The vial that 2. lid is arranged; 3. freezer; 4. narrow porcelain class vessel in the wide end of achromatization glaze mouth; 5. scrape spatula; 6. room temperature vacuum drying oven.

Synthesis step

Soaked slow fire heating in → 8 hours in 72 hours and boil and endure → filter and remove residue → add special organic solvent, cotton-shaped protein coagulating bar is gone out and shake up →-10 ℃ left standstill → extract out supernatant → eluting purification → limestone in 72 hours and contract deeply → dry in the shade → finished product.

Preparation method

1. earlier 95% medical ethanol is mixed with 80% ethanol molten night, soaks about 72 hours by 1: 10 raw material (dried Formica fusca) and alcohol solvent mass ratio.2. decoct 8 hours by adding the heating of hydrology fire at 1: 30, treat when water is evaporated to 1: 3 material-water ratio.3. by the time 1: 3 material water quality ratio the time.This moment protein, all water-soluble substanceses in formic acid water solublity, vitamin, trace element, cursive script formaldehyde or the like animal body, fully dissolving, the textile filter cloth with magenta was bleachinged and dyeing filters the residual substances that is insoluble to hot water.At this moment, the liquid after being filtered, the muddy liquid of the attitude that takes on a red color.4. with the medicinal liquid of the mixed clear liquid of red shape, the barrel-shaped glass container of packing into, fluid temperature remains between 70 ℃-80 ℃.5. inject and be dissolved with byssus 95% ethanol, the special alcoholic solution of solable matter about 70 ℃.Be layered as to the muddy liquid that presents bright tangible respectively milky white matter suspension and magenta, suspension and turbid liquid are long-pending to be always $\frac{2}{5}=\frac{3}{5}.$ Shake then and stir the companion.Suspension and muddy liquid are fully shaken up, make not only apparent suspension of branch and muddy liquid layering obviously but also recover the red muddy liquid status of hair.6. will be contained in the glass container (cup, bottle) and seal, be statically placed in the lining, icy storehouse (or freezer compartment of refrigerator) about maintenance-10 ℃, about 72 hours resting periods.7. become the magenta alcoholic solution attitude of transparent clear rut through 72 hours turbid liquid of low color contamination, under low temperature environment, take supernatant rapidly away.8. after taking supernatant away, with the light black shape flowing material that is deposited at the bottom of the glass container, in the slick porcelain container of swap-in (china bowl).9. carry out repeatedly eluting, purification.Rinsing liquid is 95% ethanol, 20% acetic acid (pure white vinegar), and food grade, the rinsing degree of purification is used earlier ethanol, and cerinic acid is used in the back, and repeated multiple times reaches eluent always, is till the colourless state.Add acetic acid then, become ethyl acetate after, left standstill one hour.10. with the red filter cloth that used once, wrap quicklime, tie up, be placed in the container of porcelain, allow quicklime sop up most hydrone, the ethyl acetate solution molecule.After reaching 80% concentrating degree, in the pasty state attitude the time.Scrape the pastel that sticks to filter cloth with scraping spatula, be placed on level and smooth porcelain, put into drying baker (room temperature vacuum drying) immediately and dry or dry in the shade, reach with till the dry anhydrous branch.(11) finished product is the black crystalline solid, all attitude materials.

Adopt above-mentioned several organic chemicalss to carry out chemical reaction mutually, all make all participate in the physical property of the former chemical substance of chemical reactions, change has taken place in chemical property, the protein of finally getting with conventional method, the attitude that is white in color, no matter any protein is white attitude.In this preparation method, in the proportioning raw materials, remove the consumption of ethanol water, big outside, other consumptions of chemical substance that participate in reaction are less, except gossypin and magenta (isatin) are solid, crystalline state, the material.Such as, ethanol water, acetic acid are the very high liquid substances of polarity, be difficult to obtain solid-state, crystalline solid.Therefore, chemical preparating process of the present invention, method are the chemical improvements to protein chemistry character.Make the protein of white attitude become brand new, chemical property, the novel substance of application function.We can say, obtained new function, the organic synthesis combinatorial chemistry novel substance of new purposes with neoteric chemical combination method.

The macromole novel organic compound that adopts the new invention combinational chemistry to obtain, its basic substance is a kind of common protein.Proteinic chemical framework is quite complicated, and molecular weight is huge, because the equipment of the finder's of novel substance chemical structure analysis is limited, still can not prove conclusively the chemical constitution of this novel substance.In a word, use the brand-new resulting material of chemical combination technology, have brand-new function and purposes.Similar pharmaceutically-active medicine with respect to traditional has more advantage, more is rich in characteristics.

Four, embodiment

The novel substance that adopts this new chemical combination technology to prepare is a kind of brand-new chemical constitution, chemical characteristic, newfound novel organic compound.By preliminary human body and animal experiment, find its chemism and function, as yet not to the chemical characteristic of the chemical entities of new initiative, deep research and understanding.Since the inventor to some property of medicine activity of this new chemical entities and function (such as: do not do the research of toxicological effect as yet, comprise chronic, acute toxicology, reproduction toxicity etc.) lack experimental condition and platform.Whether reach the organic unity and the requirement of safety and effectiveness, just present, also very in depth do not understand.Only rest on illustrating on the basis of preliminary function, the promptly preliminary preclinical study stage.Also be that this chemical entities only is described, will and be used for having on the male contraception application prospect and exploitation value in analgesia, it only also is the new discovery and the new invention of a science, still be unrealized large-scale production and application.

Claims (1)

1. Using neoteric compound method, is the new organic compound of the raw material acquisition of main source with the solable matters such as protein in the Polyhachis vicina Roger body.Ant body animal protein egg is deceived in natural existence, does not have special medicinal function and activity, after the preparation of employing new method, makes inanimate object activity, natural materials, has become to have special pharmacologically active and effect, semi-synthetic protein-based novel substance.This new compound " acetic acid ant melanocyte " has high penetration power to human body, can pass blood brain barrier and blood-testis barrier.Penetrate blood brain barrier, can act on pain nerve selectively, make pain relief, disappearance, penetrate blood-testis barrier, mankind spermatozoon is reduced, cause temporary fertility forfeiture.This product has the selectivity height, does not produce calmness, and syngignoscism does not produce dependency and addiction.To various pain all effectively (central pain and periphery pain).Do not suppress spermatogenesis, suppress testosterone secretion.No matter pain relieving of this product, antifertility, all effect rapidly, the length of holding time.The chemical stability height is suitable for characteristics such as oral, easy to use.Synthetic this functional mass, the primary raw material source is abundant, is easy to get, effective ingredient material yield height, preparation cost is low, and preparation route flow process is short, and reactions steps is few, and equipment requirements is not high, and is the most competitive, and purposes is many, the initiative novel substance that consumption is big.

   Be different from the chemical constitution composition of antifertility commonly used and analgesic preparation, mechanism of action, the new medicinal function novel organic compound of application (special envoy's antifertility activity), be the creator of this material, use the cotton ethanol extraction, chemicals such as pinkish red acetic acid are to natural materials, the water soluble protein that Polyhachis vicina Roger belongs to Formica fusca carries out chemical modification and transformation obtains, make the natural organic matter that does not originally have medicinal function and purposes change over novel chemical substance, the work fruit of the inventor's of having condensed wisdom and hardships with specific function and purposes.

   Therefore, the request state's laws obtain the legal protection of the preferential right that synthetic, route, combination material and the prescription of this active substance invented.

   One, behind the Polyhachis vicina Roger water-soluble substances (comprising water capacity protein, formic acid, formaldehyde etc.) that belongs to Formica fusca and chemical substance, byssus (ethanol extraction), pinkish red ethanol, the waterishlogging biochemical reaction, the crystalloid material that is obtained.Has potent, quick-acting, long lasting analgesic active substance, be to introduce byssus and magenta to carry out obtaining after natural materials (the Formica fusca hydrotrope) chemical modification, cotton ethanol extract and pinkish redly in the synthetic reaction process that obtains active substance, play crucial effects.Because its two derivants that chemical constitution is close in addition all have analgesic activities.Behind acetic acid replacement formic acid, then both kept analgesic activities.Has the active novel substance of remarkable antifertility again.Therefore; introduce the cotton ethanol extract; pinkish red; be carefully to be raw material from Formica fusca; two kinds of mankind that obtain chase after to be essential and ask the prescription of pharmacological action novel male oral contraceptive and novel non-addicted analgesics most critical; this is the obligee, adopts first to obtain contraception and analgesic activities prescription, and the request state's laws are protected by law the material that this prescription obtains.Require others not usefulness, the Formica fusca hydrotrope, the cotton ethanol extract, magenta, the prescription of acetic acid prepares novel substance, otherwise is regarded as infringement.