Encapsulation of podophyllotoxin and etoposide in biodegradable poly-<scp>d</scp>,<scp>l</scp>-lactide nanoparticles improved their anticancer activity

Yadav, Ramdhan; Kumar, Dharmesh; Kumari, Avnesh; Yadav, Sudesh Kumar

doi:10.3109/02652048.2013.834988

Cited by 30 publications

(18 citation statements)

References 54 publications

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“…The least toxic was convallatoxin, with 100% viability at 5μM; the most toxic was vincristine, with a CC50 of 0.04μM (Figure 4B and Table 2). The CC50 values reported here are similar to previously published results in diverse cell systems using different toxicity assays (Cereser et al, 2001a; Chen et al, 2004; Davenport et al, 2014; Li et al, 2012; Pan et al, 2013; Tran et al, 2012; Yadav et al, 2014). …”

Section: Resultssupporting

confidence: 90%

Development of a high-content screen for the identification of inhibitors directed against the early steps of the cytomegalovirus infectious cycle

et al. 2015

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Human cytomegalovirus (CMV) is a latent and persistent virus whose proliferation increases morbidity and mortality of immune-compromised individuals. The current anti-CMV therapeutics targeting the viral DNA polymerase or the major immediate-early (MIE) gene locus are somewhat effective at limiting CMV-associated disease. However, due to low bioavailability, severe toxicity, and the development of drug resistant CMV strains following prolonged treatment, current anti-CMV therapeutics are insufficient. To help address this shortfall, we established a high-content assay to identify inhibitors targeting CMV entry and the early steps of infection. The infection of primary human fibroblasts with a variant of the CMV laboratory strain AD169 expressing a chimeric IE2-yellow fluorescence protein (YFP) (AD169IE2-YFP) provided the basis for the high-content assay. The localization of IE2-YFP to the nucleus shortly following an AD169IE2-YFP infection induced a robust fluorescent signal that was quantified using confocal microscopy. The assay was optimized to achieve outstanding assay fitness and high Z′ scores. We then screened a bioactive chemical library consisting of 2080 compounds and identified hit compounds based on the decrease of fluorescence signal from IE2-YFP nuclear expression. The hit compounds likely target various cellular processes involved in the early steps of infection including capsid transport, chromatin remodeling, and viral gene expression. Extensive secondary assays confirmed the ability of a hit compound, convallatoxin, to inhibit infection of both laboratory and clinical CMV strains and limit virus proliferation. Collectively, the data demonstrate that we have established a robust high-content screen to identify compounds that limit the early steps of the CMV life cycle, and that novel inhibitors of early infection events may serve as viable CMV therapeutics.

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Section: Resultssupporting

confidence: 90%

Development of a high-content screen for the identification of inhibitors directed against the early steps of the cytomegalovirus infectious cycle

et al. 2015

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“…Meanwhile, physiologically stable and biocompatible nanoscale polyethylene glycolylated graphene oxide or stearic acid‐ g ‐chitosan oligosaccharide micelles have been employed as nanocarriers for 1 to improve the water solubility and drug efficacy of this compound and its analogues . Given their small size, slow release, and low cytotoxicity, 1 / 60 ‐loaded poly‐ d,l ‐lactide nanoparticles are a promising candidate for further development of nanochemotherapeutic anticancer drugs . Compound 60 conjugated with the nontoxic bioenhancer 4‐ethyl 5‐(3,4‐methylenedioxyphenyl)‐2 E ,4 E ‐pentadienoic acid piperidide has a 2.32‐fold higher oral bioavailability compared with free 60 …”

Section: Future Prospectsmentioning

confidence: 99%

Recent Advances in the Chemistry and Biology of Podophyllotoxins

Xiang

Che

2017

Chemistry A European J

173

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Podophyllotoxin and its related aryltetralin cyclolignans belong to a family of important products that exhibit various biological properties (e.g., cytotoxic, insecticidal, antifungal, antiviral, anti-inflammatory, neurotoxic, immunosuppressive, antirheumatic, antioxidative, antispasmogenic, and hypolipidemic activities). This Review provides a survey of podophyllotoxin and its analogues isolated from plants. In particular, recent developments in the elegant total chemical synthesis, structural modifications, biosynthesis, and biotransformation of podophyllotoxin and its analogues are summarized. Moreover, a deoxypodophyllotoxin-based chemosensor for selective detection of mercury ion is described. In addition to the most active podophyllotoxin derivatives in each series against human cancer cell lines and insect pests listed in the tables, the structure-activity relationships of podophyllotoxin derivatives as cytotoxic and insecticidal agents are also outlined. Future prospects and further developments in this area are covered at the end of the Review. We believe that this Review will provide necessary information for synthetic, medicinal, and pesticidal chemistry researchers who are interested in the chemistry and biology of podophyllotoxins.

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“…It is mainly extracted from the leaves of Stevia rebaudiana (Bertoni) and is considered to be a good anti-diabetic drug as it regulates the concentration of glucose in blood by secreting more insulin [6]. Podophyllotoxin is an anticancer molecule and found in larger concentrations in the rhizome of American Mayapple [7]. Catechin and epicatechin polyphenols are present in most abundance in tea.…”

Section: Plants and Bioactive Compoundsmentioning

confidence: 99%

Nanotechnology: A Spark to the Use of Plant Origin Bioactive Compounds in Therapeutics

Yadav¹

2015

Single Cell Biol

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Encapsulation of podophyllotoxin and etoposide in biodegradable poly-d,l-lactide nanoparticles improved their anticancer activity

Cited by 30 publications

References 54 publications

Development of a high-content screen for the identification of inhibitors directed against the early steps of the cytomegalovirus infectious cycle

Development of a high-content screen for the identification of inhibitors directed against the early steps of the cytomegalovirus infectious cycle

Recent Advances in the Chemistry and Biology of Podophyllotoxins

Nanotechnology: A Spark to the Use of Plant Origin Bioactive Compounds in Therapeutics

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