Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Carbohydrate doai
Reexamination Certificate
2002-03-19
2003-12-16
Lilling, Herbert J. (Department: 1651)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Carbohydrate doai
C424S725000
Reexamination Certificate
active
06664236
ABSTRACT:
FIELD OF INVENTION
The present invention relates to a synergistic composition of bioactive constituent essentially constituting iridoid glucosides, acetyl barlerin and shanzhiside methyl ester isolated from a plant source
Barleria prionitis linn
along with a process for the isolation of the bioactive fraction. The present invention also relates to a method of treating mammals and humans for hepatotoxicity, stress and immuno-deficiency with the synergistic bioactive composition.
BACK GROUND AND PRIOR ART REFERENCES
Barleria prionitis Linn
. (Family: Acanthaceae) is a well-known plant used in the indigenous system of medicine in India. Almost all its parts are used as medicine. The leaves are diuretic and are used in urinary infections and for the treatment of paralytic stroke, rheumatic pains and stomach disorders. The plant has antiseptic properties and its decoction is used as a wash in dropsy. The roots are used for toothache and for inflammatory disorders. The bark is given in whooping cough and as an expectorant [L. V. Asolkar et al; Glossary of Indian Medicinal Plants (second supplement), Council for Scientific and Industrial Research (CSIR), New Delhi, 1992, p. 115; Wealth of India: Raw Materials, CSIR, New Delhi, 1988, Vol. 11 B, p. 47].
The first report on chemical investigation of this plant appeared in 1970 when Moitra et al. reported the presence of &bgr;-sitosterol [Moitra, S. K. et al. (
Bull. Calcutta Sch. Trop. Med
; 1970, 18,7]. Harborne et al. reported the isolation of scutellarein-7-rhamnosyl glucoside from fresh flowers [Harborne, J. B. et al;
phytochemistry
, 1971, 10, 2822]. The structure of this compound is later modified as 5,6,4′-trihydroxy-7-0-neohesperidosylflavone [Nair, A. G. Ramchandran et al.,
Ind. J.Chem.
1982, 21 B, 1135].
The leaves and stems showed the presence of five iridoid glucosides. Four of them, acetylbarlerin (6,8-di-O-acetyl shanzhiside methyl ester), barlerin (8-O-acetyl shanzhiside methyl ester), shanzhiside methyl ester and 6-0-acetyl shanzhiside methyl ester have been characterized [Taneja, S. C. and Tiwari, H. P.,
Tetrahedron Lett
, 1975, 1995; Damtoft, S. et al.,
ibid
, 1982, 23,4155; Emary, N. A. et al.
Bull Pharm. Sci. Assuit Univ.
1990, 13 (1), 65-72].
In view of the strong hepatoprotective and immunorestorative activities exhibited by the iridoid glucosides of the roots of
Picrorhiza kurroa
viz. kutkin, picroside and kutkoside [Ansari, R. A. et al.
Indian J. Med. Research
, 1988, 87,401; Sharma, M. L., Ph.D thesis entitled “Evaluation of immunomodulatory activity of some medicinal plants in mammals”, 1991, University of Jammu] and
Vitex negundo
viz. agnuside and negundosides [Suri, J. L. et al., Indian Patent No. 178389/1997; Banerjee, S. K. et al. Indian Patent application No.1 16/DEL/98].
A detailed chemical and pharmacological investigation of
Barleria prionitis
(aerial parts) has led to the isolation of a bioactive fraction in about 14% yield having marked hepatoprotective, immunorestorative and antistress activities.
OBJECTS OF THE INVENTION
The main object of the present invention is to provide a synergistic composition of bioactive fraction essentially constituting iridoid glucosides, acetyl barlerin and shanzhiside methyl ester isolated from a plant source
Barleria prionitis linn
. Another object of the present invention is to provide a process for the isolation of the bioactive fraction. Yet another object of the present invention is to provide a method of treating mammals and humans for hepatotoxicity, stress and immuno-deficiency with the synergistic bioactive composition.
SUMMARY OF THE INVENTION
The present invention relates to a synergistic composition of bioactive fraction essentially constituting iridoid glucosides, acetyl barlerin and shanzhiside methyl ester isolated from a plant source
Barleria prionitis linn
. The present invention also provides a process for the isolation of the bioactive fraction. The present invention further provides a method of treating mammals and humans for hepatotoxicity, stress and immuno-deficiency with the synergistic bioactive composition.
DETAILED DESCRIPTION OF THE INVENTION
Accordingly, the present invention provides a novel synergistic pharmaceutical composition comprising a bioactive fraction of iridoid glucosides obtained from the plant
Barleria prionitis linn
, said bioactive fraction comprising the following ingredients
(a) barlerin in the range of 1.6-6.2%;
(b) acetyl barlerin in the range of 0.015-0.38%;
(c) shanshizide methylesters in the range of 4.4-8.0%; and
(d) pharmaceutically accepted additives, and
having hepatoprotective, antistress and immunorestorative properties on subjects.
An embodiment of the present invention, wherein said composition is used to treat hepatic injury caused by Carbon tetrachloride, Acetaminophen, and Galactosamine.
Yet another embodiment of the present invention, wherein the preferred dosage for CCl
4
induced hepatotoxicity in mammals is 20-200 mg/kg of body weight.
Still another embodiment of the present invention, wherein the hepatoprotective activity in CCl
4
induced hepatotoxic mammals is upto 88%.
Yet another embodiment of the present invention, wherein the dosage for Acetaminophen induced hepatotoxicity in mammals is in the range of 50-100 mg/kg of body weight.
Still another embodiment of the present invention, wherein the hepatoprotective activity in acetaminophen induced hepatotoxicity in mammals is upto 86%.
Yet an other embodiment of the present invention, wherein the dosage for Galactosamine induced hepatotoxicity in mammals is in the range of 50-100 mg/kg of body weight.
Still another embodiment of the present invention, wherein the hepatoprotective activity in Galactosamine induced hepatotoxicity in mammals is upto 86%.
Yet another embodiment of the present invention, wherein the dosage for anti-fatigue activity in mammals is in the range of 25-100 mg/kg of body weight.
Still another embodiment of the present invention, wherein the preferred dosage for anti-fatigue activity in mammals is in the range of 50-100 mg/kg of body weight.
Yet another embodiment of the present invention, wherein the anti-fatigue effect in mammals is over 80%.
Still another embodiment of the present invention, wherein the dosage for immunorestorative activity is in the range of 50-100 mg/kg of body weight.
Yet another embodiment of the present invention, wherein the immunorestorative activity is up to 70%.
Still another embodiment of the present invention, wherein said composition reduces the elevated levels of serum glutamin-pyruvic transaminase (GPT) by about 92%.
Yet another embodiment of the present invention, wherein said composition reduces the elevated levels of serum glutamic-oxalo acetic transaminase (GOT) by about 74%.
Still another embodiment of the present invention, wherein said composition reduces the elevated levels of serum alkaline phosphatase (ALP) by about 88%.
Yet another embodiment of the present invention, wherein said composition reduces the elevated levels of serum triglycerides by about 88%.
Still another embodiment of the present invention, wherein the hepatoprotective activity of said composition against the elevated level of bilirubin is about 85.96%.
Yet another embodiment of the present invention, wherein the subject is selected from mammals and humans.
Still another embodiment of the present invention, wherein said composition is used singly or in combination with pharmaceutically acceptable carriers.
Yet another embodiment of the present invention, wherein said composition is administered to a subject in combination with a pharmaceutically acceptable additives, carriers, diluents, solvents, filters, lubricants, excipients, binder or stabilizers.
Still another embodiment of the present invention, wherein the desired dosage is administered for both preventive and curative properties.
Yet another embodiment of the present invention, wherein said composition is administered systemically, orally or by any clinically/medically
Anand A. S.
Banerjee S. K.
Chandan Bal Krishan
Handa Sukhdev Swami
Jaggi Bupinder Singh
Council of Scientific and Industrial Research
Foley & Lardner
Lilling Herbert J.
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