Current opinion on an emergence of drug resistant strains of Plasmodium falciparum through genetic alterations

Kanchymalay, Kasturi; Mallika, Donepudi Siva; Amos, Seelam Jeevan; Venkateshaiah, Pavithra; Rao, Krs Sambasiva

doi:10.6026/97320630081114

Cited by 5 publications

(3 citation statements)

References 25 publications

(28 reference statements)

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“…The situation is becoming adverse with the rising problem of resistance to the present antimalarial drugs (Kasturi et al, 2012). At present where there is no malaria vaccine, chemotherapy is the main remedy for the management of malaria.…”

Section: Introductionmentioning

confidence: 99%

Antiplasmodial activity of aqueous extract ofBerberis aristataroots againstPlasmodium berghei-infected BALB/c mice

Chandel

Bagai

Semwal

et al. 2015

Pharmaceutical Biology

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Context: The rising problem of resistance to present antimalarial drugs stresses the need to look for newer antiplasmodial components with effective modes of action. The roots of Berberis aristata DC. (Berberidaceae) are used in the traditional medicine for malaria in various parts of India. Objective: The objective of this study was to evaluate antiplasmodial activity of B. aristata roots extract for the validation of its traditional medicinal use. Material and methods: Aqueous root extract of Berberis aristata (AREBA) was screened for its in vitro as well as in vivo antiplasmodial activity against lethal rodent malaria parasite Plasmodium berghei NK65. In vitro activity was evaluated against schizont maturation of P. berghei using various concentrations ranging from 1 to 100 mg/mL. For in vivo studies, AREBA at the doses of 150, 250, 350, and 650 mg/kg/d was administered to P. berghei infected BALB/c mice orally for 4 consecutive days (D0-D3). Results: AREBA showed in vitro antiplasmodial activity with an IC 50 value of 40 mg/mL. In vivo studies demonstrated a variable dose-dependent chemosuppression with higher efficacy at lower doses. At a dose of 350 mg/kg/d, the suppressive and preventive activities were found to be 67.1% and 53.9%, respectively, followed by enhancing mean survival period up to 12.8 d for the curative assay versus 7.5 d for the untreated mice. Discussion and conclusion: These results provide relevant scientific evidences for the traditional medicinal use of this plant as malaria remedy and further advocates the isolation and characterization of active antiplasmodial principle from this plant.

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Section: Introductionmentioning

confidence: 99%

Antiplasmodial activity of aqueous extract ofBerberis aristataroots againstPlasmodium berghei-infected BALB/c mice

Chandel

Bagai

Semwal

et al. 2015

Pharmaceutical Biology

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“…The emergence of new drug-resistant strains of Plasmodium against almost all available antimalarial agents makes the situation more worsen and challenging. [34] So monitoring the efficacy of different antimalarial drugs in a regular interval and identification of new antimalarial agents are two important aspects of fight against malaria. There are four different methods to determine the antimalarial drug efficacy – in vivo therapeutic efficacy studies, in vitro tests, molecular marker studies, and measurement of drug concentrations.…”

Section: Introductionmentioning

confidence: 99%

Drug susceptibility testing methods of antimalarial agents

Maji¹

2018

Trop Parasitol

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Resistance to almost all available antimalarial agents, particularly for Plasmodium falciparum, is an important issue throughout all malaria endemic countries. Recently, Plasmodium vivax also showed resistance to chloroquine in some part of the World. Monitoring efficacy of used antimalarial drugs plays an important role to determine the emergence of resistant power by the prevailing parasite population of a geographical area if any. There are four different methods for antimalarial drug efficacy study. In vivo therapeutic efficacy study remains the gold standard and provides primary data for formulating antimalarial drug policy by the National Malaria Control Programmes. Several in vitro assay methods for assessing antimalarial drug susceptibility have been developed during past few decades. These assay methods are simple, easier to handle and allow early detection of drug-resistant parasites and also for the screening of different newly developed agents for their antimalarial activity. Approaches of different assay methods for testing the susceptibility of antimalarial agents and their limitations are discussed in this review article.

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“…More than 200 million cases of malaria were reported in 2012, and the emergence of new drug-resistant strains of Plasmodium makes the situation more critical and alarming (1,2). Chemoresistance, drug monotherapies, the easy availability of substandard drugs, and genetic polymorphism are some of the major causes of parasite drug resistance (3,4).…”

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confidence: 99%

Assessment of SYBR Green I Dye-Based Fluorescence Assay for Screening Antimalarial Activity of Cationic Peptides and DNA Intercalating Agents

Bhatia

Gautam

et al. 2015

Antimicrob Agents Chemother

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bThe SYBR green I (SG) dye-based fluorescence assay for screening antimalarial compounds is based on direct quantitation of parasite DNA. We show that DNA-interacting cationic cell-penetrating peptides (CPPs) and intercalating agents compete with SG dye to bind to DNA. Therefore, readouts of this assay, unlike those of the [ 3 H]hypoxanthine incorporation assay, for the antimalarial activity of the above DNA binding agents may be erroneous. In the case of CPPs, false readouts can be improved by the removal of excess peptides. Malaria continues to be a major public health problem in the 21st century. More than 200 million cases of malaria were reported in 2012, and the emergence of new drug-resistant strains of Plasmodium makes the situation more critical and alarming (1, 2). Chemoresistance, drug monotherapies, the easy availability of substandard drugs, and genetic polymorphism are some of the major causes of parasite drug resistance (3, 4). Thus, it is imperative to identify new antimalarial agents. For antimalarial drug screening, the [ 3 H]hypoxanthine incorporation assay has been a gold standard (5), while parasite lactate dehydrogenase (pLDH)-(6) and histidine-rich protein II-based (7) assays are other widely used methods. However, these assays are expensive and involve multistep procedures and thus are difficult to utilize for highthroughput screening (8, 9). The SYBR green I (SG) dye-based fluorescence assay is a recently developed high-throughput screening method which has been reported to be as sensitive as the [ 3 H]hypoxanthine incorporation assay (8, 10). It has been extensively validated and compared with other known methods and is commonly used for high-throughput antimalarial drug screening (9,(11)(12)(13).Peptides and DNA intercalating agents have been widely tested for their antimalarial activity (14-17). Some cell-penetrating peptides (CPPs), e.g., TP10 (18), and a number of DNA intercalators have been shown to have antimalarial activity (16,17). Interestingly, it has been demonstrated that CPPs, like Tat, penetratin, and TP10, are efficient agents for the delivery of bioactive molecules across the plasma membrane barrier (19). It has also been shown that CPPs move to the nucleus and bind to the target DNA, forming peptide-DNA complexes (20, 21). Since SG dye, CPPs, and intercalating agents bind to DNA, the aim of the present study was to evaluate the suitability of an SG dye-based fluorescence assay for determining the antiplasmodial activity of DNA binding agents. CPPs, Tat, penetratin, TP10, P3, P8 (19,22), and control peptides (Table 1) were chemically synthesized (USV, Mumbai, India) with more than 95% purity. TP10 is a broad-spectrum antiparasitic CPP (18), while Tat has been shown to be nontoxic (at 50 M) to Plasmodium parasites (23). Synchronized Plasmodium falciparum 3D7 cultures at 2% parasitemia and 2% hematocrit were lysed (10) and treated with various concentrations (6.25 M to 100 M) of Tat, penetratin, TP10, and control peptides (control cyclic peptide [CP1] and control linear pe...

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Current opinion on an emergence of drug resistant strains of Plasmodium falciparum through genetic alterations

Cited by 5 publications

References 25 publications

Antiplasmodial activity of aqueous extract ofBerberis aristataroots againstPlasmodium berghei-infected BALB/c mice

Antiplasmodial activity of aqueous extract ofBerberis aristataroots againstPlasmodium berghei-infected BALB/c mice

Drug susceptibility testing methods of antimalarial agents

Assessment of SYBR Green I Dye-Based Fluorescence Assay for Screening Antimalarial Activity of Cationic Peptides and DNA Intercalating Agents

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