Anthracyclines: Daunorubicin, Doxorubicin, Idarubicin, Valrubicin, Bleomycin Sulphate, Mitomycin-C : Dactinomycin or Actinomycin D, Plicamycin (Mithramycin)
Antibiotics
Anthracyclines
occur as glycosides of the anthracyclinone. The glycosidic linkage usually
involves the-7hydroxyl group of anthracyclinone and the β enentiomer of sugar
with L-configuration. Anthracyclinone refers to an aglycone containing the
anthraquinone chromophore within a linear hydrocarbon skeleton related to that
of tetraycline.
Properties and uses: Daunorubicin is obtained from the fermentation
of Streptomyces peuletieues. This
drug bind to the DNA and inhibit nucleic acid synthesis, mitosis, and promote
chromosomal aberration. These drugs are used for the treatment of acute
myclocytic leukaemia, primary hepatocellular carcinomal, and ovarian
endometrial carcinoma.
Properties and uses: Doxorubicin hydrochloride is an orange-red
crystalline hygroscopic powder, soluble in water, and slightly soluble in
methanol. Doxorubicin is 14-hydroxy daunoruibicin obtained from the cultures of
Streptomyces peuletiues. It is one of
the most effective antitumour agent. It is used in the treatment of acute
lymphocytic leukaemia, breast, lung, ovarian, thyroid, gastric carcinoma, and
Hodgkin’s disease.
Assay: It is assayed by adopting liquid chromatography technique.
Dosage forms: Doxorubicin HCl injection I.P., Doxorubicin HCl tablets I.P.,
Doxorubicin injection B.P.
Properties and uses: Idarubicin is demethoxy daunorubicin. It is a synthetic analogue of naturally occurring anthracyclines. It is used in acute myelogeneous leukaemia and acute lymphocytic leukaemia.
Properties and uses: Valrubicin is a derivative of doxorubicin in
which the amino group has a trifluoroacetyl substituent and 14-hydroxy group is
converted to valerate ester.
Properties and uses: Bleomycin sulphate is a mixture of cytotoxic
glycopeptidase isolated from the strain of Streptomyces
verticillers. It is mixture of closely related compounds with bleomycin A2
and B2, Bleomycins occurs naturally as blue copper chelates. Inside,
the cell, bleomycin forms a complex with Fe (II), gives rise to hydroxyl
radical and superoxide radicals. These radicals cleave the phosphodiesterase
bond of DNA. This degradation of DNA strands is thought to be a lethal event in
cells. It is effective in the treatment of testicular carcinomas. It is also
useful in the treatment of squamous cell carcinomas of the head, neck,
oesophagus, skin, and the genito-urinary tract, including the cervix, vulva,
scrotum, and penis.
Properties and uses: Mitomycin exists as blue-violet crystals or
crystalline powder, slightly soluble in water, freely soluble in
dimethylacetamide, sparingly soluble in methanol, and slightly soluble in
acetone. It is obtained from Streptomyces
eqespitosus; it contains three different carcinostatic functions, quinone,
carbamate, and aziridine. The molecule is unreactive in its natural state. After
intracellular enzymatic or spontaneous chemical reduction of the quinone and
loss of the methoxy group, mitomycin becomes a bifunctional or trifunctional
alkylating agent. The drug inhibits DNA synthesis at the O6 and N7
positions of guanine. In addition, single-strand breakage of DNA are caused by
mitomycin. It is used in gastric and pancreatic carcinoma.
Assay: It is assayed by adopting liquid chromatography technique.
Properties and uses: It is obtained form the cultures of Streptomyces antibioticus. It consists of
tricyclic phenoxazone ring in the quinone oxidation state and two identical
polypeptide and intercalates into the double helical DNA. The main biochemical
consequence of the intercalation of actinomycin into DNA is the inhibition of
DNA and RNA synthesis, which in turn leads to depletion of protein and cell
death.
Properties and uses: It is an aureolic acid derivative obtained from Stremyles plicatus or Streptomyces argillaceus. It forms a
complex with divalent metals, such as magnesium and calcium and such complex
formation is required before binding with DNA. It inhibits DNA dependent RNA
polymerase, which leads to cell death. It is used in the treatment of embryonal
tumours of the testes and metastic cancers.
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