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Management of Pain and Inflammation
Pain affects a large population worldwide.
Potentially dangerous stimuli causing pain need to be reported immediately for our well-being. Management of pain by traditional therapies involve use of NSAIDs, opoids and antidepressants. These have low therapeutic indexes and undesirable side effects. They are often relatively ineffective in treating chronic pain. Need to evolve new molecules which are selective, possess high therapeutic index and few side-effects, if any.
PHARMA TECHNOLOGIESDept. of Chem . UoP Prof. Subhash Padhye
NEW ANTIOXIDANTS TO COMBAT INFLAMMATORYDISORDERS AND CANCERS
COOH
COX-1 COX-2
NSA ID’s
Inhibitors include:Aspirin,Ibuprofen & IndomethacinInhibition may lead to Gastric ulcers,Kidney damages
Inhibitors includeNimesulide, NS-398.No known side-effects
Pain is caused by the effects of these prostaglandins which are released in the
inflammatory process.
ProstacyclinsProstaglandins
Arachidonic acidFree radicals
PHARMA TECHNOLOGIESDept. of Chem . UoP Prof. Subhash Padhye
NEW ANTIOXIDANTS TO COMBAT INFLAMMATORYDISORDERS AND CANCERS
OUR WORK DEALS AT TWO LEVELS
Producing oral drugs which can scavenge toxic radicals
(because enzymes are ineffective by oral/I.p. routes.
Creating new COX-2 inhibitors which are effective in low doses.
00.010.020.030.040.05
Time/secs
Incr
ease
in R
adic
als
45.4
4.2 4.6
0
2
4
6Effective Lowest
dose/X 10-8MNa
tive
USL1
USL5
CR-4
Control
Nimesulide
Our compound
PHARMA TECHNOLOGIESDept. of Chem . UoP Prof. Subhash Padhye
NEW ANTIOXIDANTS TO COMBAT INFLAMMATORYDISORDERS AND CANCERS
PHARMA TECHNOLOGIESDept. of Chem . UoP Prof. Subhash Padhye
modifiedO
OH
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HO
H3CO
O N
ON
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H3CO OCH3
HOOH
H3CO OCH3
O
O
H
HM N ONH
C Cl
NH2
SO
HOOH
H3CO OCH3
M
Conjugate of L1 Conjugates of L2 & L3
0.62
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0.280.47
0.7
1.9
0
0.5
1
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2
2.5
L2
co
nju
.
L3
co
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.
L4
co
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.
IC50
in
MThe IC50 values in M of the curcumin derivatives and their
metal complexes (IC50 for native SOD = 4x10-8 M ; For [ Cu2(bpzbiap)Cl3]=
2.55x10 -7M
Ref: Reedijk et.al, IC,36 (1997)1168
NEW ANTIOXIDANTS TO COMBAT INFLAMMATORYDISORDERS AND CANCERS
PHARMA TECHNOLOGIESDept. of Chem . UoP Prof. Subhash Padhye
Both Mice received Transplant of
human Cancer cells but treatment
of the Bottom Animal with an NSAID
greatly slowed the growth of the
cells
NEW ANTIOXIDANTS TO COMBAT INFLAMMATORYDISORDERS AND CANCERS
PHARMA TECHNOLOGIESA. R. I Prof. Sabita Dey Ratnakar Chitte
A NEW THROMBOLYTIC ENZYME FOR ACUTE MYOCARDIAL INFARCTION
Quchterlony test of Actinokinase
0
5
10
15
20
25
30
35
40
45
0 20 40 60 80 100
Concentration in ug
clot
dis
solu
tion
time
(min
)
Clot dissolution time
-------Plasmin --- ---- Streptokinase-------- Urokinase ------ Actinokinase
PHARMA TECHNOLOGIES
Modern Cancer therapy Search for Immunomodulators•Sham Diwanay
Dept. of Microbiology,
Abasaheb Garware College,
Pune•Dr. Bhushan Patwardhan
School of Health Sciences,
University of Pune, Pune
Immunomodulation
• Concept and Definition: Immunomodulators are Biological Response Modifiers (BRM), used to treat cancer, exert their anti-tumor effects by improving host defense mechanisms against tumor (Encyclopedia Britannica).
• Immunostimulation in drug-induced immunosuppression and immunosuppression in experimental hyper-reactivity model by the same preparation can be said to be true immunomodulation.
PHARMA TECHNOLOGIES
Modern Cancer therapy Search for Immunomodulators•Sham Diwanay• Dr. Bhushan Patwardhan
Ashwagandha Gulwel Shatavari
PHARMA TECHNOLOGIES
Modern Cancer therapy Search for Immunomodulators•Sham Diwanay• Dr. Bhushan Patwardhan
PHARMA TECHNOLOGIES
Modern Cancer therapy Search for Immunomodulators•Sham Diwanay
Dr. Bhushan Patwardhan
Treatment with few selected test preparations resulted in :• Immunostimulatory activity in tumor-free animals receiving or not
receiving anticancer drugs.
• Protection from toxic side effects viz. myelo, immuno- suppression without compromising or interference with anticancer activity and this activity was dose dependent.
• Treatment with these candidate drugs will be important in development of supportive / adjuvant treatment to cancer therapy to avoid untoward effects.