DR ANTHONY MELVIN CRASTO

DR ANTHONY MELVIN CRASTO

ORGANIC CHEMISTRY EDUCATION

ARAB MEDICINE- KHAT

ARAB MEDICINE- KHAT

Catha edulis

Khat (Catha edulis) is a flowering plant native to the Horn of Africa and the Arabian Peninsula. Among communities from these areas, khat chewing has a long history as a social custom dating back thousands of years.

Khat contains a monoamine alkaloid called cathinone, an amphetamine-like stimulant, which is said to cause excitement, loss of appetite and euphoria. In 1980, the World Health Organization (WHO) classified it as a drug of abuse that can produce mild to moderatepsychological dependence (less than tobacco or alcohol), although the WHO does not consider khat to be seriously addictive. The plant has been targeted by anti-drug organizations such as the DEA.It is a controlled substance in some countries, such as the United States, Canada and Germany, while its production, sale and consumption are legal in other nations, including Djibouti, Ethiopia, Somalia and Yemen.

 

Man chewing khat in Sana’a, Yemen, January 2009

Khat is a slow-growing shrub or tree that grows to between 1.4 m and 3.1 m tall, depending on region and rainfall. It has evergreenleaves 5–10 cm long and 1–4 cm broad. The flowers are produced on short axillary cymes 4–8 cm long. Each flower is small, with five white petals. The fruit is an oblong three-valved capsule containing 1–3 seeds. The seeds are samaras

Allegedly according to some sources, but disputed by others, khat’s exact place of origin is uncertain.One argument is that it was first grown in Ethiopia,with the explorer Sir Richard Burton suggesting that the plant was later introduced to Yemen from Ethiopia in the 15th century. He specifically mentions the eastern city of Harar as the birthplace of the plant.

However, amongst communities in the Horn of Africa (Djibouti, Eritrea, Ethiopia, Somalia) and the Arabian Peninsula, khat chewing has a long history as a social custom dating back thousands of years.

The Ancient Egyptians considered the khat plant a divine food, which was capable of releasing humanity’s divinity. The Egyptians used the plant for more than its stimulating effects; they used it for transcending into “apotheosis”, with the intent of making the user god-like.

The earliest known documented description of khat is found in the Kitab al-Saidala fi al-Tibb كتاب الصيدلة في الطب, an 11th century work onpharmacy and materia medica written by Abū Rayhān al-Bīrūnī, a Persian scientist and biologist. Unaware of its origins, al-Bīrūnī wrote that khat is:

a commodity from Turkestan. It is sour to taste and slenderly made in the manner of  batan-alu. But  khat is reddish with a slight blackish tinge. It is believed that  batan-alu is red, coolant, relieves biliousness, and is a refrigerant for the stomach and the liver.

In 1854, Malay writer Abdullah bin Abdul Kadir noted that the custom of chewing khat was prevalent in Al Hudaydah in Yemen

You observed a new peculiarity in this city – everyone chewed leaves as goats chew the cud. There is a type of leaf, rather wide and about two fingers in length, which is widely sold, as people would consume these leaves just as they are; unlike betel leaves, which need certain condiments to go with them, these leaves were just stuffed fully into the mouth and munched. Thus when people gathered around, the remnants from these leaves would pile up in front of them. When they spat, their saliva was green. I then queried them on this matter: ‘What benefits are there to be gained from eating these leaves?’ To which they replied, ‘None whatsoever, it’s just another expense for us as we’ve grown accustomed to it’. Those who consume these leaves have to eat lots of ghee and honey, for they would fall ill otherwise. The leaves are known as  Kad.”
 

 

khat contains Cathinone ,

or benzoylethanamine (marketed as hagigat in Israel), is amonoamine alkaloid found in the shrub Catha edulis (khat) and is chemically similar toephedrine, cathine and other amphetamines. Cathinone induces the release of dopaminefrom striatal preparations that are prelabelled either with dopamine or its precursors. It is probably the main contributor to the stimulant effect of Catha edulis. Cathinone differs from many other amphetamines in that it has a ketone functional group. Other amphetamines that share this structure include the antidepressant bupropion and the stimulantmethcathinone, among others.

Internationally, cathinone is a Schedule I drug under the Convention on Psychotropic Substances. Circa 1993, the DEA added cathinone to the Controlled Substances Act’s Schedule I.

The sale of khat is legal in some jurisdictions, but illegal in others — see Khat (Regulation). Synthetic cathinone is also often used as the key ingredient of recreational drug mixes commonly known as ‘bath salts’ in the United States.

Cathinone is structurally related tomethcathinone, in much the same way asamphetamine is related to methamphetamine. Cathinone differs from amphetamine by possessing a ketone oxygen atom (C=O) on the β (beta) position of the side chain. The corresponding alcohol compound cathine is a less powerful stimulant. The biophysiological conversion from cathinone to cathine is to blame for the depotentiation of khat leaves over time. Fresh leaves have a greater ratio of cathinone to cathine than dried ones, therefore having more psychoactive effects.

Cathinone can be extracted from Catha edulis, or synthesized from α-bromopropiophenone(which is easily made from propiophenone).

 

Pfizer, GSK form productivity pact with Singapore’s A*Star

 

Pfizer, GlaxoSmithKline and engineering giant Siemens have signed on as founding members of a new consortium set up by Singapore’s Agency for Science, Technology and Research (A*Star) to address challenges such as costs, regulatory compliance and processes to bring drugs from trials to markets.

READ ALL AT

http://www.pharmatimes.com/Article/13-06-21/Pfizer_GSK_form_productivity_pact_with_Singapore_s_A_Star.aspx

The Agency for Science, Technology and Research (AbbreviationA*STARChinese: 新加坡科技研究局) is a statutory board under the Ministry of Trade and Industry of Singapore. The Agency was established in 1991 to foster scientific research and talent for a knowledge-based Singapore.

 

Established in 1991 as the former National Science and Technology Board (NSTB), A*STAR was established with the primary mission to raise the level of science and technology in Singapore.[1]

 

Leadership

 

The current chairman of A*STAR is Mr. Lim Chuan Poh. He was formerly the Permanent Secretary (Education) and the Chief of Defence Force. Mr Lim took over the reins of A*STAR from Mr. Philip Yeo, who later became Chairman of SPRING Singapore, on 1 April 2007.[2]

 

The scientific leadership includes Tan Chorh Chuan, George RaddaSydney BrennerDavid Lane, Charles Zukoski and used to include Prof Low Teck Seng. Prof Low Teck Seng left A*Star on 19 July 2012 to join the National Research Foundation of the Prime Minister’s Office.

 

A*STAR Entities

 

The agency is made up of:

 

  • The Biomedical Research Council (BMRC) – Oversees public sector research activities in the biomedical sciences
  • The Science and Engineering Research Council (SERC) – Oversees public sector research activities in the physical sciences & engineering
  • The A*STAR Joint Council (A*JC) – Promotes and supports interdisciplinary collaborations between biomedical sciences, and physical sciences & engineering
  • The A*STAR Graduate Academy (A*GA) – Administers science scholarships and other manpower development programs
  • Exploit Technologies Pte Ltd (ETPL) – Manages the intellectual property created by research institutes in Singapore, and facilitates technology transfer to industry
  • The Corporate Group – Supports the rest of the organisation with finance, human resources, legal and other services

 

The agency oversees 14 biomedical sciences, and physical sciences and engineering research institutes, and six consortia & centre, which are located in Biopolis and Fusionopolis, as well as their immediate vicinity.

 

A*STAR supports Singapore’s key economic clusters by providing intellectual, human and industrial capital to its partners in industry. It also supports extramural research in the universities, hospitals, research centres, and with other local and international partners.

 

Research Institutes & Units

 

Biomedical Research Council

 

The Biomedical Research Council (BMRC) oversees 7 research institutes and several other research units that focus on both basic as well as translational and clinical research to support the key industry clusters in Biomedical Sciencespharmaceuticals, medical technology, biotechnology and healthcare services.

 

Having established a strong foundation in basic biomedical research capabilities, there is now an added focus on translating new knowledge and technologies created at the “benches” into new clinical applications for diagnosis and treatment that can one day be delivered at the “bedsides” of our hospitals and disease centres.

 

The research institutes and units under BMRC are:

 

 

The BMRC Research Institutes focus on building up core biomedical capabilities in the areas of bioprocessing; chemical synthesis; genomics and proteomics; molecular and cell biology; bioengineering and nanotechnology and computational biology. In addition, the Institute of Medical Biology (IMB) and Singapore Institute for Clinical Sciences (SICS) focus on translational and clinical research.

 

Science and Engineering Council

 

A*STAR’s Science and Engineering Research Council (SERC) promotes public sector research and development in the physical sciences & engineering.

 

SERC manages seven research institutes and several state-of-the art centres and facilities with core competencies in a wide range of fields including communications, data storage, materials, chemicals, computational sciences, microelectronics, advanced manufacturing and metrology to tackle global technological challenges and create future industries from its headquarters at Fusionopolis, Singapore’s iconic hub for science and technology research.

 

The research institutes and units under SERC are:

 

 

The seamless integration of the research institutes is key to addressing industry needs, which may span multiple disciplines. To this end, SERC’s broad range of capabilities are in a unique position to develop new technologies in areas such as automotives, aerospace, energy, electronic healthcare and medical technology, nanotechnology, photonics, sensors and sensor networks.

 

In July 2012, it was announced that A*STAR collaborates with Chinese language internet search provider Baidu to open a joint laboratory, called the Baidu-I2R Research Centre (BIRC), which aims to develop language processing technologies.[3]

 

Scholarships

 

Each year, the Agency gives out a number of scholarships and awards to young and aspiring scientists. These awards are meant to help Singapore achieve its goal of becoming a research hub by nurturing home-grown PhDs to serve both in the public sector and in industry. In 2008, a total of 101 scholarships were awarded to Bachelor of Science and PhD students who were to embark on their studies in overseas universities.[4] The administration of these awards are governed by the A*Star Graduate Academy, some of which are listed below:

 

  • National Science Scholarship (BS)
  • National Science Scholarship (PhD)
  • A*Star Graduate Scholarship
  • Singapore International Graduate Award (SINGA)
  • Singapore International Pre-Graduate Award (SIPGA)
  • A*Star Pre-Graduate Award
  • A*Star International Fellowship

 

References

www.a-star.edu.sg

 

Pfizer, GSK form productivity pact with Singapore’s A*Star

 

Pfizer, GlaxoSmithKline and engineering giant Siemens have signed on as founding members of a new consortium set up by Singapore’s Agency for Science, Technology and Research (A*Star) to address challenges such as costs, regulatory compliance and processes to bring drugs from trials to markets.

READ ALL AT

http://www.pharmatimes.com/Article/13-06-21/Pfizer_GSK_form_productivity_pact_with_Singapore_s_A_Star.aspx

The Agency for Science, Technology and Research (AbbreviationA*STARChinese: 新加坡科技研究局) is a statutory board under the Ministry of Trade and Industry of Singapore. The Agency was established in 1991 to foster scientific research and talent for a knowledge-based Singapore.

 

Established in 1991 as the former National Science and Technology Board (NSTB), A*STAR was established with the primary mission to raise the level of science and technology in Singapore.[1]

 

Leadership

 

The current chairman of A*STAR is Mr. Lim Chuan Poh. He was formerly the Permanent Secretary (Education) and the Chief of Defence Force. Mr Lim took over the reins of A*STAR from Mr. Philip Yeo, who later became Chairman of SPRING Singapore, on 1 April 2007.[2]

 

The scientific leadership includes Tan Chorh Chuan, George RaddaSydney BrennerDavid Lane, Charles Zukoski and used to include Prof Low Teck Seng. Prof Low Teck Seng left A*Star on 19 July 2012 to join the National Research Foundation of the Prime Minister’s Office.

 

A*STAR Entities

 

The agency is made up of:

 

  • The Biomedical Research Council (BMRC) – Oversees public sector research activities in the biomedical sciences
  • The Science and Engineering Research Council (SERC) – Oversees public sector research activities in the physical sciences & engineering
  • The A*STAR Joint Council (A*JC) – Promotes and supports interdisciplinary collaborations between biomedical sciences, and physical sciences & engineering
  • The A*STAR Graduate Academy (A*GA) – Administers science scholarships and other manpower development programs
  • Exploit Technologies Pte Ltd (ETPL) – Manages the intellectual property created by research institutes in Singapore, and facilitates technology transfer to industry
  • The Corporate Group – Supports the rest of the organisation with finance, human resources, legal and other services

 

The agency oversees 14 biomedical sciences, and physical sciences and engineering research institutes, and six consortia & centre, which are located in Biopolis and Fusionopolis, as well as their immediate vicinity.

 

A*STAR supports Singapore’s key economic clusters by providing intellectual, human and industrial capital to its partners in industry. It also supports extramural research in the universities, hospitals, research centres, and with other local and international partners.

 

Research Institutes & Units

 

Biomedical Research Council

 

The Biomedical Research Council (BMRC) oversees 7 research institutes and several other research units that focus on both basic as well as translational and clinical research to support the key industry clusters in Biomedical Sciencespharmaceuticals, medical technology, biotechnology and healthcare services.

 

Having established a strong foundation in basic biomedical research capabilities, there is now an added focus on translating new knowledge and technologies created at the “benches” into new clinical applications for diagnosis and treatment that can one day be delivered at the “bedsides” of our hospitals and disease centres.

 

The research institutes and units under BMRC are:

 

 

The BMRC Research Institutes focus on building up core biomedical capabilities in the areas of bioprocessing; chemical synthesis; genomics and proteomics; molecular and cell biology; bioengineering and nanotechnology and computational biology. In addition, the Institute of Medical Biology (IMB) and Singapore Institute for Clinical Sciences (SICS) focus on translational and clinical research.

 

Science and Engineering Council

 

A*STAR’s Science and Engineering Research Council (SERC) promotes public sector research and development in the physical sciences & engineering.

 

SERC manages seven research institutes and several state-of-the art centres and facilities with core competencies in a wide range of fields including communications, data storage, materials, chemicals, computational sciences, microelectronics, advanced manufacturing and metrology to tackle global technological challenges and create future industries from its headquarters at Fusionopolis, Singapore’s iconic hub for science and technology research.

 

The research institutes and units under SERC are:

 

 

The seamless integration of the research institutes is key to addressing industry needs, which may span multiple disciplines. To this end, SERC’s broad range of capabilities are in a unique position to develop new technologies in areas such as automotives, aerospace, energy, electronic healthcare and medical technology, nanotechnology, photonics, sensors and sensor networks.

 

In July 2012, it was announced that A*STAR collaborates with Chinese language internet search provider Baidu to open a joint laboratory, called the Baidu-I2R Research Centre (BIRC), which aims to develop language processing technologies.[3]

 

Scholarships

 

Each year, the Agency gives out a number of scholarships and awards to young and aspiring scientists. These awards are meant to help Singapore achieve its goal of becoming a research hub by nurturing home-grown PhDs to serve both in the public sector and in industry. In 2008, a total of 101 scholarships were awarded to Bachelor of Science and PhD students who were to embark on their studies in overseas universities.[4] The administration of these awards are governed by the A*Star Graduate Academy, some of which are listed below:

 

  • National Science Scholarship (BS)
  • National Science Scholarship (PhD)
  • A*Star Graduate Scholarship
  • Singapore International Graduate Award (SINGA)
  • Singapore International Pre-Graduate Award (SIPGA)
  • A*Star Pre-Graduate Award
  • A*Star International Fellowship

 

References

www.a-star.edu.sg

 

PLASTIC SURGERY-Breast Lift Surgery-mastopexy

PLASTIC SURGERY-Breast Lift Surgery-mastopexy

Breast lift, or mastopexy, surgery raises and firms the breasts by removing excess skin and tightening the surrounding tissue to reshape and support the new breast contour.

Breast lift procedure steps

What happens during breast lift surgery? Your mastopexy surgery can be achieved through a variety of incision patterns and techniques. The appropriate technique for you will be determined based on:

  • Breast size and shape
  • The size and position of your areolas
  • The degree of breast sagging
  • Skin quality and elasticity as well as the amount of extra skin

Step 1 – Anesthesia

Medications are administered for your comfort during breast lift surgery. The choices include intravenous sedation and general anesthesia. Your doctor will recommend the best choice for you.

Step 2 – The incision

There are three common incision patterns:

Around the areola, . note-pics deleted

Around the areola and vertically down from the areola to the breast crease

Around the areola, vertically down from the breast crease and horizontally along the breast crease

Step 3 – Reshaping your breasts

After your doctor makes the incisions:

  • The underlying breast tissue is lifted and reshaped to improve breast contour and firmness.
  • The nipple and areola are repositioned to a natural, more youthful height.
  • If necessary, enlarged areolas are reduced by excising skin at the perimeter.
  • Excess breast skin is removed to compensate for a loss of elasticity.

Step 4 – Closing the incisions

After your breasts are reshaped and excess skin is removed, the remaining skin is tightened as the incisions are closed.

Some incision lines resulting from breast lifts are concealed in the natural breast contours; however, others are visible on the breast surface. Incision lines are permanent, but in most cases will fade and significantly improve over time.

Sutures are layered deep within the breast tissue to create and support the newly shaped breasts. Sutures, skin adhesives and/or surgical tape may be used to close the skin.

Step 5 – See the results

The results of your breast lift surgery are immediately visible. Over time, post-surgical swelling will resolve and incision lines will fade.

Satisfaction with your new image should continue to grow as you recover and realize the fulfillment of your goal for breasts which have been restored to a more youthful and uplifted position.

FDA Approves Pediatric Indication for Astellas’ Mycamine (micafungin sodium) for Injection

FDA Approves Pediatric Indication for Astellas’ Mycamine (micafungin sodium) for Injection

File:Micafungin.svg

micafungin sodium

  • C56-H70-N9-O23-S.Na
     
    1292.265
     
    Fujisawa (Originator), Merck & Co. (Codevelopment)
     
    Antifungal Agents, ANTIINFECTIVE THERAPY, 1,3-beta-Glucan Synthase Inhibitors, Echinocandins
     
    Launched-2002

{5-[(1S,2S)-2-[(3S,6S,9S,11R,15S,18S,20R,21R,24S,25S,26S)-3-[(1R)-2-carbamoyl-1-hydroxyethyl]-11,20,21,25-tetrahydroxy-15-[(1R)-1-hydroxyethyl]-26-methyl-2,5,8,14,17,23-hexaoxo-18-[(4-{5-[4-(pentyloxy)phenyl]-1,2-oxazol-3-yl}benzene)amido]-1,4,7,13,16,22-hexaazatricyclo[22.3.0.09,13]heptacosan-6-yl]-1,2-dihydroxyethyl]-2-hydroxyphenyl}oxidanesulfonic acid

June 24, 2013 , Astellas Pharma US, Inc. (“Astellas”), a U.S. subsidiary of Tokyo-based Astellas Pharma Inc. (Tokyo: 4503), announced that the U.S. Food and Drug Administration (FDA) has approved its Supplemental New Drug Application (sNDA) for the use of MYCAMINE® (micafungin sodium) for injection by intravenous infusion for the treatment of pediatric patients four months and older with candidemia, acute disseminated candidiasis, Candida peritonitis and abscesses, esophageal candidiasis, and prophylaxis of Candida infections in patients undergoing hematopoietic stem cell transplants (HSCT).

http://www.drugs.com/newdrugs/fda-approves-pediatric-indication-astellas-mycamine-micafungin-sodium-3827.html

Micafungin (trade name Mycamine) is an echinocandin antifungal drug developed by Astellas Pharma. It inhibits the production ofbeta-1,3-glucan, an essential component of fungal cell walls. Micafungin is administered intravenously. It received final approval from the U.S. Food and Drug Administration on March 16, 2005, and gained approval in the European Union on April 25, 2008.

Micafungin is indicated for the treatment of candidemia, acute disseminated candidiasisCandida peritonitisabscesses andesophageal candidiasis. Since January 23, 2008, micafungin has been approved for the prophylaxis of Candida infections in patients undergoing hematopoietic stem cell transplantation (HSCT).

Micafungin works by way of concentration-dependent inhibition of 1,3-beta-D-glucan synthase resulting in reduced formation of 1,3-beta-D-glucan, which is an essential polysaccharide comprising one-third of the majority of Candida spp. cell walls. This decreased glucan production leads to osmotic instability and thus cellular lysis

  • Micafungin sodium, FK-463, Mycamine, Funguard,208538-73-2

  • The synthesis of FK-463 can be performed as follows: The enzymatic deacylation of FR-901379 with Streptomyces anulatas No. 4811, S. anulatas No. 8703, Streptomyces strain No. 6907 or A. utahensis IFO13244 gives the deacylated lipopeptide FR-179642 (1), which is then reacylated with 1-[4-[5-(4-pentyloxyphenyl)isoxazol-3-yl]benzoyl]benzotriazole 3-oxide (VI) by means of dimethylaminopyridine (DMAP) in DMF. The acylating compound (VI) can be obtained as follows: The cyclization of 4-pentyloxyphenylacetylene (I) with 4-(hydroxyiminomethyl)benzoic acid methyl ester (II) by means of triethylamine in hot THF gives 4-[5-(4-pentyloxyphenyl)isoxazol-3-yl]benzoic acid methyl ester (III), which is hydrolyzed with NaOH in hot THF/water yielding the corresponding free acid (IV). Finally, this compound is condensed with 1-hydroxybenzotriazole (V) by means of 1-ethyl-3-[3-(dimethylamino)propyl]carbodiimide (EDMCA) in dichloromethane.
     
    Fromtling, R.A.; Castr, Drugs Fut 1998, 23, 12, 1273
     
     
    The synthesis of FK-463 can be performed as follows: The enzymatic deacylation of FR-901379 with Streptomyces anulatas No. 4811, S. anulatas No. 8703, Streptomyces strain No. 6907 or A. utahensis IFO13244 gives the deacylated lipopeptide FR-179642 (1), which is then reacylated with 1-[4-[5-(4-pentyloxyphenyl)isoxazol-3-yl]benzoyl]benzotriazole 3-oxide (VI) by means of dimethylaminopyridine (DMAP) in DMF. The acylating compound (VI) can be obtained as follows: The cyclization of 4-pentyloxyphenylacetylene (I) with 4-(hydroxyiminomethyl)benzoic acid methyl ester (II) by means of triethylamine in hot THF gives 4-[5-(4-pentyloxyphenyl)isoxazol-3-yl]benzoic acid methyl ester (III), which is hydrolyzed with NaOH in hot THF/water yielding the corresponding free acid (IV). Finally, this compound is condensed with 1-hydroxybenzotriazole (V) by means of 1-ethyl-3-[3-(dimethylamino)propyl]carbodiimide (EDMCD) in dichloromethane.
  • 38th Intersci Conf Antimicrob Agents Chemother (Sept 24 1998, San Diego)1998,:Abst F-145

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