# Presentation: 884133

## Using Space to EnhanceNature’s Pharmacy

**	****Since  the  dawn  of  civilization,  plants  have  been  used  as  a  natural  healing **
**therapeutic.  Today,  most  pharmaceuticals  and  75%  of  all  new  drug  discoveries  are still derived  from  natural  sources,  many  of  which  include  plants  from  the  rain  forest. **

**One such tropical plant, called Vinca, produces**
**vinca alkaloids which are used in cancer chemo-**
**therapy.  Space offers a unique environment in which to grow these plants for enhanced pharmaceutical production.  Previous space experiments have shown that plants adapt**
**to space by producing less **
**structural components (lignin)**
**necessary to support their**
**weight.  With less energy and **
**materials going into struc-**
**tural components, greater**

**Earth**

**Space**

**Bioserve Space Technologies and Bristol-Myers Squibb flew Vinca plants on Shuttle flight STS-77. Compare before and after shots of Vinca grown for 8 days in space.**

**production of secondary metabolites (pharmaceuticals**
**like vinca alkaloids) should occur. Data gathered from space results could lead to methods of enhancing plants **
**used for pharmaceuticals on the ground. Increased plant supplies could significantly reduce drug costs.**

- Searching for new plants with pharmaceutical properties.

*Using Space to Enhance**Nature’s Pharmacy*

## Characterizing Bone Growth and Immune Systems in Microgravity

***IMMUNE***

***Characterizing Bone Growth and Immune Systems in Microgravity***

**BioServe Space Technologies and Chiron Inc. have conducted several experiments aboard the SPACEHAB mission using an animal enclosure module to both collect data and test several types of candidate drugs.  Results to date of drugs tested in the ****IMMUNE**** series are very promising toward development of future treatments for Osteoporosis.**

**Researchers in space monitor **
**both immune and skeletal systems**

**IMMUNE hardware **
**.**

## New anti-parasite drug?

*New anti-parasite drug?*

**               ****Over a       billion of  mostly third world people are infected with a   **
**       ****roundworm known as ascarids.  Ascarids are tiny parasites that infect       **
**  ****the intestinal tract of vertebrates. Movement of the larvae into the brain or other parts of the body can prove fatal.  Space-based research is providing new hope in   **
**     ****combating  these parasitic worms. Ascarids are dependent upon a substance  **
**        ****known as malic enzyme to regulate**
**               ****certain bodily functions.  A **
**                       ****new drug designed to**
**                          ****interfere with normal **
**                             ****functioning of  malic**
**                                      ****enzyme should **
**                                          ****prove deadly**
**                                              ****to ascarids.**
** **
** ****Y**

**For over two**
**years, Upjohn **
**had been stymied in**
**its efforts to produce**
**malic enzyme crystals **
**of  the  quality needed to **
**determine its structure for **
**drug design.The Center for **
**Macromolecular Crystallography,**
**along with the University of North **
**Texas have since grown malic enzyme **
**crystals on the USML-1 Spacelab mission. **
**Although these crystals proved to be smaller **
**than ground based ones, they were more perfectly **
**formed, therefore producing better data for drug design. **

## Light Emitting Diodes...a new Cancer Treatment

***Light Emitting Diodes******...a new Cancer Treatment***

**To treat a wide variety of cancers (including cancers of the brain, **
**skin, esophagus, bladder, lung and eye) light activated, tumor killing**
**drugs are injected.  These drugs accumulate in the rapidly growing**
**tumor. The LED light activates the drug in the tumor while sparing the non-cancerous parts of the body.**

**Lasers, which have traditionally been used in this therapy, are more expensive, less effective and can cause ancellary damage.**

**Status: **
*** FDA approved Phase I **
**   ****clinical trial.**
*** FDA approval for**
**   **_**in vitro,**_** and **_**in vivo**_** **
**   ****protocols from**
**   ****Pharmacyclics, Inc.**
*** Recent LED publication **
**   ****in **_**NeuroSurgery**_**.**

**The LED probe,**
**developed by the Wisconsin Center**
**for Space Automation and Robotics, is **
**more reliable and less expensive than the current laser source.**

**High intensity light emitting diodes were developed for space plant  research   (shown right).  They use less power and produce less unwanted heat.**

## Fighting Diabetes in Space

**Diabetes is a very serious disease that can lead to blindness, heart attack, stroke and kidney failure.  It is the fourth leading cause of disease in the US, killing more than 160,000 Americans each year.**

**Although there is no cure for diabetes,  maintaining the right level of insulin in the blood can  permit a near normal life.  Exciting new data from space may **
**help  to  develop drugs to maintain the proper level in the bloodstream  longer. **

**Lacking in the arsenal of medications to fight the ravages of diabetes is a very long acting formulation of insulin.  Recent efforts have focused on binding insulin molecules together to slow their release in the diabetic patient’s bloodstream.  Candidate linking molecules have proven effective in the laboratory but are known to be toxic to patients.  On STS-60, crystals of insulin bound together with the linking molecule (right) grew larger than their **
**earth-grown counterparts.  **
**Space grown crystals enabled **
**researchers to clearly **
**determine why the toxic effect **
**occurred.  This information  **
**may enable the design of a **
**nontoxic new linking molecule **

**with the desired time release effect.  This advance may allow **
**patients to receive injections of insulin much less frequently.**

**computer image of human insulin generated from crystals grown in space**

**Crystals grown by The Center for Macromolecular Crystallography and the Hauptman-Woodward Medical Research Center,Inc.**** **

*Fighting Diabetes in Space*

## Flu Remedy Coming Soon from Research in Space

- <date/time>

**                 ****Influenza affects 20 to 40 million people and results in some 20 thousand deaths annually in the US, but relief is on the way!**

**The loss of productivity due to flu  is staggering.  Costs range as much as $20 billion/year.**
**High  mutation rates of the flu virus have hindered development of new drugs or vaccines.**
**But new data from  protein crystals grown in space and on earth have unlocked the secret of the flu bug and revealed its Achilles heel! **
**The  secret  lies in a small molecule which is attached to  the host cell’s surface. Each flu virus, no matter what strain, must remove this small molecule to escape the host cell  to spread infection.  **

**Using data from space and earth grown crystals, researchers from the Center of Macromolecular Crystallography  (CMC)  are designing drugs (keys) to bind with this protein’s active site (lock).**
** **
**This lock and key fit reduces the spread of flu in the body by blocking its escape route.**
**In collaboration with its corporate partner, the CMC has refined  drug structure in preparation for clinical trials.**
**Tested and approved  relief is expected to reach drugstores by 2004.**

**Three Dimensional Protein Structure reconstructed from x-ray crystallography image.**

***Flu Remedy Coming Soon from Research in Space***

## Open Heart Surgery

- <date/time>

***..made  easier  from  drugs  designed  using  ******crystals  grown in Space   ***

**Open heart surgery offers hope for a new lease on life, but the trauma caused by the surgery itself often triggers  massive inflammation.  This is because the immune system, which fights external factors, overreacts.  Factor D  is the protein which plays a key role in the biological steps that activate this immune response.**

**By  blocking the natural action**
**of Factor D, the immune sys-**
**tem is prevented from inap-**
**propriately running “out of**
**control,” allowing the patient **
**to recover more rapidly.**
**To know how to block this**
**protein,  detailed data about its**
**3-D structure is needed****.**

**Factor D crystals grown**
**in space were used to determine this 3-D structure.**
**This data from crystals grown in space allowed **
**researchers to develop inhibitors which**
**specifically  block Factor D’s active site.**

**Factor D blockers, with their great potential to alleviate the complication of inflammation associated with heart surgery, are now being developed for clinical trials.  This work is being spearheaded by The Center for Macromolecular Crystallography together with its corporate partner.  These new drugs, developed from space research, should be commercially**
** ****available as soon as 2001! **

**Shown above is the reconstructed 3-D structure of Factor D determined from  crystals grown in space.**

***Open Heart Surgery***

## CONTACT LENSES FROM SPACE

- <date/time>

**Paragon Vision Sciences and Langley Research Center are conducting  polymer research **
**in space for improved semi-rigid contact lenses.**
**Of the 51 million contact lens wearers in the world, 12 million must wear semi-rigid contact lenses*****.  *****Soft lenses are known for their comfort. However, they are not durable, can tear and have greater risk of biological contamination.  Hard lenses are more durable but cause eyes to dry out. Unfortunately, ****semi-rigid lenses with the comfort and breathability of soft lenses do not exist.**

**Samples prepared in space are**** more uniform and porous****. This allows oxygen to pass through easier**.** **
**Results from space may be used to develop a *****new breed  of rigidified contact  lenses. *****These lenses may not only  be more durable and more comfortable, but may “breathe” better, ****enabling long-term, comfortable, low-risk use.**

**Because of gravity, the material used for polymer research on Earth has settled to the bottom. In space, this same material remains dispersed, resulting in a better material to make contact lenses.**

**T h e    E y e s    H a v e    I t**

***CONTACT LENSES FROM SPACE***

## Searching for Drugs to fight Bone Loss

- <date/time>

**• ****BioServe Space Technologies and Chiron Inc.                     have conducted several space experiments.****	**
**• ****The resulting**** drugs ****will not only ****counter bone loss on Earth ****but will also**** ****aid long term human  spaceflight.**

***Osteoporosis is a serious concern to post-menopausal women,***
***the annual US cost is $3.8B***

***Searching for Drugs to fight ******Bone Loss***

**The **
**yellow **
**areas show**
**bone growth **
**that occurred in space.**

**•**** ****Osteoporosis decreases bone mass ****resulting in fragile                    ****	****bones which can break easily.****  This changes ****is ****mimicked ****	****and accelerated in the space environment.**
**• ****Space is used to test ****candidate drugs****,  assisting the  ****	****	****development of new drugs. **

## Longer  Lasting  Drugs  from  Space

***Longer  Lasting  Drugs  from  Space***

***Alpha- Interferon ***
**is a  drug used  to**
**treat a  number  of **
**diseases  including  hairy**
** ****cell leukemia,  multiple  myeloma, **
**AIDS-related  Kaposi’s sarcoma  and**
** ****chronic  hepatitis B and C.    The current**
** ****formulation  of the  *****drug  made  on  Earth  doesn’t ***
***last very long  in  the  bloodstream  and  requires  the***
*** ******patient  to  take  frequent doses.     *****However,  a  formulation**
** ****of the  drug using  alpha-interferon *****crystals  grown  in space ***
***works  in  the  bloodstream  four  to  six  times  longer.***

**Shown in the**
**background **
**are crystals of **
**Alpha-I- Interferon **
**grown  on  STS-52  by the **
**Center for  Macromolecular **
**Crystallography,  a  NASA **
**Commercial  Space  Center.   These **
**space-grown  crystals  are  larger  and **
**have  a  more  perfect  crystalline  structure **
**than  their  Earth-grown  counterparts .     This**
**better  structure  results  in  a  more  stable  crystal **
**which  dissolves  slower  when  put  into  the  bloodstream.  **
**As  a  result,  the   drug  lasts  longer  at  a  more  consistent concentration.**