Blasticidin S

422.44

422.44

606-640-2

1758

613045

2588

DTXSID0058015

Colorless crystals

29349990

215.67000

0.25370

COLOURLESS CRYSTALS.

1.61 g/cm3

235-236 °C (decomp)

539.06°C (rough estimate)

1.707

>30 g l -1 (20 °C)

Low

Oral-Rat LD50: 16 mg/kg; Oral-Mouse LD50: 38 mg/kg

Combustion produces toxic nitrogen oxide gas

D11 +108.4° (water)

pKa1: 2.4 (carboxylic aicd); pKa2: 4.6 (amine); pKa3: 8.0 (amine); pKa4: >12.5 (amine)

Light brown solid /Technical/

II

6.1(a)

3172

28

24/25-36/37-45

EC4900000

T+

The warehouse is ventilated, low temperature and dry; stored and transported separately from food materials

Incompatible with strong oxidizing agents.

SRP: The most favorable course of action is to use an alternative chemical product with less inherent propensity for occupational exposure or environmental contamination. Recycle any unused portion of the material for its approved use or return it to the manufacturer or supplier. Ultimate disposal of the chemical must consider: the material's impact on air quality; potential migration in soil or water; effects on animal, aquatic, and plant life; and conformance with environmental and public health regulations.

Incompatible with alkaline materials. /benzylaminobenzenesulfonate (BABS) salt/

Combustible. Gives off irritating or toxic fumes (or gases) in a fire.

|Danger|H300: Fatal if swallowed [Danger Acute toxicity, oral]|P264, P270, P301+P310, P321, P330, P405, and P501|H300 (100%): Fatal if swallowed [Danger Acute toxicity, oral]|Aggregated GHS information provided by 206 companies from 1 notifications to the ECHA C&L Inventory.|P260, P264, P270, P280, P301+P310, P305+P351+P338, P309+P311, P312, P321, P330, P331, P332+P313, P337+P313, P405, and P501

Use powder, water spray, foam, carbon dioxide.

SRP: The scientific literature for the use of contact lenses in industry is conflicting. The benefit or detrimental effects of wearing contact lenses depend not only upon the substance, but also on factors including the form of the substance, characteristics and duration of the exposure, the uses of other eye protection equipment, and the hygiene of the lenses. However, there may be individual substances whose irritating or corrosive properties are such that the wearing of contact lenses would be harmful to the eye. In those specific cases, contact lenses should not be worn. In any event, the usual eye protection equipment should be worn even when contact lenses are in place.|The protective clothing should be kept in separate places where it cannot be contaminated with toxic chemicals. It should be forbidden to keep this clothing in living quarters. Protective clothing must be washed at least once a week and each time it is contaminated with pesticides. Before washing the clothing should be soaked for several hours in a calcium carbonate solution. /Pesticides/|Smoking, eating, and drinking before washing should be absolutely prohibited when any pesticide ... is being handled or used. /Pesticides/

Severe eye irritant.|Blasticidin-S causes irritation and inflammation upon contact with eyes and mucous membranes. A survey of ophthalmic disturbances conducted in the 1960's showed that in some years one-third of the applicators suffered some damage, including skin eruptions all over the body.

Personal protection: particulate filter respirator adapted to the airborne concentration of the substance. Sweep spilled substance into sealable containers. If appropriate, moisten first to prevent dusting. Carefully collect remainder. Then store and dispose of according to local regulations.

Separated from food and feedstuffs. Well closed.

A harmful concentration of airborne particles can be reached quickly when dispersed, especially if powdered.

The substance is severely irritating to the eyes. The substance is irritating to the respiratory tract and skin. Corrosive on ingestion. Exposure at high levels could cause death.

NO open flames.

PREVENT DISPERSION OF DUST! STRICT HYGIENE! AVOID EXPOSURE OF ADOLESCENTS AND CHILDREN! IN ALL CASES CONSULT A DOCTOR!

Avoid inhalation of dust. Use local exhaust or breathing protection.

Protective gloves. Protective clothing.

Wear face shield or eye protection in combination with breathing protection if powder.

most toxic

LD50 Rat dermal 3100 mg/kg|LD50 Rat oral (female) 55.9 mg/kg|LD50 Rat oral (male) 56.8 mg/kg|LD50 Mouse iv 2.82 mg/kg|For more Non-Human Toxicity Values (Complete) data for BLASTICIDIN-S (9 total), please visit the HSDB record page.

...Those who have vitamin B2 deficient whole blood (8.05 gamma/dl) were most sensitive to /acute ocular impairment from/ blasticidin S.

Production by the fermentation of Streptomyces griseochromogenes.

Blasticidin-S's former production and use as an antibiotic(2) may have resulted in its release to the environment through various waste streams; its former use in the US as a fungicide(1) will have resulted in its direct release to the environment(SRC).

TERRESTRIAL FATE: Based on a classification scheme(1), an estimated Koc value of 1,500(SRC), determined from a structure estimation method(2), indicates that blasticidin-S is expected to have low mobility in soil(SRC). Blasticidin-S has pKa1, pKa2, pKa3, and pKa4 of 2.4 (carboxylic acid), 4.6, 8.0, and >12.5 (amino groups), respectively,(5), indicating that this compound will primarily exist with an overall positive charge in the environment and cations generally adsorb to organic carbon and clay more strongly than their neutral counterparts(6). Volatilization of blasticidin-S from moist soil surfaces is not expected to be an important fate process(SRC) given an estimated Henry's Law constant of 1.5X10-34 atm-cu m/mole(SRC), using a fragment constant estimation method(3), and its ionic character. Blasticidin-S is not expected to volatilize from dry soil surfaces(SRC) based upon an estimated vapor pressure of 1.8X10-16 mm Hg(SRC), determined from a fragment constant method(4). Half-lives in two soil types with organic content of 2.53 and 9.6% and moisture of 42.6 and 87%, respectively, at pH 6.0 and 25 °C were <2 days(5).|AQUATIC FATE: Based on a classification scheme(1), an estimated Koc value of 1,500(SRC), determined from a structure estimation method(2), indicates that blasticidin-S is expected to adsorb to suspended solids and sediment(SRC). Blasticidin-S has pKa1, pKa2, pKa3, and pKa4 of 2.4 (carboxylic acid), 4.6, 8.0, and >12.5 (amino groups), respectively(3), indicating that this compound will primarily exist with an overall positive charge in the environment and cations generally adsorb to organic carbon and clay more strongly than their neutral counterparts(4). Since this compound is expected to exist with an overall positive charge in the environment, volatilization from water surfaces is not expected to be an important fate process. According to a classification scheme(5), an estimated BCF of 3.1(SRC), from an estimated log Kow of -4.68(6) and a regression-derived equation(7), suggests the potential for bioconcentration in aquatic organisms is low.|ATMOSPHERIC FATE: According to a model of gas/particle partitioning of semivolatile organic compounds in the atmosphere(1), blasticidin-S, which has an estimated vapor pressure of 1.8X10-16 mm Hg at 25 °C(SRC), determined from a fragment constant method(2), is expected to exist solely in the particulate phase in the ambient atmosphere. Particulate-phase blasticidin-S may be removed from the air by wet and dry deposition(SRC).

Blasticidin-S is not expected to undergo hydrolysis in the environment due to the lack of hydrolyzable functional groups(1). Blasticidin-S does not absorb light with wavelengths >290 nm in aqueous solution at acidic or basic conditions(2), and direct photolysis by sunlight would not be expected(SRC).

An estimated BCF of 3.1 was calculated for blasticidin-S(SRC), using an estimated log Kow of -4.68(1) and a regression-derived equation(2). According to a classification scheme(3), this BCF suggests the potential for bioconcentration in aquatic organisms is low(SRC). Blasticidin-S has pKa1, pKa2, pKa3, and pKa4 of 2.4 (carboxylic acid), 4.6, 8.0, and >12.5 (amino groups), respectively(4), indicating that this compound will primarily exist with an overall positive charge in the environment and would be expected to have a low potential for bioconcentration(SRC).

Using a structure estimation method based on molecular connectivity indices(1), the Koc for blastinidin-S can be estimated to be 1,500(SRC). According to a classification scheme(2), this estimated Koc value suggests that blasticidin-S is expected to have low mobility in soil. Blasticidin-S has pKa1, pKa2, pKa3, and pKa4 of 2.4 (carboxylic acid), 4.6, 8.0, and >12.5 (amino groups), respectively(3), indicating that this compound will primarily exist with an overall positive charge in the environment, and cations generally adsorb to organic carbon and clay more strongly than their neutral counterparts(4).

Blasticidin-S has pKa1, pKa2, pKa3, and pKa4 of 2.4 (carboxylic acid), 4.6, 8.0, and >12.5 (amino groups)(1), respectively, indicating that this compound will primarily exist with an overall positive charge in the environment, and therefore volatilization from water surfaces or moist soil surfaces are not expected to be an important fate processes(SRC). Blasticidin-S is not expected to volatilize from dry soil surfaces(SRC) based upon an estimated vapor pressure of 1.8X10-16 mm Hg(SRC), determined from a fragment constant method(2).

Occupational exposure to blasticidin-S may have occurred through inhalation and dermal contact with this compound at workplaces where blasticidin-S was produced or used. Occupational exposure and general population exposure should be low or non-existent since blasticidin-S is no longer produced or used in the US. (SRC)

Compounds or agents that combine with an enzyme in such a manner as to prevent the normal substrate-enzyme combination and the catalytic reaction. (See all compounds classified as Enzyme Inhibitors.)|Agents destructive to the protozoal organisms belonging to the suborder TRYPANOSOMATINA. (See all compounds classified as Trypanocidal Agents.)|Substances that destroy fungi by suppressing their ability to grow or reproduce. They differ from FUNGICIDES, INDUSTRIAL because they defend against fungi present in human or animal tissues. (See all compounds classified as Antifungal Agents.)|Substances that inhibit the growth or reproduction of BACTERIA. (See all compounds classified as Anti-Bacterial Agents.)

Upon oral application to the mouse, blasticidin-S and metabolites were excreted in the urine and feces within 24 hr.

In rice plants, cytomycin and deaminohydroxy blasticidin-S were identified as the main metabolites.

Protein synthesis inhibitor.|Blasticidin-S is a peptidyl nucleoside antibiotic isolated from the culture broth of Streptomyces griseochromogenes. It specifically inhibits protein synthesis in both prokaryotes and eukaryotes through inhibition of peptide bound formation in the ribosomal machinery.

Fresh air, rest. Refer immediately for medical attention.

Remove contaminated clothes. Rinse and then wash skin with water and soap. Refer for medical attention if skin irritation occurs.

Rinse with plenty of water (remove contact lenses if easily possible). Refer immediately for medical attention.

...Antidotes have not been observed to be effective in cases of oral ingestion. Suggested methods of treatment included intravenous fluid administration, management of body fluid and electrolyte balance, adequate hydration to maintain normal blood pressure and urinary output, prevention of aspiration pneumonitis, and use of supportive ventilation. ...Recognition of blasticidin-S poisoning and early intervention methods should prove effective in cases of accidental or intentional ingestion.|Basic treatment: Establish a patent airway. Suction if necessary. Watch for signs of respiratory insufficiency and assist ventilations if needed. Administer oxygen by nonrebreather mask at 10 to 15 L/min. Monitor for pulmonary edema and treat if necessary ... . Monitor for shock and treat if necessary ... . Anticipate seizures and treat if necessary ... . For eye contamination, flush eyes immediately with water. Irrigate each eye continuously with normal saline during transport ... . Do not use emetics. For ingestion, rinse mouth and administer 5 ml/kg up to 200 ml of water for dilution if the patient can swallow, has a strong gag reflex, and does not drool ... . Cover skin burns with dry sterile dressings after decontamination ... . /Poison A and B/|Advanced treatment: Consider orotracheal or nasotracheal intubation for airway control in the patient who is unconscious, has severe pulmonary edema, or is in respiratory arrest. Positive pressure ventilation techniques with a bag valve mask device may be beneficial. Monitor cardiac rhythm and treat arrhythmias as necessary ... . Start an IV with D5W /SRP: "To keep open", minimal flow rate/. Use lactated Ringer's if signs of hypovolemia are present. Watch for signs of fluid overload. Consider drug therapy for pulmonary edema ... . For hypotension with signs of hypovolemia, administer fluid cautiously. Watch for signs of fluid overload ... . Treat seizures with diazepam (Valium) ... . Use proparacaine hydrochloride to assist eye irrigation ... . /Poison A and B/

/HUMAN EXPOSURE STUDIES/ ...Group application of Blasticidin-S on paddy field by 30 persons with application times of 30, 60, and 120 min /resulted in/ pains in the pharynx in 15, headache in 9, nausea in 5, abdominal pains in 10, eye disturbance in 2, coughing in 13, dyspnea in 5, pyrexia in 4, and dermatitis in 7 min ... . Chest roentgenography was carried out on 12 of 22 persons and abnormal density was found in eight patients; hospitalization of three serious cases resulted. The hospital histories of the three patients are described in detail; pre-hospitalization symptoms included vomiting (2/3), photophobia, lacrimation (3/3), cough (2/3), pyrexia (3/3), and diarrhea. All showed increased pulmonary markings and spot-like shadows in roentgenography. These anomalies were cleared up completely or partly. Negative results were obtained with patch tests with Blasticidin-S.|/CASE REPORTS/ In three fatal cases, nausea, vomiting, and severe diarrhea appeared almost immediately after ingesting 100 to 250 ml of undiluted formulation of containing 2 to 5 g blasticidin-S... . Pain in the oral cavity and pharynx was noted in all patients. In one case, the vomitus was bloody and esophageal pain was claimed. All patients were completely conscious and restless during the 6 to 10 hr after ingestion. Hypotension associated with tachycardia became more pronounced as time passed. Marked cold, pale, and perspired extremities were usually noted. Thermal symptoms indicated insufficient peripheral circulation. No cardiac anomalies were seen. The average hematocrit and hemoglobin concentrations for the three fatal cases were 52.9 and 17.4 g/100 ml, respectively. Remarkable hemoconcentration was consistently noticed. laboratory findings reveled moderate hepatic dysfunction. In the terminal phase of the fatal cases, blood pressure dropped and pulse rates increased above 120 beats/min. Death occurred about 1 day after ingestion.|/CASE REPORTS/ A 41-yr-old male developed acute interstitial pneumonia after inhalation of Blasticidin S, an antibiotic effective against rice blast disease. He presented with diarrhea, followed by dry cough, dyspnea and fever. A chest roentgenogram showed bilateral diffuse ground glass appearance, superimposed by patchy shadows. Arterial blood gas analysis revealed severe hypoxemia. Bronchoalveolar lavage fluid specimen showed moderate increase in total cell count, lymphocytes, neutrophils and eosinophils with marked elevation of CD4/8 ratio. Antibiotic therapy with minocycline failed to improve his condition, and methylprednisolone pulse therapy followed by methylprednisolone (48 mg) resulted in clinical remission with resolution of the chest roentgenogram findings. ...|/CASE REPORTS/ ...4 ...cases of acute poisoning from ingesting blasticidin S for suicidal attempts /are reported/. Three of the /poisonings/ were fatal. The symptoms observed in the patients included vomiting immediately after ingestion and severe, persistent, watery diarrhea. The toxic effects of blasticidin S were noted in ectodermal tissues including the skin, conjunctiva, cornea, and intestine. Massive loss of intestinal fluid resulted in progressively pronounced hypotension associated with tachycardia. ...|/CASE REPORTS/ Cases of acute blasticidin-S poisonings in Taiwan between July 1985 and December 1993 were analyzed in an attempt to clarify the toxicity of acute blasticidin-S ingestion. Altogether, 28 blasticidin-S poisonings, 24 of which were suicidal ingestions, were recorded. The primary pathological effects of blasticidin-S poisoning occurred in selective mucosal membranes such as the intestine, conjunctiva, and cornea as well as the skin. In most cases, the symptoms presented were immediate vomiting, diarrhea, sore throat, and abdominal pain, which resolved after traditional treatment methods such as gastric lavage, delivery of activated charcoal, and administration of atropine. In more severe cases, hypotension, arrhythmia, acrocyanosis, aspiration, and coma occurred. Profound hypotension and severe aspiration pneumonitis were the main causes for fatalities in five patients. ...

blasticidin S

The substance can be absorbed into the body by inhalation of its aerosol and by ingestion.

Sore throat. Cough. Headache. Laboured breathing. See Ingestion.

Redness.

Redness. Pain.

Formulation types EC; DP; WP. /benzylaminobenzenesulfonate (BABS) salt/|Bla-S

The WHO Recommended Classification of Pesticides by Hazard identifies Blasticidin-S (technical grade) as Class IB: highly hazardous; Main Use: fungicide, other than for seed treatment.|Blasticidin S is used to select transfected cells carrying bsr or BSD resistance genes in mammalian and plant cells.|Damage can be caused to alfalfa, aubergines, clover, potatoes, soya beans, tobacco, and tomatoes. Excessive application produces yellow spots on rice leaves. Formulated as the benzylaminobenzenesulfonate to reduce phytotoxicity.

Product analysis by bioassay with Bacillus cereus IAM-1729. Residues determined by bioassay with Fulvia fulva ACI-1164.