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Synthesis and evaluation of cardamonin derivatives as antiproliferative agents to human cancer cells
Selvaraj Baskar,이상혁,Sang Nguyen Qui Ngoc,이희수,이재욱 대한화학회 2023 Bulletin of the Korean Chemical Society Vol.44 No.3
Twenty novel cardamonin derivatives were synthesized and evaluated for antiproliferative activity against four cancer cell lines (HT-29, DLD-1, MDA-MB-231, and HepG2). Among the derivatives, SWA2 showed the most potent effects with an IC50 value of 4.43–11.0 μM against three cancer cell lines except for HepG2. Further investigation showed that SWA2 induced cancer cell death by apoptosis. Flow cytometry analysis showed that SWA2 treatment increased the ratio of apoptotic and dead cells. Further western blot analysis revealed that SWA2 treatment increased cleaved PARP. In summary, SWA2 can be utilized as a lead structure for anticancer therapy.
Neuroprotective Mechanism of Corydaline in Glutamate-Induced Neurotoxicity in HT22 Cells
Baskar Selvaraj,Dae Won Kim,Ki Yeon Yoo,Keunwan Park,Thi Thu Thuy Tran,Jae Wook Lee,Heesu Lee 대한구강생물학회 2024 International Journal of Oral Biology Vol.49 No.1
Glutamate-mediated oxidative stress causes neuronal cell death by increasing intracellular Ca 2+ uptake, reactive oxidative species (ROS) generation, mitogen-activated protein kinase (MAPK) activation, and translocation of apoptosis-inducing factor (AIF) to the nucleus. In the current study, we demonstrated that corydaline exerts potent neuroprotective effects against glutamate-induced neurotoxicity. Treatment with 5 mmol/L glutamate increased cellular Ca 2+ influx, ROS generation, MAPK activation, and AIF translocation. In contrast, corydaline treatment decreased cellular Ca 2+ influx and ROS generation. Western blot analysis revealed that glutamate-mediated MAPK activation was attenuated by corydaline treatment. We further demonstrated that corydaline treatment inhibited the glutamate-mediated translocation of AIF to the nucleus. We propose that corydaline is a promising lead structure for the development of safe and effective neuroprotectants.
Flavonoids as anti-inflammatory and neuroprotective agents
Lee, Heesu,Selvaraj, Baskar,Yoo, Ki Yeon,Ko, Seong-Hee The Korean Academy of Oral Biology 2020 International Journal of Oral Biology Vol.45 No.2
Neuroinflammation is known as the main mechanism implicated in the advancement of neurodegenerative diseases such as Alzheimer's disease and Parkinson's disease. The main feature of neuroinflammation is associated with the activation of microglia. The activated microglia increase proinflammatory cytokine production and induce progressive neuronal cell death. Citrus flavonoids show neuroprotective effects that are associated with the anti-inflammatory action of flavonoids in neurodegenerative diseases. Among these citrus flavonoids, kaempferol, naringin, and nobiletin show inhibitory effects on nuclear factor-κB and mitogen-activated protein kinase signaling pathways that can modulate inflammatory conditions in microglial cells. In the present review, we present the anti-inflammatory activities of citrus flavonoids and therapeutic potential of flavonoids as neuroprotective agents.
Enhanced lipid content in Chlorella sp. FC2 IITG via high energy irradiation mutagenesis
Debasish Das,Baskar Selvaraj,Basavaraj Palabhanvi,Vikram Kumar,Muthusivaramapandian Muthuraj 한국화학공학회 2019 Korean Journal of Chemical Engineering Vol.36 No.1
High energy ultra-violet radiation was used to induce mutations in the wild type strain Chlorella sp. FC2 IITG and the mutants obtained were screened for enhanced lipid content targeted towards biodiesel production. Screening of mutants under nitrogen starved photoautotrophic condition showed five mutant strains with higher lipid content as compared to the wild type strain. Maximum neutral lipid content of 22.26% (w/w, DCW) was found for FC2-25UV mutant strain, which was 48.4% higher than that of wild type culture. Further characterization under photoautotrophic two stage high cell density cultivation of lipid rich FC2-25UV resulted in total lipid content of 68% (w/w, DCW), which was 21.43% higher than the wild type strain with a marginal improvement of 11% in the total lipid productivity. Comparison of enzyme activity assays under nitrogen starved conditions in both the strains revealed an 18.2% and 31.25% increase in acetyl CoA carboxylase and di-acyl-glycerol transferase activity of mutant. The FAME composition analysis showed 41.5% and 24% increase in the fractions of C18:2 and C18:1 in the mutant strain when compared to the wild type strain with no significant difference in the other FAME fractions. Thus, the mutant strain could be a potential candidate for biodiesel production.
Synthetic Anion Transporters as Endoplasmic Reticulum (ER) Stress Inducers
Aslam, Adil S.,Fuwad, Ahmed,Ryu, Hyunil,Selvaraj, Baskar,Song, Jae-Won,Kim, Dae Won,Kim, Sun Min,Lee, Jae Wook,Jeon, Tae-Joon,Cho, Dong-Gyu American Chemical Society 2019 ORGANIC LETTERS Vol.21 No.19
<P>Cl<SUP>-</SUP>-ion transporters (<B>2a</B>-<B>2h</B>) were synthesized based on the binding motifs of prodigiosin. Transporter <B>2e</B> clearly displays Cl<SUP>-</SUP>-ion transportation activity across both model and live cell membranes. Furthermore, <B>2e</B> can disrupt Ca<SUP>2+</SUP> homeostasis and increase the intracellular concentration of Ca<SUP>2+</SUP> in the DLD-1 cell. This disruption can lead to Caspase-dependent apoptosis supported by CHOP expression (a marker of ER stress) and the appearance of the cleaved forms of Caspase 3 and PARP.</P> [FIG OMISSION]</BR>