Echinacoside alleviates glucocorticoid induce osteonecrosis of femoral head in rats through PI3K/AKT/FOXO1 pathway
We examined the protective effect of Ech against SONFH using in vivo and in vitro experiments. Specifically, dexamethasone (Dex) decreased p-PI3K and p-AKT levels, which were reversed following Ech addition. Validation of the PI3K inhibitor (LY294002) and molecular docking of Ech and PI3K/AKT further indicated that Ech could directly enhance PI3K/AKT activity to alleviate Dex-induced inhibition. Interestingly, Dex upregulated the expression of FOXO1, Bax, cleaved-caspase-9, and cleaved-caspase-3 and enhanced MC3T3-E1 apoptosis; application of Ech and siRNA-FOXO1 reversed these effects. In vitro, Ech decreased the number of...
Source: Chemico-Biological Interactions - February 9, 2024 Category: Molecular Biology Authors: Liang Kun Huang Xiao Shuang Zeng Ze Wen Jiang Hao Peng Fei Sun Source Type: research

Myt1 kinase inhibitors - Insight into structural features, offering potential frameworks
Chem Biol Interact. 2024 Feb 6;391:110901. doi: 10.1016/j.cbi.2024.110901. Online ahead of print.ABSTRACTThe cell cycle includes two checkpoint arrests allowing to repair of damaged DNA. Many cancer cell lines exhibit weak G1 checkpoint mechanisms relying significantly more on the G2 checkpoint than do healthy cells. Inhibition of Myt1 kinase (PKMYT1), a forgotten member of the Wee family, cyclin-dependent kinase 1 (Cdk1) inhibitory kinase, target for G2 checkpoint abrogation, whose inhibition forces cells into premature unchecked mitosis resulting in cell death, is a promising concept for anticancer therapy. There are not...
Source: Chemico-Biological Interactions - February 8, 2024 Category: Molecular Biology Authors: Katarina Tomovi ć Pavlović Gordana Koci ć Andrija Šmelcerović Source Type: research

Role of microsomal metabolism in bromfenac-induced cytotoxicity
In conclusion, this research sheds light on the metabolic intricacies leading to cytotoxicity induced by bromfenac, especially emphasizing the role of UGT-dependent metabolism and the formation of reactive intermediates like bromfenac lactam. These findings offer insight into the mechanistic basis of DILI and emphasize the importance of understanding metabolism-mediated toxicity.PMID:38331335 | DOI:10.1016/j.cbi.2024.110903 (Source: Chemico-Biological Interactions)
Source: Chemico-Biological Interactions - February 8, 2024 Category: Molecular Biology Authors: Jang Su Jeon Hyemin Kim Seongyea Jo Jaehoon Sim Sang Kyum Kim Source Type: research

Different concentrations of betaxolol switch cell fate between necroptosis, apoptosis, and senescence in human corneal stromal cells
In this study, we used in vitro HCSCs and in vivo rabbit corneal models to investigate betaxolol cytotoxic effects and mechanism of action. At near-clinical concentrations (0.28% and 0.14%), betaxolol inhibited caspase-8 activity, activated receptor-interacting protein kinase (RIPK)1, RIPK3, and mixed-spectrum kinase-like domain (MLKL), and phosphorylated MLKL to induce necroptosis in HCSCs. Similarly, moderate concentrations of betaxolol (0.07%-0.0175%) activated caspase-8 to trigger the exogenous apoptotic pathway. Through the intrinsic apoptotic pathway, betaxolol upregulated the expression of Bcl-2 family apoptotic pro...
Source: Chemico-Biological Interactions - February 7, 2024 Category: Molecular Biology Authors: Jing-Yu Sun Jun Zha Yue Qiu Ting-Jun Fan Source Type: research

Change in function and homeostasis of HPA axis: The role of vitamin family
Chem Biol Interact. 2024 Feb 5;391:110899. doi: 10.1016/j.cbi.2024.110899. Online ahead of print.ABSTRACTWith the improvement of living quality, people pay more and more attention to vitamin supplements. The vitamins in the daily diet can meet the needs of the body. Whether additional vitamin supplementation is necessary still needs to be further explored. Many studies have reported that vitamin deficiency and excessive vitamin supplementation could lead to abnormal development in the body or increase the risk of diseases. Here, we summarize the abnormal levels of vitamins can cause the homeostasis imbalance of hypothalamu...
Source: Chemico-Biological Interactions - February 7, 2024 Category: Molecular Biology Authors: Xuan Xia Kaiqi Chen Yawen Chen Source Type: research

Co-treatment with melatonin and ortho-topolin riboside reduces cell viability by altering metabolic profiles in non-small cell lung cancer cells
Chem Biol Interact. 2024 Feb 5:110900. doi: 10.1016/j.cbi.2024.110900. Online ahead of print.NO ABSTRACTPMID:38325522 | DOI:10.1016/j.cbi.2024.110900 (Source: Chemico-Biological Interactions)
Source: Chemico-Biological Interactions - February 7, 2024 Category: Molecular Biology Authors: Ji Won Lee Hwanhui Lee Soon-Wook Noh Hyung-Kyoon Choi Source Type: research

Layered double hydroxides (LDHs) as efficient and safe carriers for miRNA inhibitors: In vitro and in vivo assessment of biocompatibility
In conclusion, our data suggest that LDHs are biocompatible and efficient carriers for miRNA inhibitors and can be used as a viable and effective tool in functional miRNA inhibition assays.PMID:38311162 | DOI:10.1016/j.cbi.2024.110874 (Source: Chemico-Biological Interactions)
Source: Chemico-Biological Interactions - February 4, 2024 Category: Molecular Biology Authors: Mykaella Andrade de Ara újo Erivaldo Davi Dos Santos J únior Bruna Priscila Dos Santos Ygor Daniel Ramos Dos Santos Pedro Augusto Tib úrcio Paulino Elane Concei ção Dos Santos Tayhana Priscila Medeiros Souza Lucas Anhezini Ênio José Bassi Marcelo D Source Type: research

Casticin ameliorates osteoarthritic cartilage damage in rats through PI3K/AKT/HIF-1 α signaling
Chem Biol Interact. 2024 Feb 1;391:110897. doi: 10.1016/j.cbi.2024.110897. Online ahead of print.ABSTRACTKnee osteoarthritis (KOA) is a chronic, disabling knee joint lesion in which degeneration and defects in articular cartilage are the most important features. Casticin (CAS) is a flavonoid extracted from the Chinese herb Vitex species that has anti-inflammatory and antitumor effects. The aim of this study was to investigate the therapeutic and mechanistic effects of CAS on cartilage damage in KOA. A KOA rat model was established by anterior cruciate ligament transection (ACLT), and cartilage morphological changes were as...
Source: Chemico-Biological Interactions - February 3, 2024 Category: Molecular Biology Authors: Deren Liu Wei Mei Junfeng Kang Taiyang Liao Yibao Wei Lishi Jie Lei Shi Peimin Wang Jun Mao Peng Wu Source Type: research

Pholiotic acid promotes apoptosis in human metastatic melanoma cells
In conclusion, these findings, starting point for further investigation, implement available our data to support pholiotic acid as an attractive potential chemopreventive agent, and provide a basis for further research into the use of this polyamine derivative as potential anticancer agent for melanoma in combination with existing therapies to improve treatment efficacy and overcome the obstacle of drug resistance.PMID:38301881 | DOI:10.1016/j.cbi.2024.110894 (Source: Chemico-Biological Interactions)
Source: Chemico-Biological Interactions - February 1, 2024 Category: Molecular Biology Authors: R Avola A C E Graziano A Madrid M Clericuzio V Cardile A Russo Source Type: research

Aldo-keto reductases 7A subfamily: A mini review
Chem Biol Interact. 2024 Jan 30:110896. doi: 10.1016/j.cbi.2024.110896. Online ahead of print.ABSTRACTAldo-keto reductase-7A (AKR7A) subfamily belongs to the AKR superfamily and is associated with detoxification of aldehydes and ketones by reducing them to the corresponding alcohols. So far five members of ARK7A subfamily are identified: two human members-AKR7A2 and AKR7A3, two rat members-AKR7A1 and AKR7A4, and one mouse member-AKR7A5, which are implicated in several diseases including neurodegenerative diseases and cancer. AKR7A members share similar crystal structures and protein functional domains, but have different s...
Source: Chemico-Biological Interactions - February 1, 2024 Category: Molecular Biology Authors: Mengli Zhao Jiajin Chen Hongyu Chen Jingdong Zhang Dan Li Source Type: research

Mechanisms of action of mineral fibres in a placental syncytiotrophoblast model: An in vitro toxicology study
Chem Biol Interact. 2024 Feb 25;390:110895. doi: 10.1016/j.cbi.2024.110895. Epub 2024 Feb 1.ABSTRACTAsbestos has been widely used due to its unique characteristics. It is known that exposure to asbestos causes serious damage to health but one species, chrysolite, is still used because it is considered less toxic and not biopersistent in some countries. The aim of our study was to investigate if cellular process underlying the proliferation, differentiation and cell death of placental tissues could be modify in presence of asbestos fibres (50 μg/ml final concentration), long chrysolite fibres (CHR-L) and short chrysolite f...
Source: Chemico-Biological Interactions - February 1, 2024 Category: Molecular Biology Authors: Sonia Fantone Giovanni Tossetta Laura Cianfruglia Andrea Frontini Tatiana Armeni Antonio D Procopio Armanda Pugnaloni Alessandro F Gualtieri Daniela Marzioni Source Type: research

PPAR γ activation in chondrocytes alleviates glucocorticoid-induced oxidative stress, mitochondrial impairment, and pyroptosis via autophagic flow enhancement
This study investigated the role of glucocorticoids, specifically dexamethasone, in OA progression, with a particular focus on their effects on chondrocytes. Although glucocorticoids are commonly used for OA pain relief, our research demonstrated that high concentrations of dexamethasone may accelerate OA progression by enhancing the ability of reactive oxygen species to inhibit chondrocyte autophagy, resulting in cell death and accelerated cartilage degeneration. Despite reports on the acceleration of pathogenesis and cartilage damage in some patients of OA taking corticosteroids, the mechanism behind the same has not bee...
Source: Chemico-Biological Interactions - January 29, 2024 Category: Molecular Biology Authors: Dengying Wu Zhenyu Shen Yong Gou Tao Yu Jiaqian Hong Yitong Wang Feifei Ni Naren Qiqige Hongwei Lu Enxing Xue Source Type: research

Pharmacokinetic interactions of niclosamide in rats: Involvement of organic anion transporters 1 and 3 and organic cation transporter 2
Chem Biol Interact. 2024 Feb 25;390:110886. doi: 10.1016/j.cbi.2024.110886. Epub 2024 Jan 25.ABSTRACTNiclosamide is an anthelmintic drug with a long history of use and is generally safe and well tolerated in humans. As the conventional dose of niclosamide results in a low but certain level in systemic circulation, drug interactions with concomitant drugs should be considered. We aimed to investigate the interaction between niclosamide and drug transporters, as such information is currently limited. Niclosamide inhibited the transport activity of OATP1B1, OATP1B3, OAT1, OAT3, and OCT2 in vitro. Among them, the inhibitory ef...
Source: Chemico-Biological Interactions - January 27, 2024 Category: Molecular Biology Authors: Min-Ji Kang Min Ju Kim Aeran Kim Tae-Sung Koo Kyeong-Ryoon Lee Yoon-Jee Chae Source Type: research

Fisetin suppresses chondrocyte senescence and attenuates osteoarthritis progression by targeting sirtuin 6
This study found SIRT6 level to be negatively correlated with OA severity. SIRT6 downregulation was validated in the joint cartilages of DMM rats and IL-1β-treated chondrocytes. It was also notably demonstrated that FST can activate SIRT6. Both the administration of FST and activation of SIRT6 using MDL were found to rescue cartilage erosion, decrease extracellular matrix (ECM) degradation, prevent cartilage from apoptosis, and improve detrimental senescence-related phenotype. The alleviative effects of FST against inflammation, ECM degradation, apoptosis, and senescence in IL-1β-stimulated chondrocytes were also confirm...
Source: Chemico-Biological Interactions - January 26, 2024 Category: Molecular Biology Authors: Xuezhong Wang Xuyang Li Jianlin Zhou Zheng Lei Xiaoming Yang Source Type: research

f25, a novel synthetic quinoline derivative, inhibits tongue cancer cell invasion and survival by the PPAR pathway in vitro and vivo
Chem Biol Interact. 2024 Jan 24;391:110891. doi: 10.1016/j.cbi.2024.110891. Online ahead of print.ABSTRACTTongue cancer has a very high incidence in China, and there is a need to develop new anti-tumour drugs against it. We synthesised 31 novel quinoline derivatives to test their anti-tumour activity. A compound referred to as "f25" was identified through screening for its high in vitro toxicity against an oral squamous carcinoma cell line (CAL-27). f25 exhibited significant cytotoxicity against CAL-27 cells (IC50 = 7.70 ± 0.58 μΜ). f25 also inhibited the migration and invasion of CAL-27 cells to a level comparable with...
Source: Chemico-Biological Interactions - January 26, 2024 Category: Molecular Biology Authors: Tuo Liu Lili Yang Zeng Li Ming Sun Na Lv Source Type: research