Do you know what these plants are?

1. Do you know what these plants are?

2. BANABA • 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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4. Guava leaves • 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.

5. What do these two have in common? They are both painkillers

6. Both are sources of pain killers!!! Aspirin Prialt- nonopioid painkiller

7. Designing Medicines Taking Hints from Nature and Beyond Lourdes L. Herold, Ph.D.

8. Purpose • How chemists make new drugs in the lab that imitates the effects of plants and animals • From nature -> lab -> synthetic medicine

9. Why not just isolate medicine from plants • Reason the active ingredients come in very small amounts in natural sources

10. Taxol-from bark to anticancer pills • Observe how animals react to certain plants or organisms. • Isolate the active ingredient. • Identify their structure. • Make them in the lab.

11. Prialt (ziconotide) – finding hints from snails • Baldomero Olivera heard stories of the deadly effects of cone snail species Conus magusas 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-Cys-Ser-Arg-Leu-Met-Tyr-Asp-Cys-Cys-Thr-Gly-Ser-Cys-Arg-Ser-Gly-Lys-Cys-NH2 • Blocks calcium channels in nerve transmitting cells

12. Prialt • How many times stronger than morphine? 1000 times • How long did it take to finally get it in the market? More than 40 years. • 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.

13. Organic Chemistry-study of carbon containing compounds

14. Most drugs are organic compounds • Organic compounds - • made up of mostly C attached to one another forming short or long chains. • Carbons are attached to H and may also bond to O, N, S, P or halogens (Cl,Br,F) • They have functional groups. • Functional groups - • atoms attached together that work as one unit and defines how molecule works.

15. How aspirin is made

16. How better versions are made • Challenge in drug design • Strength • Safety • Commerciability • Know how the drug works in the first place • Find out what part in the molecule makes it work

17. Enzymes – make reactions in the body to go faster • Enzymes are proteins. • It has an active site –place where substrates attaches to enzyme resulting in a reaction

18. Let us take a break – • Three persons • Three keys • Which key will open the box

19. Lock and Key Model - Rigid model on how enzyme and substrate interact • The substrate- key • Enzyme is lock. • 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.

20. Size 9 right foot print in the sand- better model • 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.

21. Example of tweaking a molecule- Designing a better form of morphine – less addictive • 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.

22. Structure-Based Drug Design- use of competitive inhibition • 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. • Growth of an invading bacterium is inhibited or the synthesis of particular molecule is turned off.

23. HIV Protease Inhibitor • 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.

24. AZT (drug for HIV) mimics thymidine • 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 )

25. Virtual drug screening- computers make life easier for organic chemists • Quantitative Structure Activity Relationships (QSAR) • Instead of screening actual drug candidates, computer simulations are used. • Saves time and money

26. Interested to be a chemist? • What they do: • 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: • Likes to solve problems • Curious • Likes science and mathematics • Patient • Accurate • Open minded • Questioning

27. Different types of chemists • Organic Chemist • Analytical Chemist • Inorganic Chemist • Physical Chemist • Biochemist

28. Research I worked on • 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 • Developed methods for analyzing ditropan. • Attempted isolating active ingredients in ampalaya • Gene Therapy – finding lipidic vehicle to deliver good genes to replace bad ones.

29. IUP (Indiana University of Pennsylvania)

30. Thank you. Questions??

31. Comments on my talk I wrote after. • 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.