scholarly journals Tetraphenylethene-based highly emissive metallacage as a component of theranostic supramolecular nanoparticles

2016 ◽  
Vol 113 (48) ◽  
pp. 13720-13725 ◽  
Author(s):  
Guocan Yu ◽  
Timothy R. Cook ◽  
Yang Li ◽  
Xuzhou Yan ◽  
Dan Wu ◽  
...  
Keyword(s):  
Cancer Treatment ◽  
Self Assembly ◽  
Biologically Active ◽  
In Vivo Studies ◽  
Active Components ◽  
Theranostic Agent ◽  
Supramolecular Coordination ◽  
Targeting Ability

A theranostic agent combines diagnostic reporter with therapeutic activity in a single entity, an approach that seeks to increase the efficacy of cancer treatment. Herein, we describe the synthesis of a highly emissive tetraphenylethene-based metallacage using multicomponent coordination-driven self-assembly that exhibits a coordination-triggered aggregation-induced emission (AIE) enhancement. The formation of metallacage-loaded nanoparticles (MNPs) occurs when the assembly is treated with two variants of a 1,2-distearoyl-phosphatidylethanolamine (DSPE)/polyethylene glycol (PEG) conjugate, mPEG-DSPE, and biotin-PEG-DSPE. This combination endows the resultant MNPs with excellent stability and targeting ability, specifically enabling selective delivery of the metallacages to cancer cells that overexpress biotin receptors via receptor-mediated endocytosis. Although the mechanism of activity is based on existing Pt(II) anticancer drugs such as oxaliplatin, carboplatin, and cisplatin, in vitro and in vivo studies indicate that the MNPs are more active and show low systemic activity while also possessing emissive properties that allow for fluorescence-based imaging. This pioneering example of a metallacage that combines biologically active components with AIE imaging establishes supramolecular coordination complexes imbedded within nanoparticles as a promising potential theranostic platform for cancer treatment.

Metabolomics of Healthy Berry Fruits

2019 ◽  
Vol 25 (37) ◽  
pp. 4888-4902 ◽  
Author(s):  
Gilda D'Urso ◽  
Sonia Piacente ◽  
Cosimo Pizza ◽  
Paola Montoro
Keyword(s):  
Biological Activities ◽  
Biologically Active ◽  
In Vivo Studies ◽  
Bioactive Metabolites ◽  
Active Metabolites ◽  
Positive Effects ◽  
Cell Functions ◽  
Berry Fruits

The consumption of berry-type fruits has become very popular in recent years because of their positive effects on human health. Berries are in fact widely known for their health-promoting benefits, including prevention of chronic disease, cardiovascular disease and cancer. Berries are a rich source of bioactive metabolites, such as vitamins, minerals, and phenolic compounds, mainly anthocyanins. Numerous in vitro and in vivo studies recognized the health effects of berries and their function as bioactive modulators of various cell functions associated with oxidative stress. Plants have one of the largest metabolome databases, with over 1200 papers on plant metabolomics published only in the last decade. Mass spectrometry (MS) and NMR (Nuclear Magnetic Resonance) are the most important analytical technologies on which the emerging ''omics'' approaches are based. They may provide detection and quantization of thousands of biologically active metabolites from a tissue, working in a ''global'' or ''targeted'' manner, down to ultra-trace levels. In the present review, we highlighted the use of MS and NMR-based strategies and Multivariate Data Analysis for the valorization of berries known for their biological activities, important as food and often used in the preparation of nutraceutical formulations.

An effective and safe treatment strategy for rheumatoid arthritis based on human serum albumin and Kolliphor® HS 15

Nanomedicine ◽  
2019 ◽  
Vol 14 (16) ◽  
pp. 2169-2187 ◽  
Author(s):  
Ting Gong ◽  
Pei Zhang ◽  
Caifeng Deng ◽  
Yu Xiao ◽  
Tao Gong ◽  
...  
Keyword(s):  
Rheumatoid Arthritis ◽  
Human Serum Albumin ◽  
Serum Albumin ◽  
Human Serum ◽  
Therapeutic Strategy ◽  
Inflammatory Cell ◽  
In Vivo Studies ◽  
Targeting Ability

Aim: We aimed to construct human serum albumin-Kolliphor® HS 15 nanoparticles (HSA-HS15 NPs) to overcome the limitations in targeted therapy for rheumatoid arthritis (RA) and enhance the safety of drug-loaded HSA NPs. Methodology: Celastrol (CLT)-loaded HSA-HS15 NPs were prepared and the properties were adequately investigated; the treatment effect were evaluated in RA rats; in vitro and in vivo studies were performed to explain the mechanism. Results: CLT-HSA-HS15 NPs had remarkable treatment ability and enhanced safety in the treatment of RA compared with free CLT and CLT-HSA NPs. Conclusion: HSA-HS15 NPs could be a safe and efficient therapeutic strategy for the treatment of RA, because of the inflammatory targeting ability of albumin, the added HS15 and ELVIS effect (extravasation through leaky vasculature followed by inflammatory cell-mediated sequestration) of nanoparticles.

scholarly journals The West African Sorghum Bicolor Leaf Sheath Extract Jobelyn® and Its Diverse Therapeutic Potentials

2017 ◽  
Author(s):  
Samira Makanjuola ◽  
Olajuwon Okubena ◽  
Louis Ajonuma ◽  
Adedoyin Dosunmu ◽  
Solomon Umukoro ◽  
...  
Keyword(s):  
Sorghum Bicolor ◽  
Leaf Sheath ◽  
West African ◽  
Biologically Active ◽  
In Vivo Studies ◽  
The West ◽  
Total Extract ◽  
Active Compounds

The West-African variety of Sorghum bicolor leaf sheath (SBLS) Jobelyn® is a natural remedy, which has gained international recognition for its anti-anemic effect and energy boosting qualities in debilitating diseases. The widespread use of traditional medicine in the region usually confirms its safety, but not its efficacy or deep assessment of their pharmacological properties. The other major issue for herbal-based treatments is the lack of definite and complete information about the composition of the extracts.  Despite limitations, efforts have been made in isolation and characterisation of active compounds in this specie of sorghum showing various subclasses of flavonoids including apigeninidin, a stable 3-deoxyanthocyanidin and potential fungal growth inhibitor, which accounts for 84% of the total extract. Non-clinical in vitro and in vivo studies support previous indications that this variety of Sorghum bicolor possesses several biologically active compounds with potent antioxidant, anti-inflammatory, anti-aging and neuro-protective properties.  Clinical studies show that SBLS has the ability to boost hemoglobin concentrations in anemic conditions and most remarkably to increase CD4 count in HIV-positive patients. The multiple effects and high safety profiles of this extract may encourage its development as a therapeutic agent for the treatment of anemia, chronic inflammatory conditions or in the symptomatic management of HIV infections. This review describes the potential therapeutic aspects of SBLS extract and its potential benefits.

scholarly journals The anti-malignant activity of Macrotyloma uniflorum mediated green synthesized Cu and Zn metal-ligand nano complexes

2020 ◽  
Vol 11 (SPL4) ◽  
pp. 1573-1580
Author(s):  
Savita Belwal ◽  
Sujana Kariveda ◽  
Saritha Ramagiri ◽  
Swathi A ◽  
Shubham Kute ◽  
...  
Keyword(s):  
Metal Complexes ◽  
Biologically Active ◽  
In Vivo Studies ◽  
Chemistry Laboratory ◽  
Condensation Process ◽  
Spectroscopic Techniques ◽  
Macrotyloma Uniflorum ◽  
Cu And Zn

The green biological route has been employed to convert macro-sized zinc and copper metal complexes into nano-sized metal complexes. These bioactive metal complexes were synthesized by template condensation process in the chemistry laboratory. The newly synthesized biologically active complexes were converted into nano range from phytochemical aqueous extract of Macrotyloma uniflorum (horse gram). Biologically converted nano complexes have been characterized by physicochemical as well as spectroscopic techniques such as UV-visible spectrophotometer and FTIR. The reduced Cu and Zn metal nanoparticles were analyzed with SEM for shape and size, which showed most of the nanoparticles, were nearly spherical with nano range size. To estimate the potentiality of newly manufactured copper and zinc nanoparticles in vitro  and in in vivo  studies, i.e. antifungal and antibacterial and anti-cancer activities were performed. The biogenic nanoparticles of Cu and Zn were evaluated for their activity on cancer A-549 cell lines by standard MTT assay for metabolically active mitochondria and cell viability. Further flow cytometric studies showed Cu, and Zn nano complexes had inhibition efficacy of cancer cells compared to normal cells. This study elevates that biosynthesized Cu & Zn nano complexes can be an alternative for the treatment of cancer.

scholarly journals Identification on the potential mechanism of Radix pueraria on colon cancer based on network pharmacology

2021 ◽  
Author(s):  
Yi Li ◽  
Chunli Zhang ◽  
Xiaohan Ma ◽  
Liuqing Yang ◽  
Huijun Ren
Keyword(s):  
Colon Cancer ◽  
Chinese Medicine ◽  
Target Genes ◽  
Enrichment Analysis ◽  
In Vivo Studies ◽  
Network Pharmacology ◽  
Biological Mechanism ◽  
Active Components

Abstract Radix Puerariae (RP), a dry root of the Pueraria lobata (Willd.) Ohwi, is used to treat a variety of diseases, including cancer. Several in vitro and in vivo studies have demonstrated the efficacy of RP in the treatment of colon cancer (CC). However, the biological mechanism of RP in the treatment of colon cancer remains unclear. In this study, the active component of RP and its potential molecular mechanism against CC were studied by network pharmacology and enrichment analysis. The methods adopted included screening of active ingredients of Chinese medicine, prediction of target genes of Chinese medicine and disease, construction of protein interaction network, and GO and KEGG Enrichment Analysis. Finally, the results of network pharmacology were further validated by molecular docking experiments and cell experiments. 8 active constituents and 14 potential protein targets were screened from RP, including EGFR, JAK2 and SRC. The biological mechanism of RP against CC was analyzed by studying the relationship between active components, targets, and enrichment pathway. This provides a basis for understanding the clinical application of RP in CC.

scholarly journals Evaluation of Radioiodinated Fluoronicotinamide/Fluoropicolinamide-Benzamide Derivatives as Theranostic Agents for Melanoma

2020 ◽  
Vol 21 (18) ◽  
pp. 6597
Author(s):  
Chao-Cheng Chen ◽  
Yang-Yi Chen ◽  
Yi-Hsuan Lo ◽  
Ming-Hsien Lin ◽  
Chih-Hsien Chang ◽  
...  
Keyword(s):  
Absorbed Dose ◽  
Radiochemical Yield ◽  
Amelanotic Melanoma ◽  
In Vivo Studies ◽  
Log P ◽  
Theranostic Agent ◽  
Biodistribution Studies ◽  
Theranostic Agents

Malignant melanoma is the most harmful type of skin cancer and its incidence has increased in this past decade. Early diagnosis and treatment are urgently desired. In this study, we conjugated picolinamide/nicotinamide with the pharmacophore of 131I-MIP-1145 to develop 131I-iodofluoropicolinamide benzamide (131I-IFPABZA) and 131I-iodofluoronicotiamide benzamide (131I-IFNABZA) with acceptable radiochemical yield (40 ± 5%) and high radiochemical purity (>98%). We also presented their biological characteristics in melanoma-bearing mouse models. 131I-IFPABZA (Log P = 2.01) was more lipophilic than 131I-IFNABZA (Log P = 1.49). B16F10-bearing mice injected with 131I-IFNABZA exhibited higher tumor-to-muscle ratio (T/M) than those administered with 131I-IFPABZA in planar γ-imaging and biodistribution studies. However, the imaging of 131I-IFNABZA- and 131I-IFPABZA-injected mice only showed marginal tumor uptake in A375 amelanotic melanoma-bearing mice throughout the experiment period, indicating the high binding affinity of these two radiotracers to melanin. Comparing the radiation-absorbed dose of 131I-IFNABZA with the melanin-targeted agents reported in the literature, 131I-IFNABZA exerts lower doses to normal tissues on the basis of similar tumor dose. Based on the in vitro and in vivo studies, we clearly demonstrated the potential of using 131I-IFNABZA as a theranostic agent against melanoma.

Response of preimplantation rat blastocysts in vitro to extracellular uterine luminal components, serum and hormones

1977 ◽  
Vol 25 (1) ◽  
pp. 265-277
Author(s):  
M.A. Surani
Keyword(s):  
Calf Serum ◽  
Giant Cells ◽  
Biologically Active ◽  
Foetal Calf Serum ◽  
Active Components ◽  
Rat Serum ◽  
Pregnant Females ◽  
Trophoblast Giant Cells

The influence of extracellular environmental factors on preimplantation rat blastocysts was tested by determining the number of embryos which escaped from their zonae pellucidae, followed by attachment and outgrowth of trophoblast giant cells, after 72 h in culture Uterine luminal ocmponents from individual females, or hormones, were included in Dulbecco's medium which contained 4 mg/ml bovine serum albumin. In about 20% of cases, uterine fluids were embryotonic. However, uterine fluids from day-5 pregnant females, the day of implantation in the rat, were more potent in these tests than uterine fluids obtained from ovariectomized females treated with progesterone alone. The potency of a mixture of the 2 fluids was also high. Uterine fluids obtained at 14 h after an injection of oestradiol and progesterone to the ovariectomized females, were also effective in these tests. Rat serum and foetal calf serum were effective too, but steroids or insulin alone in the medium had no detectable influence on embryos. Serum or uterine luminal proteins appear to be essential for maintaining the viability of the blastocysts and for inducing the responses observed here. In the uterine fluids, some proteins released into the lumen after treatment of females with oestradiol and progesterone appear to be the biologically active components. Differences in the responses of blastocysts in vitro are compared with those in vivo.

New gold-198 nanoparticle synthesis to be used in cancer treatment

2021 ◽  
Vol 9 (1A) ◽  
Author(s):  
Carla Daruich de Souza ◽  
Carla Daruich de Souza ◽  
Carlos Alberto Zeituni ◽  
Wilmmer Alexander Arcos Rosero ◽  
Beatriz Ribeiro Nogueira ◽  
...  
Keyword(s):  
Gold Nanoparticles ◽  
Cancer Treatment ◽  
Nuclear Reactor ◽  
Nanoparticle Synthesis ◽  
Average Energy ◽  
In Vivo Studies ◽  
Chloroauric Acid ◽  
Repeated Heating

Gold nanoparticles (NPs) have been intriguing scientists for over 100 years. Recently, they have been studied for new applications such as cancer treatment. Although the synthesis of gold nanoparticles is extensively reported, in the majority of cases the methodology is confused and/or not clear. We describe a new synthesis methodology for radioactive gold‐198 NPs. Gold-198 was activated in IPEN IEA-01 nuclear reactor. After that, chloroauric acid (HAuCl4) was formed by dissolving the radioactive gold with aqua regia and performing repeated heating cycles. 0.1 mM HAuCl4 containing 100 μL of 1 M NaOH was prepared in a flask equipped with a reflux condenser. The solution was brought to boil and stirred with a PTFE‐coated magnetic stir‐bar. Then 5 mL of sodium citrate was rapidly added. The reaction turns from light yellow to clear, black, dark purple until the solution attained a wine‐red color (2–3 min). Dynamic light scattering (DLS) confirmed 8 nm particles. The presence of gold‐198 (197.968 g/mol; half‐life: 2.69517; decay mode: β‐; average energy: 1.3723 MeV) was confirmed by an ORTEC HPGe detector. DLS was performed after complete decay confirming the 8 nm diameter maintenance. We were able to achieve radioactive gold‐198 NPs and are performing further studies such as: coating reactions, in‐vitro and in‐vivo studies.

scholarly journals Magnetic Hyperthermia for Cancer Treatment: Main Parameters Affecting the Outcome of In Vitro and In Vivo Studies

Molecules ◽  
2020 ◽  
Vol 25 (12) ◽  
pp. 2874
Author(s):  
Vânia Vilas-Boas ◽  
Félix Carvalho ◽  
Begoña Espiña
Keyword(s):  
Adjuvant Therapy ◽  
Cancer Treatment ◽  
Magnetic Hyperthermia ◽  
In Vivo Studies ◽  
Clinical Context ◽  
Notable Increase ◽  
The 1950S

Magnetic hyperthermia (MHT) is being investigated as a cancer treatment since the 1950s. Recent advancements in the field of nanotechnology have resulted in a notable increase in the number of MHT studies. Most of these studies explore MHT as a stand-alone treatment or as an adjuvant therapy in a preclinical context. However, despite all the scientific effort, only a minority of the MHT-devoted nanomaterials and approaches made it to clinical context. The outcome of an MHT experiment is largely influenced by a number of variables that should be considered when setting up new MHT studies. This review highlights and discusses the main parameters affecting the outcome of preclinical MHT, aiming to provide adequate assistance in the design of new, more efficient MHT studies.

scholarly journals Bacteriophage T4 Self-Assembly: In Vitro Reconstitution of Recombinant gp2 into Infectious Phage

2000 ◽  
Vol 182 (3) ◽  
pp. 672-679 ◽  
Author(s):  
G. R. Wang ◽  
A. Vianelli ◽  
E. B. Goldberg
Keyword(s):  
Self Assembly ◽  
Burst Size ◽  
Bacteriophage T4 ◽  
Biologically Active ◽  
Phage Infection ◽  
Direct Role ◽  
In Vitro Reconstitution ◽  
Phage Dna

ABSTRACT T4 gene 2 mutants have a pleiotropic phenotype: degradation of injected phage DNA by exonuclease V (ExoV) in therecBCD + host cell cytoplasm and a low burst size due, at least in part, to a decreased ability for head-to-tail (H-T) joining. The more N terminal the mutation, the more pronounced is the H-T joining defect. We have overexpressed and purified the recombinant gene 2 product (rgp2) to homogeneity in order to test its role in H-T joining, during in vitro reconstitution. When we mix extracts of heads from a gp2+ phage infection (H+) with tails from a gp2+ or gp2− phage infection (T+ or T−), the H-T joining is fast and all of the reconstituted phage grow equally well on cells with or without ExoV activity. When heads from gene 2 amber mutants (H−) are used, addition of rgp2 is required for H-T joining. In this case, H-T joining is slow and only about 10% of the reconstituted phage can form plaques on ExoV+ cells. When extracts of heads with different gene 2 amber mutations are mixed with extracts of tails (with a gene 2 amber mutation) in the presence of rgp2, we find that the size of the gp2 amber peptide of the head extract is inversely related to the fraction of reconstituted phage with a 2+ phenotype. We conclude that free rgp2 is biologically active and has a direct role in H-T joining but that the process is different from H-T joining promoted by natural gp2 that is incorporated into the head in vivo. Furthermore, it seems that gp2 has a domain which binds it to the head. Thus, the presence of the longer gp2am mutants (with this domain) inhibits their replacement by full-length rgp2.

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