N-((S)-1,2,3,10-TETRAMETHOXY-9-OXO-5,6,7,9-TETRAHYDRO-BENZO[A]HEPTALEN-7-YL)-ACETAMIDE
Colchicine
CAS: 64-86-8
Molecular Formula: C22H25NO6
N-((S)-1,2,3,10-TETRAMETHOXY-9-OXO-5,6,7,9-TETRAHYDRO-BENZO[A]HEPTALEN-7-YL)-ACETAMIDE - Names and Identifiers
N-((S)-1,2,3,10-TETRAMETHOXY-9-OXO-5,6,7,9-TETRAHYDRO-BENZO[A]HEPTALEN-7-YL)-ACETAMIDE - Physico-chemical Properties
| Molecular Formula | C22H25NO6 |
| Molar Mass | 399.44 |
| Density | 1.2770 (rough estimate) |
| Melting Point | 150-160°C (dec.)(lit.) |
| Boling Point | 522.37°C (rough estimate) |
| Specific Rotation(α) | -250 º (c=1, alcohol) |
| Flash Point | 392.9°C |
| Water Solubility | 45 g/L (20 ºC) |
| Solubility | Soluble in ethanol, chloroform |
| Vapor Presure | 6.21E-21mmHg at 25°C |
| Appearance | White powder |
| Color | white to yellow with a green cast |
| Merck | 14,2471 |
| BRN | 2228813 |
| pKa | 12.36(at 20℃) |
| Storage Condition | 2-8°C |
| Stability | Stable. Light sensitive. Incompatible with strong oxidizing agents. |
| Sensitive | Light Sensitive |
| Refractive Index | 1.5614 (estimate) |
| MDL | MFCD00078484 |
| Physical and Chemical Properties | Light yellow crystal or crystalline powder, taste, taste bitter, see light discoloration. Mp157 ℃ (ethyl acetate recrystallization), specific rotation [α]17D-429 °(1.72%, water), -121 °(0.9%, chloroform), the maximum absorption wavelength in ethanol was 243nm and 350.5nm. This product is soluble in water, ethanol and chloroform, soluble in benzene and ether, insoluble in petroleum ether, 0.5% of this solution is weakly acidic. LD50 (mouse, abdominal cavity) 6.1 mg/kg. |
| Use | Anti-gout and anti-tumor drugs for the treatment of acute gout and cancer |
N-((S)-1,2,3,10-TETRAMETHOXY-9-OXO-5,6,7,9-TETRAHYDRO-BENZO[A]HEPTALEN-7-YL)-ACETAMIDE - Risk and Safety
| Risk Codes | R26/28 - Very toxic by inhalation and if swallowed. R41 - Risk of serious damage to eyes R46 - May cause heritable genetic damage |
| Safety Description | S13 - Keep away from food, drink and animal foodstuffs. S45 - In case of accident or if you feel unwell, seek medical advice immediately (show the label whenever possible.) S36/37/39 - Wear suitable protective clothing, gloves and eye/face protection. S28 - After contact with skin, wash immediately with plenty of soap-suds. S26 - In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. S53 - Avoid exposure - obtain special instructions before use. |
| UN IDs | UN 1544 6.1/PG 1 |
| WGK Germany | 3 |
| RTECS | GH0700000 |
| TSCA | Yes |
| HS Code | 29399990 |
| Hazard Class | 6.1 |
| Packing Group | I |
| Toxicity | LD50 in rats (mg/kg): 1.6 i.v. (Rosenbloom, Ferguson); in mice (mg/kg): 4.13 i.v. (Beliles) |
N-((S)-1,2,3,10-TETRAMETHOXY-9-OXO-5,6,7,9-TETRAHYDRO-BENZO[A]HEPTALEN-7-YL)-ACETAMIDE - Reference
| Reference Show more | 1. Li Peining, Chen Xiu Juan, Jiang Yi et al. Effects of three compounds on chromosome aberration of CHL cells induced by UV [J]. Daily Chemical Industry 2019 49(006):37-380 387. 2. Fan Sufang, Ma Junmei, Liu Min, et al. Determination of 15 toxic alkaloids in foods by high performance liquid chromatography-tandem mass spectrometry [J]. Food Science, 2018, 39(22):290-295. 3. Liu et al Qing-Shan [IF = 9.229]. "Novel Beta-Tubulin-Immobilized Nanoparticles Affinity Material for Screening β-tubulin Inhibitors from a Complex Mixture. Acs Appl Mater Inter. 2017;9(7):5725-5732 |
N-((S)-1,2,3,10-TETRAMETHOXY-9-OXO-5,6,7,9-TETRAHYDRO-BENZO[A]HEPTALEN-7-YL)-ACETAMIDE - Nature
Open Data Verified Data
light yellow needle-like crystals or crystalline powder. Molecular weight 399. The melting point was 155-157 °c. When wet or heated, there is a smell of grass, bitter taste. Slightly soluble in water (lg soluble in 22ml of water) and ether (lg soluble in 220ml of ether). Soluble in ethanol and chloroform. The crystals precipitated from the aqueous solution contained six crystals of water.
Last Update：2024-01-02 23:10:35
N-((S)-1,2,3,10-TETRAMETHOXY-9-OXO-5,6,7,9-TETRAHYDRO-BENZO[A]HEPTALEN-7-YL)-ACETAMIDE - Preparation Method
Open Data Verified Data
The colchicine can be extracted from the raw material of the mushroom. The mushroom is pulverized into 40~80 mesh powder, 60 ~ 70kg per cylinder, 85% ~ 95% ethanol 18 0 ~ 210L, heated to reflux for 4H, Suction filtration, and ethanol reflux extraction, A total of 3 times, the third suction filter mother liquor is applied, the 1st and 2nd suction filtrate is concentrated under reduced pressure, and ethanol is recovered. The distillation residue was added with 3 to 5 times the amount of water, stirred and left to stand, and then precipitated with the same colloid and filtered with a cloth bag. The colloid was washed with water three times, and the washing liquid was combined with the filtrate. The filtrate was adjusted to Ph 2 with 10% sulfuric acid, and was extracted by shaking with chloroform until the chloroform extract was colorless. The combined chloroform solution was washed once with about 300mL of 5% sodium hydroxide solution, and the chloroform layer was separated, dehydration was performed with anhydrous sodium sulfate, and chloroform was distilled to near dryness to obtain a gum. The resulting gum was added to 5 times the amount of ethyl acetate, heated and dissolved, filtered, crystallized and filtered, and the crude product was dried at less than 60 ° C. To obtain crude colchicine. Colchicine crude product was added with 2 times of chloroform, heated and dissolved, filtered, and the filtrate was recovered with 1/2 of chloroform, which was left overnight, suction filtered to dryness, firstly removed the residual chloroform, and then dried at low temperature to obtain colchicine salt crystals. Then, a further 5 times amount of ethyl acetate was added, dissolved by heating, left to crystallize, filtered, and the crystals were dried at less than 60 ° C. To give colchicine as a finished product.
Last Update：2022-01-01 11:14:54
N-((S)-1,2,3,10-TETRAMETHOXY-9-OXO-5,6,7,9-TETRAHYDRO-BENZO[A]HEPTALEN-7-YL)-ACETAMIDE - Standard
Authoritative Data Verified Data
This product is an alkaloid extracted from the bulbs of the Liliaceae plant Lijiang shanci via Iphigenia indicakunthet Benth. Calculated as anhydrous and solvent-free, the content of C22H25N06 shall not be less than 97.0%.
Last Update：2024-01-02 23:10:35
N-((S)-1,2,3,10-TETRAMETHOXY-9-OXO-5,6,7,9-TETRAHYDRO-BENZO[A]HEPTALEN-7-YL)-ACETAMIDE - Trait
Authoritative Data Verified Data
- This product is white-like to light yellow crystalline powder; Odorless; Slightly hygroscopicity; Dark color in case of light.
- This product is soluble in ethanol or chloroform, dissolved in water (but in a certain concentration of aqueous solution can form the crystallization of hemihydrate), very slightly dissolved in ether.
specific rotation
take this product, precision weighing, plus ethanol dissolution and quantitative dilution to make a solution containing about 10 mg per lml, according to the law (General 0621), according to the water, no solvent, the specific rotation is from one to 240 ° to one to 250 °.
Last Update：2022-01-01 13:42:38
N-((S)-1,2,3,10-TETRAMETHOXY-9-OXO-5,6,7,9-TETRAHYDRO-BENZO[A]HEPTALEN-7-YL)-ACETAMIDE - Use
Open Data Verified Data
mainly for the treatment of breast cancer, uterine cancer, esophageal cancer, lung cancer, gastric cancer also has a certain effect.
Last Update：2022-01-01 11:14:55
N-((S)-1,2,3,10-TETRAMETHOXY-9-OXO-5,6,7,9-TETRAHYDRO-BENZO[A]HEPTALEN-7-YL)-ACETAMIDE - Differential diagnosis
Authoritative Data Verified Data
- take this product, dissolve and dilute with ethanol to make a solution containing about 10ug per lml, according to UV-Vis spectrophotometry (General 0401), the absorbance was measured at a wavelength of 243nm and 350mn, and the ratio of the absorbance at a wavelength of 243nm to the absorbance at a wavelength of 350nm should be 1.7 to 1.9.
- The infrared absorption spectrum of this product should be consistent with that of the control (Spectrum set 277).
Last Update：2022-01-01 13:42:39
N-((S)-1,2,3,10-TETRAMETHOXY-9-OXO-5,6,7,9-TETRAHYDRO-BENZO[A]HEPTALEN-7-YL)-ACETAMIDE - Exam
Authoritative Data Verified Data
Related substances
operation in the dark. Take an appropriate amount of this product, add water-methanol (1:1) to dissolve and dilute to make a solution containing about 1 mg per 1 ml, as a test solution; Take an appropriate amount of precision, water-methanol (1:1) was added and quantitatively diluted to prepare solutions containing 10UG and 0.5ug per 1 ml, respectively, as control solutions (1) and (2). According to the high performance liquid chromatography (General 0512) test, using octanosilane bonded silica gel as filler, water as mobile phase A, methanol-water (55:45) as mobile Phase B, the flow rate was 1.0mL per minute and the detection wavelength was 254mn. First, isocratic elution was performed with mobile phase A- mobile phase B(30:70), column temperature was 20°C, and gradient elution was performed immediately after completion of colchicine peak elution; the number of theoretical plates is not less than 5000 based on the colchicine peak, and the separation degree between the impurity I Peak (relative retention time is about 0.9) and the colchicine peak should meet the requirements. 20u1 injection liquid chromatograph, colchicine peak signal-to-noise ratio is not less than 10; Then take sample solution and control solution (1) 20 u1 of each of the control solution (2) were injected into the liquid chromatograph, and the chromatogram was recorded to 2.5 times the retention time of colchicine peak. In the chromatogram of the test solution, the peak area of impurity I shall not be greater than 3.5 times (3.5%) of the main peak area of the control solution (1), and the peak area of other individual impurities shall not be greater than the control solution (1) main Peak area (1% ), the sum of each impurity peak area shall not be greater than 5 times (5%) of the main peak area of the control solution (1), the peaks in the chromatogram of the test solution which are smaller than the main peak area of the control solution (2) are ignored.
norcolchicine
take 0.05g of this product, add 5ml of water to dissolve, add 0.1ml of ferric chloride test solution, shake, if Green, with the same volume of control solution (take 1ml of cobalt chloride solution for color comparison, compare with 2.5 potassium dichromate solution for color comparison and copper sulfate solution for color comparison, no deeper.
residual solvent
take about 0.3g of this product, weigh it accurately, put it in a 20ml headspace bottle, Add 10ml of water accurately to dissolve it, seal it, and use it as a test solution; accurately weigh the appropriate amount of ethyl acetate and three-gas methane respectively, add water to make a mixed solution containing about 0.75mg and 3ug per 1 ml, accurately weigh 10ml, put it in a 20ml headspace bottle, and seal it, as a control solution. According to the test for determination of residual solvents (General rule 0861, Method 1), polyethylene glycol (PEG-20M) (or similar polarity) was used as the stationary liquid, the column temperature was 75°C, and the inlet temperature was 200°C, the detector temperature was 250°C, the headspace bottle equilibration temperature was 80°C, and the equilibration time was 30 minutes. Take the reference solution headspace injection, ethyl acetate peak and chloroform peak separation should meet the requirements. The sample solution and the reference solution were sampled by Headspace injection respectively. The chromatogram was recorded and the peak area was calculated according to the external standard method. Containing ethyl acetate not more than 6.0%, containing chloroform not more than 0.01%.
moisture
take this product, according to the determination of moisture (General 0832 first method 1), the water content shall not exceed 2.0%.
ignition residue
not more than 0.1% (General rule 0841).
Last Update：2022-01-01 13:42:40
N-((S)-1,2,3,10-TETRAMETHOXY-9-OXO-5,6,7,9-TETRAHYDRO-BENZO[A]HEPTALEN-7-YL)-ACETAMIDE - Content determination
Authoritative Data Verified Data
take this product about 0.25g, precision weighing, add anhydrous glacial acetic acid 50ml to dissolve, add acetic anhydride 5ml, according to the potential titration method (General rule 0701), with perchloric acid titration solution (0.1 mol/L) titration, and the results of the titration were corrected with a blank test. Each 1 ml of perchloric acid titration solution (0.1 mol/L) corresponds to 39.94mg of C22H25NO6.
Last Update：2022-01-01 13:42:41
N-((S)-1,2,3,10-TETRAMETHOXY-9-OXO-5,6,7,9-TETRAHYDRO-BENZO[A]HEPTALEN-7-YL)-ACETAMIDE - Category
Authoritative Data Verified Data
anti-gout drugs, antineoplastic drugs.
Last Update：2022-01-01 13:42:41
N-((S)-1,2,3,10-TETRAMETHOXY-9-OXO-5,6,7,9-TETRAHYDRO-BENZO[A]HEPTALEN-7-YL)-ACETAMIDE - Storage
Authoritative Data Verified Data
light shielding, sealed storage.
Last Update：2022-01-01 13:42:41
N-((S)-1,2,3,10-TETRAMETHOXY-9-OXO-5,6,7,9-TETRAHYDRO-BENZO[A]HEPTALEN-7-YL)-ACETAMIDE - Colchicine tablets
Authoritative Data Verified Data
This product contains colchicine (C22H25N06) should be 90.0% to 110.0% of the label amount.
trait
This product is white tablet.
identification
In the chromatogram recorded under the content determination item, the retention time of the main peak of the test solution should be consistent with the retention time of the main peak of the control solution.
examination
- Content uniformity 1 tablet of this product is placed in a 50ml(0.5mg specification) or lOOml(lmg specification) measuring flask, according to the method under the content determination item, starting from "adding appropriate amount of water, determination of content according to law, should comply with the provisions (General 0941).
- the dissolution of this product, according to the dissolution and release determination method (General rule 0931 third method), water 200ml as the dissolution medium, the speed of 50 rpm, according to the law, after 30 minutes, the appropriate amount of the solution was filtered, and the filtrate was taken as the test solution, add water to dissolve and quantitatively dilute to make a solution containing about 2.5ug(0.5mg specification) or 5ug(lmg specification) per 1 ml., as a control solution. According to the method under the content determination item, take the sample solution and the reference solution of 100 u1(0.5mg specification) or 5ul (lmg specification), respectively, and inject the human liquid chromatograph, the dissolution amount of each tablet was measured according to the law. The limit is 80% of the labeled amount and shall be in accordance with the provisions.
- others shall be in accordance with the relevant provisions under the item of tablets (General rule 0101).
Content determination
- measured by high performance liquid chromatography (General 0512).
- chromatographic conditions and system suitability test using octanosilane bonded silica gel as filler; Methanol-water (40:60) as mobile phase; The detection wavelength was 254mn. The number of theoretical plates shall not be less than 5000 based on the colchicine peak, and the separation degree between colchicine and adjacent chromatographic peaks shall meet the requirements.
- determination of 20 tablets of this product, precision weighing, fine grinding, precision weighing an appropriate amount (about equivalent to colchicine lmg), put in a 100ml measuring flask, add an appropriate amount of water, shake for 1 hour to dissolve colchicine, dilute to the scale with water, shake well, filter, take the filtrate as the test solution, and inject 20u1 into the liquid chromatograph to record the chromatogram; in addition, the colchicine reference substance was accurately weighed, dissolved by adding water and quantitatively diluted to prepare a solution containing about 10ug per lml, which was determined by the same method. According to the external standard method to calculate the peak area, that is.
category
Same as colchicine.
specification
(1)0.5mg (2)lmg
storage
light shielding, sealed storage.
Last Update：2022-01-01 13:42:42
N-((S)-1,2,3,10-TETRAMETHOXY-9-OXO-5,6,7,9-TETRAHYDRO-BENZO[A]HEPTALEN-7-YL)-ACETAMIDE - Reference Information
| NIST chemical information | information provided by: webbook.nist.gov (external link) |
| EPA chemical substance information | information provided by: ofmpeb.epa.gov (external link) |
| alkaloid | colchicine, also known as colchicine, is an alkaloid extracted from the bulbs and seeds of the Liliaceae plant colchicine, it is found naturally in the Liliaceae plant jialanensis (0.11%) and Lijiang (0.1%). Light yellow needle-like crystals. It is slightly odorous and bitter. Melting point 157 ℃, soluble in cold water, alcohol, chloroform and formaldehyde, poor solubility in hot water, not soluble in benzene and ether, almost insoluble in petroleum ether, 0.5% solution pH 5.9, after hydrolysis by ammonia, the toxicity can be reduced. Colchicine has anti-mitotic and anti-tumor effects. In 1889, the effect of colchicine on mitosis was first discovered by an Italian scholar, Pernica, who described that the mitotic phase of the cells in the inner wall of the Dog stomach was suppressed by colchicine and the spindle was destroyed, paralysis of chromosome action, abnormal mitotic cells remain in a large number of metaphase. This abnormal division caused by colchicine is called colchicine mitosis (C-mitosis for short). Colchicine is one of the most widely used chemical agents in karyotype analysis and polyploid mutagenesis. The concentration of the aqueous solution is positively correlated with the efficacy of its action, and the higher the concentration, the stronger the effect. Various plants and different tissues respond differently to colchicine. In summary, the treatment time for young and rapidly dividing tissues (such as the embryo of germinating seeds) can be shorter and the concentration should be lower; Whereas the treatment time can be longer and the concentration should be higher. The effective concentration of colchicine treatment was 0.01~10 ~ 0.4%, and about 0.2% of the most widely used. For example, the concentration of 0.2 ~ 0.4% colchicine solution drops on the growth point of diploid watermelon seedlings, once a day, for 4 consecutive days, and shade to maintain humidity, can induce tetraploid watermelon. For cereal crops, such as rice, the robust seedlings with more than four true leaves can be cut at the root neck, and immersed in 0.025 ~ 0.05% colchicine solution without cutting the growing point, submerged incision, after 8 to 14 days (20 degrees C) can also be obtained tetraploid plants. At present, colchicine is widely used for chromosome doubling of haploid plants obtained from anther (powder) and ovary culture. |
| anti-gout drugs | colchicine has a good effect on acute gout, which can relieve pain quickly and prevent the onset of arthritis, its mechanism of action is related to inhibiting the proliferation and activity of leukocytes and affecting the release of lysosomes. The pharmacological effect of this product is to reduce the activity and phagocytosis of leukocytes in inflammatory tissues, reduce the inflammation caused by uric acid crystals, and thus play an anti-inflammatory, detumescence and analgesic effect, therefore, it has a selective anti-inflammatory effect on acute gouty arthritis. In addition, this product is also a kind of mitotic toxin, which has a strong effect of inhibiting cell division, so that the cell stops in the division phase, resulting in the death of tumor cells, so it can be used for cancer treatment. This product is easy to absorb after oral administration, 30% is combined with plasma protein, the peak time of blood drug concentration is 0.5~2 hours after oral administration, and the peak concentration of 2mg is about 2.2ng/ml, after 12 hours of acute gout administration, the drug effect can be sustained for 50 to 70 hours, and the drug concentration in the isolated neutrophils is higher than the plasma concentration and can be maintained for 10 days. Most of this product is metabolized by the liver, metabolites and prototype drugs are excreted by the bile, reabsorbed by the intestine, not absorbed by the intestine. The remaining about 10% ~ 20% by the kidney with urinary excretion. This product does not affect the formation, dissolution and excretion of uric acid salt, and thus has no effect of lowering blood uric acid. It is clinically used to treat acute attack of gouty arthritis, prevent acute attack of recurrent gouty arthritis, familial Mediterranean fever, leukemia, skin cancer, Hodgkin's disease, aplastic anemia, etc. Also used for breast cancer, lung cancer, esophageal cancer, cervical cancer, nasopharyngeal carcinoma, Hodgkin's disease, chronic myelogenous leukemia, skin cancer and other malignant diseases M stage cycle specific treatment. |
| adverse reactions | and dose size were significantly correlated. 1. Gastrointestinal reactions: Nausea, Abdominal Pain, Diarrhea, Vomit and loss of appetite for the common early adverse reactions, the incidence rate of up to 80%, severe cases can cause dehydration and electrolyte disorders and other performance, such as the reaction immediately discontinued. Long-term users may develop severe hemorrhagic gastroenteritis or malabsorption syndrome. 2. Blood system reaction: Long-term medication can cause agranulocytosis, thrombocytopenia, aplastic anemia, and sometimes life-threatening. 3. Other toxic reactions; Mainly for urethral irritation symptoms, such as frequency, urgency, dysuria, hematuria, Oliguria, and even renal failure. Stomach, pharynx or skin burning sensation, and Fever, bloody Diarrhea, mental changes, myasthenia gravis, respiratory depression and other symptoms. 4. Check hemogram, liver and kidney function during taking colchicine. Hematopoietic insufficiency, liver and kidney damage, severe heart disease and gastrointestinal disease patients should be used with caution. Contraindicated in pregnant women. 5. Muscle, peripheral neuropathy: proximal muscle weakness, and serum creatine kinase increased; Muscle damage in the peripheral nerve axonal polyneuropathy may occur at the same time, manifested as numbness, tingling and weakness; muscle neuropathy is rare, often in the prevention of gout and long-term users and mild renal insufficiency appear. |
| dosage and usage | tablet: 0.5mg per tablet; Injection: 1mg, 2mg. 1. For the treatment of acute gout: adult oral tablets, the first dose of 0.5~1mg, after every 1~2 hours to take 0.5~0.6mg, until the joint symptoms or gastrointestinal symptoms, that is, withdrawal. The general total dose of 4~10mg effective. Note that the earlier the drug is used in the acute phase, the better the effect is. If intravenous injection, the first dose of 1~2mg, with normal saline 20ml slow injection, time of not less than 5 minutes, if necessary, every 6~12 hours intravenous injection of 0.5~1mg, until effective, the total dose of 4~5mg/d. The effect of intravenous injection was better than that of oral administration, and the gastrointestinal reaction was significantly reduced. 2. For the prevention of acute gout: adult tablets 0.5~0.6mg each time, 2 times a day or intravenous injection of 1~2mg/d. 3. For the experimental diagnosis of gout: such as acute joint symptoms after medication relief, that is helpful to confirm the diagnosis. |
| preparation | 1. Organic Solvent extraction method According to the nature of colchicine and its analogs, generally using ethanol, methanol and benzene as solvent extraction, this method is simple, low cost, less solvent consumption, but the extraction rate is low; There are a few literature water, chloroform, ethyl acetate as solvent. The effects of solvent type, extraction time and extraction method on the extraction effect of Mid-Autumn Chinese medicine Lily were investigated. The extraction agent was ethanol, the extraction time was 8H, and the alkalization of Lily powder could significantly improve the extraction effect, the extraction rate increased from 0.95% to 1.77%. 2. Supercritical carbon dioxide fluid extraction supercritical fluid extraction (SFE) is a new extraction technology developed in recent years. The research shows that supercritical fluid extraction can be used not only for fat-soluble alkaloids, but also for water-soluble alkaloids. This method is 1~10 times higher than the conventional method. Compared with the classical sample processing methods (such as Soxhlet extraction, liquid-liquid extraction, etc.), it has the following characteristics:(1) fast and efficient;(2) good selectivity;(3) less pollution, less sample consumption;(4) can be combined with other analytical techniques. Now the supercritical fluid extraction as an example to illustrate the process: CO2-SFE extraction of colchicine in mushroom, with 76% ethanol as entrainer, particle size of 10 mesh, extraction pressure 45kpa, extraction for 9H, the extraction rate of colchicine was 0.585%. The results showed that the average extraction rate of CO2-SFE with 76% entrainer was 1.25 times higher than that of reflux extraction, and the extraction time was reduced. |
| risk characteristics | colchicine itself is less toxic, but is metabolized (oxidized) in vivo after absorption A highly toxic oxidized colchicine (oxydicolicine), has a strong stimulating effect on the digestive tract, can inhibit hematopoietic cells, cause agranulocytosis and aplastic anemia. The nerve center, smooth muscle paralysis, resulting in vasodilation, respiratory center paralysis death. The lethal dose of colchicine to human is 6mg ~ 7mg. Mouse oral LD was 66.6mg/kg; Mouse intraperitoneal injection LD50 was 3.5mg/kg. Rats were injected subcutaneously with an LD50 of 4 mg/kg. This product has long been used in the treatment of acute gout, and has been found to have a strong inhibitory effect on cell division. It is used in medical treatment for various cancers, such as breast cancer, cervical cancer, esophageal cancer, skin cancer and chronic myeloid leukemia, etc. However, due to the great toxicity of colchicine, in order to reduce the toxicity and improve the efficacy, the structure of colchicine was modified, and the toxicity of the obtained compounds was reduced, such as colchicine (TMCA,I), colchicine (Demecolcine II), are now used in clinical. colchicine poisoning has a certain incubation period, generally in the oral or injection after 3d ~ 6d (or longer) symptoms, throat burning, Nausea, Vomit, Abdominal Pain Diarrhea, watery stool, hematuria, urination, hands and feet numbness, limb pain, muscle spasm, hair loss, mydriasis, convulsions, central nerve paralysis, respiratory depression death. In addition, local reactions can also occur, such as injection of the drug solution extravasation, local tissue necrosis can occur. Most of the poisoning cases were caused by accidental ingestion or drug overdose, and some were used for Suicide. The main treatment method was symptomatic treatment. Swallowing colchicine or colchicine poisoning prohibit the use of potassium permanganate and other oxidants, so as to avoid the oxidation of colchicine in the body to generate a large number of oxidized two colchicine and increase toxicity. |
| Use | used in the study of plant genetics; Used as selenium reagent; Clinical as antitumor drugs. This product is a typical mitotic toxin. For acute gout and the treatment of breast cancer. It is also used as a selenium reagent for plant genetics and cancer research. is an anti-gout and anti-tumor drug, used in the treatment of acute gout and tumor colchicine can inhibit mitosis, destroy the spindle, and make the chromosome arrest in the metaphase of division. |
| production method | This product is an alkaloid extracted from the bulbs of the Liliaceae plant, C. Licheniformis. The powder was extracted by heating and refluxing with 85% ethanol for 4H. The obtained ethanol solution was concentrated under reduced pressure to semi-gelatinous substance, diluted with distilled water, and the filtrate acidified with 10% sulfuric acid was extracted with chloroform, then the chloroform extract is concentrated and the crude colchicine obtained by crystallization is recrystallized to obtain the finished product. The total yield of the crude drug powder was 0.15%. Abroad, most of them are extracted from the bulbs of the genus colchicine of Liliaceae. The corms and seeds of the iprigenia India or the lily plant colchicine were extracted and refined with ethanol. |
| category | toxic substances |
| toxicity grade | highly toxic |
| Acute toxicity | intravenous-rat LD50: 1.6 mg/kg; Oral-mouse LD50: 5.886 mg/kg |
| stimulation data | eyes-rabbit 1%/3 days weight |
| flammability hazard characteristics | flammable; Thermal decomposition of toxic NOx fumes |
| storage and transportation characteristics | The warehouse is low temperature, ventilated and dry, and stored separately from food raw materials |
| extinguishing agent | water, carbon dioxide, dry powder, sand |
| toxic substance data | information provided by: pubchem.ncbi.nlm.nih.gov (external link) |
Last Update：2024-04-09 20:48:19
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QQ: 3785839865
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