In Vitro Antileishmanial, Trypanocidal, and Mammalian Cell Activities of Diverse N,N’ -Dihetaryl Substituted Diamines and Related Compounds.

In vitro antileishmanial, trypanocidal, and Mammalian cell activities of diverse n,n’ -dihetaryl substituted diamines and related compounds.

Sci Pharm. 2013 Mar; 81(1): 43-55
Leal SM, Amado DF, Kouznetsov VV, Escobar P

The leishmaniasis and Chagas diseases constitute a serious public health problem worldwide with few and ineffective treatment options. The search for new antiparasitic candidates at the initial steps of drug discovery and development is still necessary. The synthesis of 22 de novo synthetized N,N’-dihetaryl-alkyldiamine derivatives and in vitro antiparasitic activity were evaluated for the first time against intracellular and extracellular forms of Leishmania (Leishmania) infantum, L. (Viannia) panamensis, L. (Leishmania) amazonensis, and Trypanosoma cruzi. Additionally, the toxicity on mammalian cells was determined. Some of these substituted N,N’-diamines (25-35 % of the tested compounds) showed interesting results against free-living forms of parasites with activities at the inhibitory concentration (IC 50 ) level of 1.96 to 28.83 ?M for L. (L.) infantum promastigotes and IC50 of 0.02 to 5.31 ?M for T. cruzi epimastigotes. No activity at the IC50 level on intracellular amastigotes of T. cruzi was observed. However, N (1),N (2)-dibenzylethane-1,2-diamine 5a revealed an important activity against the intracellular amastigotes of L. infantum (IC50 25.42 ?M ±0.33) and L. panamensis (IC50 58.20 ?M ±3.23), while their analogue N(1),N(4) -dibenzylbutane-1,4-diamine 5c resulted in activity only against L. panamensis (IC50 11.19 ?M ±0.20) without toxicity on Vero and THP-1 mammalian cells. The active compounds against intracellular parasites with low toxicity in mammalian cells may be considered for future studies in experimental models. HubMed – drug


Anti-counterfeit technologies: a pharmaceutical industry perspective.

Sci Pharm. 2013 Mar; 81(1): 1-13
Bansal D, Malla S, Gudala K, Tiwari P

Growth of international free trade and inadequate drug regulation have led to the expansion of trade in counterfeit drugs worldwide. Technological protection is seen to be the best way to avoid this problem. Different technologies came into existence like overt, covert, and track and trace technologies. This review emphasises ideal technological characteristics, existing anti-counterfeit technologies, and their adoption in different countries. Developed countries like the USA have implemented RFID while the European trend is towards 2D barcodes. The Indian government is getting sensitised about the extent of the problem and has formulated rules mandating barcodes. Even the pharmaceutical companies have been employing these technologies in order to detain illegitimate drugs in their supply chain. HubMed – drug


Identification of plumbagin and sanguinarine as effective chemotherapeutic agents for treatment of schistosomiasis.

Int J Parasitol Drugs Drug Resist. 2013 Dec; 3: 28-34
Zhang SM, Coultas KA

Schistosomiasis, a snail-borne parasitic disease, affects more than 200 million people worldwide. Currently the treatment of schistosomiasis relies on a single therapy of praziquantel, a drug developed over 30 years ago. Thus, there is an urgent need to develop alternative antischistosomal drugs. In the pursuit of novel antischistosomal drugs, we examined the antischistosomal activities of 45 compounds that had been reported to exhibit antimicrobial and/or antiparasitic activities. Two plant-derived compounds, plumbagin and sanguinarine, were found to possess potent antischistosomal activities in vitro. For both the compounds, a concentration of 10 ?M (equivalent to 1.88 ?g/ml for plumbagin and 3.68 ?g/ml for sanguinarine) resulted in 100% mortality at 48 h, which meets the World Health Organization’s (WHO) criterion of “hit” compounds for the control of schistosomiasis. Morphological changes and tegumental alterations of the dead worms treated by the two compounds were quite different. The significant morphological changes of worms after treatment by the two compounds suggest the two compounds target different biological pathways, both of which result in parasite’s death. This study provides evidence to suggest plumbagin and sanguinarine have real potential as effective alternative chemotherapeutic agents for the treatment of schistosomiasis. HubMed – drug


Pharmacist-led medication-related needs assessment in rural Ghana.

Springerplus. 2013 Dec; 2(1): 163
Wilby KJ, Lacey J

Access to both essential and non-essential medications is increasing worldwide. While increased drug access is a positive development, many countries lack the infrastructure for appropriate distribution, administration, and monitoring of drug therapy. The objective of this study was to assess medication and pharmacy-related needs in the rural Ashanti Region of Ghana and to determine barriers of achieving optimal health outcomes in this region. Qualitative domains and associated themes were identified by observations from integration into community culture and from conduction of semi-structured interviews with local community leaders, health workers, or those with knowledge of health-related issues. Eight semi-structured interviews were completed and four thematic domains were identified; access to care, resource shortages, medication safety, and education/training. Barriers and challenges identified under each thematic domain included (but were not limited to) availability of clean water sources, shortages of medications and diagnostic equipment, financial considerations, misunderstanding of medication indications and directions for use, and shortages of qualified pharmacy or dispensary staff. Most respondents also expressed a need for continuing education and training of healthcare personnel. It can be concluded that there is a need for development of health services related to medications. Locally supported interventions and future research should focus on barriers and challenges identified from the thematic domains. HubMed – drug