Self-assembling a natural small molecular inhibitor that shows aggregation-induced emission and potentiates antitumor efficacy

2021 ◽  
Vol 6 (1) ◽  
pp. 33-42
Author(s):  
Xiaona Chen ◽  
Zhen Hu ◽  
Liqian Zhou ◽  
Fu Zhang ◽  
Jianqin Wan ◽  
...  
Keyword(s):  
Antitumor Activity ◽  
Antitumor Efficacy ◽  
Aggregation Induced Emission ◽  
Self Assembling ◽  
Self Assembled ◽  
High Antitumor Activity

Self-assembled dasatinib nanoparticles exhibited aggregation-induced emission with high antitumor activity.

A New Synthetic Spiroketal: Studies on Antitumor Activity on Murine Melanoma Model In Vivo and Mechanism of Action In Vitro

2019 ◽  
Vol 19 (4) ◽  
pp. 567-578
Author(s):  
Maria P. Fuggetta ◽  
Pietro Spanu ◽  
Fausta Ulgheri ◽  
Francesco Deligia ◽  
Paola Carta ◽  
...  
Keyword(s):  
Antitumor Activity ◽  
Tumor Growth ◽  
Antitumor Effect ◽  
Antitumor Efficacy ◽  
Murine Melanoma ◽  
Melanoma Model ◽  
High Antitumor Activity ◽  
Dose Dependent

Background:In a previous study, we synthesised a new spiroketal derivative, inspired to natural products, that has shown high antiproliferative activity, potent telomerase inhibition and proapoptotic activity on several human cell lines.Objective:This work focused on the study of in vivo antitumor effect of this synthetic spiroketal on a murine melanoma model. In order to shed additional light on the origin of the antitumor effect, in vitro studies were performed.Methods:Spiroketal was administered to B16F10 melanoma mice at a dose of 5 mg/Kg body weight via intraperitoneum at alternate days for 15 days. Tumor volume measures were made every 2 days starting after 12 days from cells injection. The effects of the spiroketal on tumor growth inhibition, apoptosis induction, and cell cycle modification were investigated in vitro on B16 cells. HIF1α gene expression, the inhibition of cells migration and the changes induced in cytoskeleton conformation were evaluated.Results:Spiroketal displayed proapoptotic activity and high antitumor activity in B16 cells with nanomolar IC50. Moreover it has shown to inhibit cell migration, to strongly reduce the HIF1α expression and to induce strongly deterioration of cytoskeleton structure. A potent dose-dependent antitumor efficacy in syngenic B16/C57BL/6J murine model of melanoma was observed with the suppression of tumor growth by an average of 90% at a dose of 5 mg/kg.Conclusion:The synthesized spiroketal shows high antitumor activity in the B16 cells in vitro at nM concentration and a dose-dependent antitumor efficacy in syngenic B16/C57BL/6J mice. The results suggest that this natural product inspired spiroketal may have a potential application in melanoma therapy.

Hierarchical nanostructures self-assembled from δ-MnO2 ultrathin nanosheets and Mn3O4 octahedrons for efficient room-temperature HCHO oxidation

2021 ◽  
Author(s):  
Lifang Qi ◽  
Yao Le ◽  
Chao Wang ◽  
Rui Lei ◽  
Tian Wu
Keyword(s):  
Room Temperature ◽  
Hierarchical Nanostructures ◽  
Low Level ◽  
Ultrathin Nanosheets ◽  
Self Assembling ◽  
Formaldehyde Oxidation ◽  
Self Assembled

Self-assembling ultrathin active δ-MnO2 nanosheets and Mn3O4 octahedrons into hierarchical texture enhances room-temperature formaldehyde oxidation at a low-level of Pt.

Self-Assembled Photonic Microsensors with Strong Aggregation-Induced Emission for Ultra-Trace Quantitative Detection

ACS Nano ◽  
2021 ◽  
Vol 15 (3) ◽  
pp. 5534-5544
Author(s):  
Qiu-Jun Liu ◽  
Yulian Li ◽  
Jing-Cheng Xu ◽  
Hai-Feng Lu ◽  
Yuesheng Li ◽  
...  
Keyword(s):  
Quantitative Detection ◽  
Aggregation Induced Emission ◽  
Self Assembled ◽  
Ultra Trace

scholarly journals Superhydrophilic Coating of Pine Wood by Plasma Functionalization of Self-Assembled Polystyrene Spheres

Coatings ◽  
2021 ◽  
Vol 11 (2) ◽  
pp. 114
Author(s):  
Sebastian Dahle ◽  
John Meuthen ◽  
René Gustus ◽  
Alexandra Prowald ◽  
Wolfgang Viöl ◽  
...  
Keyword(s):  
Dip Coating ◽  
Face Centered Cubic ◽  
Wood Substrate ◽  
Polystyrene Spheres ◽  
Pine Wood ◽  
Self Assembling ◽  
Monodisperse Polystyrene ◽  
Self Assembled ◽  
Face Centered ◽  
Plasma Functionalization

Self-assembling films typically used for colloidal lithography have been applied to pine wood substrates to change the surface wettability. Therefore, monodisperse polystyrene (PS) spheres have been deposited onto a rough pine wood substrate via dip coating. The resulting PS sphere film resembled a polycrystalline face centered cubic (FCC)-like structure with typical domain sizes of 5–15 single spheres. This self-assembled coating was further functionalized via an O2 plasma. This plasma treatment strongly influenced the particle sizes in the outermost layer, and hydroxyl as well as carbonyl groups were introduced to the PS spheres’ surfaces, thus generating a superhydrophilic behavior.

scholarly journals A Novel Paclitaxel Microemulsion Containing a Reduced Amount of Cremophor EL: Pharmacokinetics, Biodistribution, andIn VivoAntitumor Efficacy and Safety

2011 ◽  
Vol 2011 ◽  
pp. 1-10 ◽  
Author(s):  
Ying Wang ◽  
Ke-Chun Wu ◽  
Bing-Xiang Zhao ◽  
Xin Zhao ◽  
Xin Wang ◽  
...  
Keyword(s):  
Antitumor Activity ◽  
Therapeutic Efficacy ◽  
Antitumor Efficacy ◽  
Allergic Reactions ◽  
Cremophor El ◽  
Efficacy And Safety ◽  
Tumor Bearing ◽  
Allergic Effect ◽  
Injection Product

The purpose of this study was to prepare a novel paclitaxel (PTX) microemulsion containing a reduced amount of Cremophor EL (CrEL) which had similar pharmacokinetics and antitumor efficacy as the commercially available PTX injection, but a significantly reduced allergic effect due to the CrEL. The pharmacokinetics, biodistribution,in vivoantitumor activity and safety of PTX microemulsion was evaluated. The results of pharmacokinetic and distribution properties of PTX in the microemulsion were similar to those of the PTX injection. The antitumor efficacy of the PTX microemulsion in OVCRA-3 and A 549 tumor-bearing animals was similar to that of PTX injection. The PTX microemulsion did not cause haemolysis, erythrocyte agglutination or simulative reaction. The incidence and degree of allergic reactions exhibited by the PTX microemulsion group, with or without premedication, were significantly lower than those in the PTX injection group (P<.01). In conclusion, the PTX microemulsion had similar pharmacokinetics and anti-tumor efficacy to the PTX injection, but a significantly reduced allergic effect due to CrEL, indicating that the PTX microemulsion overcomes the disadvantages of the conventional PTX injection and is one way of avoiding the limitations of current injection product while providing suitable therapeutic efficacy.

Cemiplimab in a very frail population of patients with advanced or metastatic cutaneous squamous cell carcinoma: A monocenter real-life experience from Italy.

2021 ◽  
Vol 39 (15_suppl) ◽  
pp. e21524-e21524
Author(s):  
Michele Guida ◽  
Annarita Fanizzi ◽  
Davide Quaresmini ◽  
Annalisa Nardone ◽  
Andrea Armenio ◽  
...  
Keyword(s):  
Squamous Cell Carcinoma ◽  
Antitumor Activity ◽  
Cell Carcinoma ◽  
Clinical Outcomes ◽  
Squamous Cell ◽  
Life Experience ◽  
Locally Advanced ◽  
Real Life ◽  
Cutaneous Squamous Cell Carcinoma ◽  
High Antitumor Activity

e21524 Background: Cutaneous squamous cell carcinoma (CSCC) is the second most common skin cancer. Although representing less than 5% of all CSCCs, advanced stages are difficult to treat. Cemiplimab, an antiPD-1 monoclonal antibody, is the first approved immunotherapy in the US and EU for patients with locally advanced (laCSCC) or metastatic (mCSCC) CSCC. Phase I-II studies showed high antitumor activity and good tolerability, but few data are still available regarding cemiplimab in real life experience in non-selected patients. Methods: We recruited 30 consecutive patients with laCSCC (25 pts) and mCSCC (5 pts) treated with cemiplimab from August 2019 to November 2020 at our Institution. Median age was 81 years (range 36-95); 24 males; median ECOG PS 1 (range 0-2). Five patients had an immunosuppressive condition including 3 patients with stable hematologic malignancies and two patients on immunosuppressive therapy for kidney transplantation and Crohn’s disease, respectively. The majority of patients had comorbidities (median 3). Cemiplimab was administered at the flat dose of 350 mg i.v. every 21 days until disease progression or unacceptable toxicity. In all patients we evaluated clinical outcomes, toxicity, and associations between clinical outcomes and peripheral blood parameters. Results: We reported 23 responses (ORR 76.7%) with CR in 5 patients (16.7%). One patient had SD for 5 months. The global DCR was 80%. The median duration of response and PFS was not reached at a median follow-up of 6 months. We observed a higher ORR in head and neck primary tumours (87% vs. 42.9% of others, p = 0.016) and in patients with haemoglobin level > 12 g/dL (87.5% vs. 64.3%). No significative difference in ORR was observed with respect to the median age (81.3% in >81 years vs. 71.4% in < 81 years). Among the 5 patients with immunosuppressive status, a response was obtained in 4 patients (80%), including 1 CR. Nine patients died, 7 for PD and 2 for causes unrelated to the disease. Twenty patients (67.7%) still have an ongoing response. The treatment was well tolerated by the majority of patients. The most common adverse events were fatigue in 7 patients (23.3%) and skin toxicity in 10 patients (33.3%) including pruritus in 6 patients, rash in 3 patients, bullous erythema in 1 patient. Only 3 (10%) patients experienced severe (grade 3/4) toxicity. Three responder patients interrupted treatment (2 for toxicity after 7 and 9 cycles, and one for pre-existing dementia) but maintaining their response. Conclusions: In our real-life experience cemiplimab showed high antitumor activity with acceptable safety profile similar to those in selected patients of trials. Moreover, its antitumor activity resulted not impaired in very elderly patients or in those with immunocompromized status.

PRIMA-1Met/APR-246 Displays High Antitumor Activity in Multiple Myeloma By Induction of p73 and Noxa

2013 ◽  
Vol 12 (11) ◽  
pp. 2331-2341 ◽  
Author(s):  
Manujendra N. Saha ◽  
Hua Jiang ◽  
Yijun Yang ◽  
Donna Reece ◽  
Hong Chang
Keyword(s):  
Multiple Myeloma ◽  
Antitumor Activity ◽  
High Antitumor Activity

Self-assembled nano-aggregates of fluorinases demonstrate enhanced enzymatic activity, thermostability and reusability

2020 ◽  
Vol 8 (2) ◽  
pp. 648-656
Author(s):  
Chunhao Tu ◽  
Jin Zhou ◽  
Lei Peng ◽  
Shuli Man ◽  
Long Ma
Keyword(s):  
Aqueous Solution ◽  
Enzyme Activity ◽  
Enzymatic Activity ◽  
Self Assembling ◽  
Self Assembled

Three SAP (self-assembling peptide)-tagged fluorinases (FLAs) are successfully prepared. All three SAP-tagged FLAs bear enzymatic activity and they form nano-sized particles in aqueous solution. One of them displays improved enzyme activity, thermostability and reusability.

A highly sensitive humidity sensor based on an aggregation-induced emission luminogen-appended hygroscopic polymer microresonator

2021 ◽  
Author(s):  
Airong Qiagedeer ◽  
Hiroshi Yamagishi ◽  
Minami Sakamoto ◽  
Hanako Hasebe ◽  
Fumitaka Ishiwari ◽  
...  
Keyword(s):  
Humidity Sensor ◽  
High Sensitivity ◽  
Aggregation Induced Emission ◽  
Highly Sensitive ◽  
Self Assembled

A self-assembled microsphere resonator, comprising a hygroscopic polymer with aggregation-induced emission luminogen pendants, can sense humidity with high sensitivity and repeatability.

scholarly journals Self-assembled nanostructured photosensitizer with aggregation-induced emission for enhanced photodynamic anticancer therapy

2019 ◽  
Vol 63 (1) ◽  
pp. 136-146 ◽  
Author(s):  
Wenkun Han ◽  
Song Zhang ◽  
Rong Deng ◽  
Yangyang Du ◽  
Jingyu Qian ◽  
...  
Keyword(s):  
Anticancer Therapy ◽  
Aggregation Induced Emission ◽  
Self Assembled
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