Preparation and evaluation of peptide-dendrimer-paclitaxel conjugates for treatment of heterogeneous stage 1 nonsmall cell lung cancer in 293T and L132 cell lines

Purpose: To develop peptide-dendrimer-paclitaxel conjugates for the treatment of heterogeneous stage 1 non small cell lung cancer (NSCLC) in 293T and L132cell line.Method: Dendrimer-paclitaxel conjugates (PAMAM-PTX) were prepared by NHS method and the conjugates were used for the synthesis of peptide-dendrimer-paclitaxel conjugates (GE-PAMAM-PTX). The particle sizes of PAMAM-PTX and GE-PAMAM-PTX were measured. Entrapment efficiency of PTX in PAMAM-PTX was measured while GE-PAMAM-PTX. PTX release from PAMAM-PTX and GEPAMAM- PTX was determined using a dialysis bag in pH 7.4 phosphate buffer. The cytotoxicity of PAMAM-PTX, GE-PAMAM-PTX, PAMAM and PTX was evaluated by 3-(4,5-dimethylthiazol-2-Yl)-2,5- diphenyltetrazolium bromide (MTT) assay using 293T cell lines. In vitro cellular uptake assay of PAMAM-PTX and GE-PAMAM-PTX and PTX at concentrations ranging from 0.01 to 0.5μM for 8 h was carried out in NSCLC cell lines 293T and L132.Results: More than 95 % entrapment efficiency of GE-PAMAM-PTX was observed with loading efficiency of 25 %. GE-PAMAM-PTX conjugates showed sustained release of PTX (~85 %) towards the end of 50 h. GE-PAMAM-PTX conjugates were more cytotoxic than pure PTX and PAMAM-PTX conjugates. The remarkable uptake of GE-PAMAM-PTX appear to be due to receptor-mediated endocytosis in the cell lines. The presence of ligand (GE) on PAMAM-PTX surface enabled the complex to bind to the over-expressed receptors on the cell lines.Conclusion: GE-PAMAM-PTX can facilitate targeting of paclitaxel to lung cancer cell lines and tumors and facilitate release of the drugs in a sustained manner to improve the therapeutic efficacy of PTX.Keywords: Paclitaxel, Lung cancer, Non-small cell lung cancer, Dendrimer, Peptide, PAMA

3-(7-Meth­oxy-β-carbolin-1-yl)propionic acid monohydrate

In the title compound, C15H14N2O3·H2O [systematic name: 3-(7-meth­oxy-9H-pyrido[3,4-b]indol-1-yl)propanoic acid monohydrate], the fused rings make dhedral angles of 0.4 (1), 1.1 (2) and 1.4 (2)°. In the crystal, the water mol­ecule is involved in the formation of three independent hydrogen-bonded chains via O—H⋯O and N—H⋯O hydrogen bonds, while the carb­oxy group forms an inter­molecular O—H⋯N hydrogen bond

SRIBO: An Efficient and Resilient Single-Range and Inertia Based Odometry for Flying Robots

Positioning with one inertial measurement unit and one ranging sensor is commonly thought to be feasible only when trajectories are in certain patterns ensuring observability. For this reason, to pursue observable patterns, it is required either exciting the trajectory or searching key nodes in a long interval, which is commonly highly nonlinear and may also lack resilience. Therefore, such a positioning approach is still not widely accepted in real-world applications. To address this issue, this work first investigates the dissipative nature of flying robots considering aerial drag effects and re-formulates the corresponding positioning problem, which guarantees observability almost surely. On this basis, a dimension-reduced wriggling estimator is proposed accordingly. This estimator slides the estimation horizon in a stepping manner, and output matrices can be approximately evaluated based on the historical estimation sequence. The computational complexity is then further reduced via a dimension-reduction approach using polynomial fittings. In this way, the states of robots can be estimated via linear programming in a sufficiently long interval, and the degree of observability is thereby further enhanced because an adequate redundancy of measurements is available for each estimation. Subsequently, the estimator's convergence and numerical stability are proven theoretically. Finally, both indoor and outdoor experiments verify that the proposed estimator can achieve decimeter-level precision at hundreds of hertz per second, and it is resilient to sensors' failures. Hopefully, this study can provide a new practical approach for self-localization as well as relative positioning of cooperative agents with low-cost and lightweight sensors

Euphorbia factor L8: a diterpenoid from the seeds of Euphorbia lathyris

The title compound [systematic name: (2S*,3S*,4R*,5R*,9S*,11S*,15R*)-5,15-diacet­oxy-3-nicotino­yloxy-14-oxolathyra-6(17),12(E)-diene], C30H37NO7, was isolated from the seeds of Euphorbia lathyris. The tricyclic diterpenoid molecule contains an 11-membered ring, a five-membered ring exhibiting an envelope conformation and a three-membered ring. The 11-membered ring is cis-fused with the three-membered ring and trans-fused with the five-membered ring