Transcript Making Medicine

Do you know what these plants are?
BANABA
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Banaba tea can help detoxify the body
and protect the liver.
It helps in the treatment of urinary
tract infections
It helps to lower or normalize blood
sugar, even if you are prone to have
diabetes you can lower the risk by
drinking banaba tea everyday. It is
effective for this purpose because of
its ability to regulate blood sugar and
act in a way that is similar to insulin
Banaba tea produces a positive effect
of lowering trigyceride and LDL
cholesterol, which aid in weight loss!
Banaba tea can help in weight
reduction even without dietary
restrictions.
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Guava leaves
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Health benefits from drinking guava
leaves tea:
Helps in cases of Gastroenteritis, dysentery,
diarrhea and vomiting in cholera patient
Helps fight free radicals.
Helps to clean the kidney
If you have chicken pox, drinking 4 cups of
guava tea will make the chicken pox heal
faster and the skin will have less scarring.
Contain strong antibiotic effect
It is good in controlling diabetes
Good for constipation
Gargling with lukewarm tea can help
remedy swollen gums and oral ulcers.
Help relieves colds and bronchitis
Helps skin disorders because it is rich in
vitamin C.
What do these two have in
common?
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They are both painkillers
Both are sources of pain killers!!!
Aspirin
Prialt- nonopioid painkiller
Designing Medicines
Taking Hints from Nature and Beyond
Lourdes L. Herold, Ph.D.
Purpose
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How chemists make new drugs in the lab
that imitates the effects of plants and
animals
From nature -> lab -> synthetic medicine
Why not just isolate medicine from
plants
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Reason the active ingredients come in
very small amounts in natural sources
Taxol-from bark to anticancer pills
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Observe how animals
react to certain plants
or organisms.
Isolate the active
ingredient.
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Identify their structure.
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Make them in the lab.
Prialt (ziconotide) – finding hints
from snails
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Baldomero Olivera heard stories of
the deadly effects of cone snail
species Conus magus as a chlld
growing up in the Philippines.
He got a “hint” and worked on it at
University of Utah in the early 1980s
with Michael McIntosh who was
barely out of high school. Michael
discovered ziconotide.
It is a polypeptide made of amino
acids.
H-Cys-Lys-Gly-Lys-Gly-Ala-Lys-CysSer-Arg-Leu-Met-Tyr-Asp-Cys-CysThr-Gly-Ser-Cys-Arg-Ser-Gly-Lys-CysNH2
Blocks calcium channels in nerve
transmitting cells
Prialt
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How many times stronger than morphine? 1000 times
How long did it take to finally get it in the market? More
than 40 years.
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1960’s (idea started)
1980’s (active ingredient isolated and identified)
2004) FDA approved its sale under the name Prialt on December
28, 2004, and the European Commission on February 22, 2005.
Organic Chemistry-study of carbon containing
compounds
Most drugs are organic compounds
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Organic compounds 
made up of mostly C attached to one another forming short or long
chains.
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Carbons are attached to H and may also bond to O, N, S, P or halogens
(Cl,Br,F)
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They have functional groups.
Functional groups 
atoms attached together that work as one unit and defines how molecule
works.
How aspirin is made
How better versions are made
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Challenge in drug design
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Strength
Safety
Commerciability
Know how the drug works in the first place
Find out what part in the molecule makes it
work
Enzymes – make reactions in the
body to go faster
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Enzymes are proteins.
It has an active site –
place where
substrates attaches to
enzyme resulting in a
reaction
Let us take a break –
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Three persons
Three keys
Which key will open the box
Lock and Key Model - Rigid model
on how enzyme and substrate
interact
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The substrate- key
Enzyme is lock.
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The active site is the specific
region of the enzyme which
combines with the substrate.
It is the key hole of the lock
(enzyme)
Geometric shape of active
site must match geometric
shape of a substrate molecule.
Only the correctly sized key
(substrate) fits into the key
hole (active site) of the lock
(enzyme)
So only one compound fits the
lock?? Not true.
Size 9 right foot print in the
sand- better model
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All left feet and those greater
than size 9 will not fit.
But as long as it is right foot
and size nine, any foot will fit
not just one particular one.
More than one drug replaces
substrate rather than just one
as the lock and key model
thinks.
Example of tweaking a moleculeDesigning a better form of
morphine – less addictive
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Find certain functional groups of proper polarity
in right places that are responsible for activity.
Then make drugs with this specific active portion
with nonactive remainder of molecule.
Structure-Based Drug Design
- use of competitive inhibition
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Know the protein
structure, and/or its
binding site, and/or its
active ligand (possibly
bound to protein)
Find a new molecule that
changes the protein’s
activity
Drug prevents enzyme,
cell membrane or other
biological unit from
carrying out its chemistry.
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Growth of an invading
bacterium is inhibited or
the synthesis of
particular molecule is
turned off.
HIV Protease Inhibitor
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HIV protease – enzyme responsible for HIV replication.
Goal - find a drug that mimics the structure of the
substrate that fits the active site or is a HIV protease
inhibitor. The drug gets stuck to the binding site and
the usual substrate cannot come in and the enzyme
cannot function.
AZT (drug for HIV) mimics
thymidine
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Thymidine – one of
nitrogen bases that make
up DNA and RNA.
AZT (inhibits reverse
transcriptase , the
enzyme that HIV uses to
make a DNA copy of its
RNA )
Virtual drug screening
- computers make life easier for organic chemists
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Quantitative Structure
Activity Relationships
(QSAR)
Instead of screening
actual drug
candidates, computer
simulations are used.
Saves time and
money
Interested to be a chemist?
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What they do:
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Make new things (like drugs)
Analyze what is inside the substance (SOCO)
Find out what is happening in a reaction
Teach in universities and high schools
Qualities you need to be a chemist:
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Likes to solve problems
Curious
Likes science and mathematics
Patient
Accurate
Open minded
Questioning
Different types of chemists
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Organic Chemist
Analytical Chemist
Inorganic Chemist
Physical Chemist
Biochemist
Research I worked on
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Determine if “sapal” can be used as fertilizers
Determine DDT levels in human fat samples
Fluropyrole synthesis (similar to flurouracil or 5-FU,
anticancer drug)
Alpha beta unsaturated stannanes
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Developed methods for analyzing ditropan.
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Attempted isolating active ingredients in ampalaya
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Gene Therapy – finding lipidic vehicle to deliver good
genes to replace bad ones.
IUP (Indiana University of
Pennsylvania)
Thank you.
Questions??
Comments on my talk I wrote after.
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I did not show the first four slides since this usb did not work and the other one which I used did not have most the slides I added the
day before the talk.
Noticed however it was better to not have had those slides (see other usb) which included qualities of chemist slides, since I solicited
the answers from them. It was more interactive and class was paying attention.
Questions were: What plants do you know which have medicinal use? And for the other slide, what qualities does a chemist have? In
both cases I noted a more alive class. At the end since most of the questions were about the united states rather than chemistry I
asked them to give five things that they learned. They tried and did well stating things like organic cpds, functional groups without
coaching. I think I could have shown a list of all functional groups and then as an activity ask them to determine where they were in the
slide of the rxn to make aspirin. Another interactive approach.
They knew what an enzyme is from previous lecture from their teacher but I noted I had to coaxed from there what it had namely the
active site and also about the substrates’ role. They did answer them. Also I need to coax the idea of competitive inhibition.
It might have been better to dramatize competitive inhibition using a guy and two girls. I did use the metaphor but perhaps actual in
class drama would help. The plot would about a guy with a girl friend. But then another came along a girl with same qualities (inhibitor
or drug). He would be attracted to her and it becomes a competition and the presence of the other girl inhibits interaction with the
original girl (substrate).
Perhaps re-title the demerol morphine slide as tweaking the functional groups to get different effects. This emphasizes this point.
Re-title the competitive inhibition, as how drugs stop a bad process to occur.
Another thought: since my goal is to get them to consider chem as a career I wonder if I should have just developed a slide of different
careers in chemistry. What subjects are covered in college etc. I did one like that when I was at carlow univ. In this slide I decided to
entice them by showing one particular application namely drug design. It might have been more exciting to include csi type work for
example. My original intention in doing this is to do both: present so they learn chem and hopefully consider chem as career. A few
raised their hands when asked if they do consider it. But then again they might just be trying to be polite. I asked them before class
and I think only one did. There were some who are into computers. Perhaps they do not know what they want yet. They are seniors
who have had chem in their junior year. Elen masa, gelay’s tutor, the contact person was there during the talk. Ms annie the chem
teacher was not and I think she was taking care of elen’s class. Not sure why.