Novel Semisynthetic Derivative of Dehydrozingerone (DHZ-15) Modulates Lipopolysaccharide-Stimulated Macrophages by Targeting the NF-κB/p65 Pathway and In Vivo Evaluation in a Sepsis BALB/c Model.

Natural products and their semisynthetic derivatives possess tremendous medicinal properties and have the potential to modulate the immune system, providing new therapeutic options for drug development. In this study, we evaluated Dehydrozingerone-15, a novel dehydrozingerone derivative, for its anti-inflammatory and antioxidant properties through standardised in vitro and in vivo approaches. Dehydrozingerone-15 suppressed the stimulatory effect of LPS in RAW 264.

5-(3, 4-methylenedioxyphenyl)-4-ethyl-2E, 4E-pentadienoic acid piperidide as MdeA efflux pump inhibitor of Staphylococcus aureus.

The analogue of piperine 5-(3,4-methylenedioxyphenyl)-4-ethyl-2E,4E-pentadienoic acid piperidide (IIIM-1133), was evaluated in this in combination with pseudomonic acid A, commonly known as mupirocin against of S. aureus including Methicillin Resistant S. aureus (MRSA).

Evaluation of Anti-Inflammatory and Immunosuppressant Potential of Isotelekin in Lipopolysaccharide (LPS) Stimulated Macrophage (RAW 264.7) and Sheep Red Blood Cells (SRBC) Sensitized Murine Models.

The present study explored the natural compound Isotelekin isolated from Inula racemose against anti-inflammatory and immunomodulatory potential in LPS-induced RAW264.7 cell lines and immune-elevated SRBC-sensitized animal models. Isotelekin in in vitro studies, inhibited the production of Th-1 cytokines Interleukin-6 (IL-6), Tumour necrosis factor (TNF-α), and Interferon-gamma (INF-γ), and increased Th-2 cytokines Interleukin-10 (IL-10).

C-30 analogues of betulinic acid as potent cytotoxic agents: design, synthesis, biological evaluation and studies.

In an endeavour to improve the anti-cancer activity of betulinic acid (BA), a series of C-30 derivatives were envisaged and synthesized with a novel synthetic approach. All the derivatives were evaluated for cytotoxic activity by MTT assay against six different human cancer cell lines: prostate (PC3), lung (A549), human hepatocellular carcinoma (HepG2), human leukemia (Molt-4), pancreatic (Panc-1) and breast (MCF-7). The data revealed that compound was observed most promising cytotoxic agent with IC values of μM, μM, and μM against A549, MCF-7, and PC3 cancer cell lines respectively.

Discovery of Anti-NRLP3 Inflammasome, Immunomodulatory Phytochemicals from the Extract of : An Unexplored Plant Species.

The present study describes the isolation, identification, and quantification of biomarker compounds in plant extracts of D. Don (Orchidaceae). The isolation of the compounds was carried out from D.

Repositioning the existing drugs for neuroinflammation: a fusion of computational approach and biological validation to counter the Parkinson's disease progression.

Parkinson's disease is caused by the deficiency of striatal dopamine and the accumulation of aggregated α-synuclein in the substantia nigra pars compacta (SNpc). Neuroinflammation associated with oxidative stress is a key factor contributing to the death of dopaminergic neurons in SNpc and advancement of Parkinson's disease. Two molecular targets, i.

Synthesis, characterization, and wound healing properties of α/γ hybrid peptides.

The present work describes the synthesis, characterization, and wound healing properties of α/γ hybrid peptides: Boc-Phe-γ -Phe-Val-OMe (S1), Boc- Phe-γ -Phe-Val-OMe (S2), Boc-Ala-γ -Phe-Val-OMe (S3), Boc- Ala-γ -Phe-Val-OMe (S4), Boc-Leu-γ -Phe-Val-OMe (S5), and Boc- Leu-γ -Phe-Val-OMe (S6). Peptides S1-S6 were screened against human keratinocytes (HaCaT) and RAW 264.7 cells.

Redox-Responsive Hyaluronic Acid-Tacrolimus Conjugate: Synthesis, Characterization, and Immunosuppressive Activity.

A redox-responsive macromolecular prodrug of tacrolimus, HA-ss-Tac, was constructed by conjugation of tacrolimus (TAC, FK506) through its succinate ester to cystamine-modified hyaluronic acid (HA-Cys), and its physicochemical properties and immunosuppressive activity were studied. The synthesized HA-ss-TAC was determined to contain 8% of chemically loaded TAC with significantly enhanced water solubility. The release study showed a sustained release of drug through slow degradation of linker-drug bonds.

Performance and complexity analysis using a sparse deep learning method for indoor terahertz transmission.

In this Letter, we propose and experimentally validate a sparse deep learning method (SDLM) for terahertz indoor wireless-over-fiber by transmitting a 16-quadrature amplitude modulation (QAM) orthogonal frequency-division multiplexing (OFDM) signal over a 15-km single-mode fiber (SMF) and a wireless link distance of 60 cm at 135 GHz through a cost-effective intensity-modulated direct detection (IM-DD) communications system. The proposed SDLM imposes the L1-regularized mechanism on the cost function, which not only improves performance but also reduces complexity when compared with traditional Volterra nonlinear equalizer (VNLE), sparse VNLE, and conventional DLM. Our experimental findings show that the proposed SDLM provides viable options for successfully mitigating nonlinear distortions and outperforms conventional VNLE, conventional DLM, and SVNLE with a 76%, 72%, and 61% complexity reduction, respectively, for 8-QAM without losing signal integrity.

Design and Fabrication of a Dual Protein-Based Trilayered Nanofibrous Scaffold for Efficient Wound Healing.

Chronic wound healing is a major threat all over the world. There are currently a plethora of biomaterials-based wound dressings available for wound healing applications. In this study, a dual protein-based (silk fibroin and sericin) nanofibrous scaffold from a natural source ( silkworm cocoons) with antibacterial and antioxidative properties for wound healing was investigated.

Computation efficient sparse DNN nonlinear equalization for IM/DD 112 Gbps PAM4 inter-data center optical interconnects.

In this Letter, we propose and experimentally demonstrate a novel, to the best of our knowledge, sparse deep neural network-based nonlinear equalizer (SDNN-NLE). By identifying only the significant weight coefficients, our approach remarkably reduces the computational complexity, while still upholding the desired transmission accuracy. The insignificant weights are pruned in two phases: identifying the significance of each weight by pre-training the fully connected DNN-NLE with an adaptive L2-regularization and then pruning those insignificant ones away with a pre-defined sparsity.

Reducing computation complexity by using elastic net regularization based pruned Volterra equalization in a 80 Gbps PAM-4 signal for inter-data center interconnects.

Volterra equalization (VE) presents substantial performance enhancement for high-speed optical signals but suffers from high computation complexity which limits its physical implementations. To address these limitations, we propose and experimentally demonstrate an elastic net regularization-based pruned Volterra equalization (ENPVE) to reduce the computation complexity while still maintain system performance. Our proposed scheme prunes redundant weight coefficients with a three-phase configuration.

Evaluation of the immunomodulatory and anti-inflammatory activity of Bakuchiol using RAW 264.7 macrophage cell lines and in animal models stimulated by lipopolysaccharide (LPS).

Bakuchiol (BAK) has been reported to have a diverse pharmacological property as an antibiotic, anti-cancer, anti-hypolipidemic, anti-inflammatory and anti-convulsant agent. This study aimed to elucidate the immunomodulation and anti-inflammatory mechanism of bakuchiol using lipopolysaccharide stimulated RAW 264.7 macrophages and various animal models.

Overlapping targets exist between the Par-4 and miR-200c axis which regulate EMT and proliferation of pancreatic cancer cells.

The last decade has witnessed a substantial expansion in the field of microRNA (miRNA) biology, providing crucial insights into the role of miRNAs in disease pathology, predominantly in cancer progression and its metastatic spread. The discovery of tumor-suppressing miRNAs represents a potential approach for developing novel therapeutics. In this context, through miRNA microarray analysis, we examined the consequences of Prostate apoptosis response-4 (Par-4), a well-established tumor-suppressor, stimulation on expression of different miRNAs in Panc-1 cells.

Par-4 activation restrains EMT-induced chemoresistance in PDAC by attenuating MDM-2.

Background: We recently reported prostate apoptosis response 4 (Par-4), a potential tumor suppressor protein restrains epithelial-mesenchymal transition (EMT) properties and promotes mesenchymal-epithelial transition (MET) in invasive cancer cells by repressing Twist-1 promoter activity. Here, we demonstrate that genetic as well as pharmacological modulation of Par-4 by NGD16 (a small molecule antimetastatic agent), limits EMT-induced chemoresistance in aggressive cancer cells by suppressing MDM-2, a downstream effector of Twist-1.

Methods: Matrigel invasion assay, gelatin degradation assay, cell scattering assay, MTT assay and colony formation assay were used to study the proliferation and migration abilities of invasive cancer cells.

Evaluation of the in vitro growth-inhibitory effect of epoxomicin on Babesia parasites.

Epoxomicin potently and irreversibly inhibits the catalytic activity of proteasomal subunits. Treatment of proliferating cells with epoxomicin results in cell death through accumulation of ubiquinated proteins. Thus, epoxomicin has been proposed as a potential anti-cancer drug.

Evaluation of adverse cardiac effects induced by arsenic trioxide, a potent anti-APL drug.

Arsenic trioxide (ATO/As2O3) is a promising drug for patients with a relapse of acute promyelocytic leukemia (APL); however, it frequently causes fatal arrhythmias. This study aims to investigate the various cellular and molecular mechanisms of adverse cardiac effects and the electrophysi-ological alterations caused by As2O3. We show the dose-dependent effect of ATO (0.

Modulation of haloperidol induced electrophysiological alterations on cardiac action potential by various risk factors and gender difference.

Haloperidol (HPL), well known antipsychotic drug can induce a marked QT prolongation and polymorphic arrhythmias. In this study we evaluated the influence of various induced risk factors such as electrolyte imbalance (hypokalemia and hypomagnesemia), gender difference, low pacing frequency, ischemia reperfusion insult on electrophysiological effect by haloperidol on electrically driven action potentials recorded from guinea pig papillary muscle. The doses of HPL ranging from 1 to 16 microM were used in this investigation.

Babesia bovis: effects of cysteine protease inhibitors on in vitro growth.

In the present study, we examined the effects of four kinds of cysteine protease inhibitors (E64, E64d, leupeptin, and ALLN) on the in vitro asexual growth of Babesia bovis. Of these, only the lipophilic inhibitors, E64d and ALLN, were found to effectively inhibit the growth of B. bovis.

Comparative evaluation of the sensitivity of LAMP, PCR and in vitro culture methods for the diagnosis of equine piroplasmosis.

The sensitivity of LAMP, PCR and in vitro culture methods for the detection of Theileria equi and Babesia caballi was evaluated using tenfold serially diluted culture parasites. On day 1 post-culture, both T. equi and B.