Carbon dots (CDs) were synthesized hydrothermally by mixing citric acid (CA) and an antifolic agent, sulfanilamide (SNM), employed for pH sensing and bacterial growth inactivation. Sulfanilamide is a prodrug; aromatic hetero cyclization of the amine moiety along with other chemical modifications produces an active pharmacological compound (chloromycetin and miconazole), mostly administered for the treatment of various microbial infections. On the other hand, the efficacy of the sulfanilamide molecule as a drug for antimicrobial activity was very low. We anticipated that the binding of the sulfanilamide molecule on the carbon dot (CD) surface may form antibacterial CDs. Citric acid was hybridized with sulfanilamide during the hydrothermal preparation of the CDs. The molecular fragments of bioactivated sulfanilamide molecule play a crucial role in bacterial growth inactivation for Gram-positive and Gram-negative bacteria. The functional groups of citric acid and sulfanilamide were conserved during the CD formation, facilitating the zwitterionic behavior of CDs associated with its photophysical activity. At low concentrations of CDs, the antibacterial activity was apparent for Gram-positive bacteria only. This Gram-positive bacteria selectivity was also rationalized by zeta potential measurement.

2024-02-01·Journal of immunological methods

Novel hapten design, highly sensitive monoclonal antibody production, and immunoassay development for rapid screening of illegally added chloramphenicol in cosmetics

Article

作者: Qian, Jingqi ; Wang, Zhaoxiang ; Wang, Min ; Fu, Xiaoxiang ; Wang, Mian ; Tan, Guiyu

Hapten design and synthesis have been regarded as the key factor to generate high-quality antibodies. In the present study, a novel hapten of chloramphenicol was synthesized, characterized and compared with two conventional haptens. The new hapten generated mAb 4B5 showed higher sensitivity and titer than the other two haptens-based mAbs. The haptens synthesized with the structure of chloramphenicol base generated more sensitive antibodies than the hapten with chloramphenicol succinate, and the spacer arm linked to the phenyl group hapten elicited the strongest antibody response. After optimization, a direct competitive enzyme-linked immunosorbent assay (dcELISA) and a lateral flow immunoassay (LFIA), both based on the mAb 4B5, were developed. The dcELISA had a half maximum inhibition concentration of 0.23 ng/mL and the LFIA showed a cutoff value of 5-10 ng/mL. The LFIA was applied to detect illegally-added chloramphenicol samples in anti-acne cosmetics, five out of 19 samples were tested chloramphenicol containing within 10 min, which result was confirmed with the dcELISA and HPLC. The LFIA has an adequate sensitivity and can be used as a point of care diagnostic device for rapidly screening chloramphenicol in cosmetics.

2023-08-01·Current Drug Delivery

Self-emulsifying System Co-loaded with Paclitaxel and Coix Seed Oil Deeply Penetrated to Enhance Efficacy in Cervical Cancer

作者: Hu, Qiyan ; Chen, Yunyan ; Wang, Shaozhen ; Zhou, Lingyun

Background::

Paclitaxel (PTX), voted as the promising natural medicine molecules, is widely used in the treatment of cancers. Nevertheless, its clinical application was strictly limited by its poor water solubility.

Objective::

CP-MEs (Paclitaxel-coix seed oil coloaded microemulsion), a small sized self-emulsifying nanoemulsion formed of combination of PTX and coix seed oil (CSO) was developed in order to improve the solubility of paclitaxel and enhance anti-cervical cancer efficacy in vitro. CSO was selected as the oil phase to replace conventional organic solvents and achieve synergistic anti-tumor effect with paclitaxel.

Methods::

Pseudoternary phase diagram was applied to the study of CP-MEs formulation. CP-MEs was prepared and characterized by transmission electron microscopy (TEM) and dynamic light scattering (DLS). The encapsulation efficiency and drug loading efficiency (EE and LE) was detected by HPLC. MTT was adopted to evaluate the cytotoxicity of CP-MEs against HeLa cells. The cellular uptake and apoptotic ratio of CP-MEs was evaluated by flow cytometry. Notably, HeLa 3D tumor spheroid was adopted to evaluate tumor permeability of different size microemulsion as the model

Results::

The best self-emulsifying ability was exhibited by HS 15: PEG 400 combination. The appearance of CP-MEs was clear and transparent, which exhibited a small size (30.28 ± 0.36) and slight negative surface charge (-4.40 ± 1.13) mV. The EE and LE of CP-MEs were 98.80% and 0.978%, respectively. The cumulative release rate within 48 h of the CP-MEs was 80.21%. In cellular studies, the uptake of fluorescein isothiocyanate (FITC) labeled CP-MEs (FITC/C-MEs) was 17.86-fold higher than free FITC group，leading to significant synergistic anticancer activity in terms of cytotoxicity and apoptosis induction in vitro. The apoptotic rate of CP-MEs treated was 1.70-fold higher than PTX treated. Notably, the penetration of CP-MEs in HeLa 3D tumor sphere model was enhanced, which was related to deeply penetrated microemulsion of small size mediated at the tumor site.

Conclusion::

With the advantage of small sized self- emulsifying system，CP-MEs holds great potential to become an efficient nano drug delivery system of cervical cancer treatment in clinic.

项与 Chloramphenicol Sodium Succinate 相关的新闻（医药）

2023-07-12

·Science Daily

A step toward treating chemotherapy-resistant prostate cancer

Prostate cancer is a leading cause of death among American men, and it's resistant to one of the most powerful chemotherapy medications -- cisplatin. Now, researchers have developed the first therapy of its kind that disrupts prostate cancer cells' metabolism and releases cisplatin into the weakened cells, causing them to die. In mouse models, an orally administered version shrunk tumors substantially. Prostate cancer is a leading cause of death among American men, and it's resistant to one of the most powerful chemotherapy medications -- cisplatin. Now, researchers reporting in ACS Central Science have developed the first therapy of its kind that disrupts prostate cancer cells' metabolism and releases cisplatin into the weakened cells, causing them to die. In mouse models, an orally administered version shrunk tumors substantially. Cisplatin attacks testicular, breast, bladder, lung and ovarian cancer cells, damages their DNA and effectively destroys tumors. However, it's not effective against prostate cancer for reasons that are unclear to scientists, and many advanced cases of the disease don't respond to other therapies, such as androgen deprivation. Previously, researchers have shown in mouse models that as the disease advances, tumor cells shift from glycolysis toward fatty acid oxidation to support their growth and division. So, Shanta Dhar and colleagues from Sylvester Comprehensive Cancer Center at the University of Miami wanted to develop a therapy that would inhibit fatty acid oxidation in cancer cells by targeting a mitochondrial protein that is vital to the metabolic process, making the cells susceptible to cisplatin. The researchers verified that human prostate cancer cells thrive using fatty acid oxidation by assessing the biopsies of 38 people with the disease. Then they screened several cisplatin-containing prodrug compounds, which release the platinum-based molecule when they're broken down, to see if they could inhibit fatty acid oxidation. The cisplatin prodrug Platin-L, which has a cisplatin molecule bound to a 12-carbon fatty acid on one side and succinate on the other side, had the greatest effect by binding to a key protein required for long chain fatty acid transport, a primary step in this metabolic process. And in trials, Platin-L reduced the growth of prostate cancer cells by over 50% in several different cell lines. To develop a treatment that could be taken orally, the researchers encapsulated Platin-L in nanoparticles made with a biocompatible polymer that targeted prostate cancer cells. They administered the nanoparticles to mouse models with cisplatin-resistant prostate cancer and observed that the tumors shrunk, whereas tumors in animals treated with saline or cisplatin grew. Additionally, the Platin-L nanoparticle-treated mice had steady body weight, increased survival rates and didn't display peripheral neuropathy. Because the treatment affects fatty acid metabolism, which can be elevated in other types of cancers, the researchers say their type of additive Platin-L therapy may also be applicable to additional aggressive and chemotherapy-resistant cancers.

100 项与 Chloramphenicol Sodium Succinate 相关的药物交易

登录后查看更多信息