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Piper betel plants and 5 strains of medically important fungi were selected for this study. Antifungal susceptibility test was performed to screen the antifungal activity of this plant against the selected fungi. Piper betel showed to possess antifungal property against 4 out of 5 strains of the fungus. Solid Phase extraction (SPE) technique was applied to Piper betel to achieve initial separation of active antifungal compound in the form of methanol fractions. These fractions were tested for their antifungal property. Piper betel showed the best antifungal activity against A. flavus (Ref: Nazmul MHM, Rashid MA, Jamal H. Antifungal activity of Piper betel plants in Malaysia. Drug Discovery, 2013, 6(17), 16-17).

DRUG DISCOVERY OF THE MONTH

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Discovering antibiotics by newly developed revolutionary method

Brithvi V

Antibiotics are an essential part of modern medicine. Developing new antibiotics that target non-multiplying bacteria is another approach that may lead to drugs that reduce the emergence of antibiotic resistance and increase patient compliance by shortening the duration of antibiotic therapy. These new discovery routes have given rise to compounds that are in preclinical development, but, with one exception, have not yet entered clinical trials. For the time being, the majority of new antibiotics that reach the marketplace are likely to be structural analogues of existing families of antibiotics or new compounds; both natural and non-natural which are screened in a conventional way against live multiplying bacteria. The current methods have concentrated on compounds that target logarithmic multiplying bacteria. In developed countries, life expectancy increased each year, and the number of deaths caused by infectious diseases fell. Grant funding agencies reduced financial support for fundamental antibiotic research, believing that large pharmaceutical companies would fund antibiotic research. Many major pharmaceutical companies and large biotech companies left the antibiotic research and development arena. Antibiotics are short-course therapies that cure infections. Discovery of the new method is expected to broadly impact both basic and applied research tried to understanding, controlling or preventing bacterial cell growth in specific environments.

Drug Discovery, 2013, 6(16), 7

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FDA APPROVED DRUGS

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FDA approved drugs – August 2013

Brithvi V

Tivicay is specifically indicated in combination with other antiretroviral agents for the treatment of human immunodeficiency virus type 1 (HIV-1) infection in adults and children aged 12 years and older and weighing at least 40 kg. It is supplied as a tablet for oral administration.

Drug Discovery, 2013, 6(16), 8-9

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RESEARCH

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In-vivo actions of Methanolic extract of Lantana camara on the total protein and free aminoacids content in Culex mosquito larvae

Divya S Rajan

In the present study as the methanolic extract of Lantana camara showed significant toxicity,that extract was selected for the study of invivo action of Lantana camara extract on the total protein and free aminoacid content in the Culex mosquito larvae.In the laboratory condition, 85mg/100ml was found to be very effective in creating 100% mortality of the mosquito larvae.Fourth instar mosquito larvae was put in a lethal concentration of the extract and kept them for time periods such as 2,4 and 6 hours. The LD50 of methanolic extract of Lantana camara,with respect to the larvae and was almost found to be 40mg/100ml. Within this period, the larvae showed visible symptoms of toxicity such as lack of co-ordination of movements, incapability of surfacing to take oxygen and poor response to stimuli such as touching with glass rods.A very simple observation on the pH of the larval homogenate of control and drug treated larvae showed that the homogenate of normal larvae was alkaline (pH 7.1 to 7.2) but in treated and intoxicated larvae the pH of homogenate was slightly acidic (pH 6.8 to 6.9). The protein content of whole body on wet weight basis was more than 3%.On incubating mosquito larvae in lethal concentration of Lantana camara extract,there was a gradual increase of total free amino acid together with gradual decrease in protein content.The study indicated that at the sixth hour of incubation almost 1/3rd of protein was depleted and there was a 50% increase of aminoacid that together resulted in the death of the larvae.Thus the findings proved to suggest the use of the above information in future for the formulation of effective antilarvicidal agent from the invasive weed Lantana camara, that prevents the spreading of dreadful mosquito borne diseases.

Drug Discovery, 2013, 6(16), 10-12

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Antifungal activity of Piper betel plants in Malaysia

Nazmul MHM, Rashid MA, Jamal H

Piper betel plants and 5 strains of medically important fungi were selected for this study. Antifungal susceptibility test was performed to screen the antifungal activity of this plant against the selected fungi. Piper betel showed to possess antifungal property against 4 out of 5 strains of the fungus. Solid Phase extraction (SPE) technique was applied to Piper betel to achieve initial separation of active antifungal compound in the form of methanol fractions. These fractions were tested for their antifungal property. Piper betel showed the best antifungal activity against A. flavus.

Drug Discovery, 2013, 6(17), 16-17

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DRUG DISCOVERY OF THE MONTH

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Discovery of new drugs for bird-flu

Brithvi V

A gene mutation is known to make flu viruses resistant. Scientists have identified chemical agents that block the flu virus’s ability to replicate itself in cell culture. These novel compounds show promise for a new class of antiviral medicines to fight much-feared pandemic influenzas such as the looming “bird flu” threats caused by the H5N1 influenza A virus and the new H7N9 virus responsible for a 2013 outbreak in China. Arnold and his collaborators have been working to create drugs beyond Tamiflu, especially ones that target different parts of the virus, using an approach that helped in the development of powerful anti-AIDS drugs. By synthesizing chemical compounds that bind to metal ions in a viral enzyme, the researchers found they could halt that enzyme's ability to activate a key step in the virus's replication process. Researchers Joseph Bauman and Kalyan Das first produced high-resolution images of an H1N1 flu enzyme, and Bauman and postdoctoral researcher Disha Patel screened 800 small molecule fragments for binding. A research team of Chinese virologists and epidemiologists reported that they’ve discovered evidence that H7N9 is directly contagious among humans, but also determined that human-to -human transmissibility of the virus is as yet non-aggressive, lessening the likelihood, at least so far, that H7N9 will cause a global pandemic.

Drug Discovery, 2013, 7(18), 7

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FDA APPROVED DRUGS

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FDA approved drugs – September 2013

Brithvi V

BRINTELLIX
Generic Name : Vortioxetine;
Company : Lundbeck and Takeda Pharmaceuticals America, Inc. Approved by September 2013
Treatment for Major Depressive Disorder

Drug Discovery, 2013, 7(18), 8

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PERSPECTIVES

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Inter-arm Systolic Blood Pressure Difference of 15 mm Hg and its Relationship to CRP and other Cardiovascular Risk Markers

Neil K Agarwal, Shashi K Agarwal

Blood pressure is generally measured on in one arm – usually the non-dominant arm. However, increasing data suggests that arm to arm difference in blood pressure is common and may indicate atherosclerotic peripheral vascular disease. Other causes of inter-arm blood pressure difference include vasculitis, fibromuscular hyperplasia, connective tissue disorders, radiation arteritis, thoracic outlet compression, dissecting aortic aneurysm, and congenital abnormalities. Its presence is therefore not benign. The common etiology of this abnormality has been attributed to atherosclerosis involving the subclavian arteries. It also is a proxy for generalized atherosclerotic disease. A recent meta-analysis of 20 studies revealed that a systolic blood pressure difference of more than 15 mm Hg between the right and left arm was associated with a 2.5 greater risk of peripheral vascular disease, a 1.7 fold increase in cardiovascular mortality, and a 1.6 higher risk of all-cause death. Atherosclerosis is associated with vascular inflammation. CRP is a sensitive and reliable biomarker of this phenomenon and is frequently found elevated in patients with systolic inter-arm blood pressure difference.

Drug Discovery, 2013, 7(18), 9-12

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REVIEWS

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Multidrug resistant Staphylococcus aureus: A global challenge

There YW, Wadhai VS

Multidrug resistance is one of the serious problems faced by public health at the beginning of twenty first century. It is usually associated with significant morbidity, longer hospitalization, excess costs and mortality. Staphylococcus aureus is a common pathogen in hospital and community acquired disease that causes a wide range of infection such as skin and soft tissue infection to life threatening disease like respiratory tract infection, meningitis, endocarditis, bacteraemia, musculoskeletal infection and urinary tract infection. Approximately 90% of Staphylococcus strains are resistant to penicillin.

Drug Discovery, 2013, 7(18), 13-18

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