Jul 06,2023

開發和驗證大鼠血漿中Nobiliside A定量的LC/MS/MS方法

Nobiliside A, a new triterpene glycoside, exhibits some biological activities including antifungal and cytotoxic effects. A LC/MS/MS method was developed and validated for determination of Nobiliside A in rat plasma, would prove to be useful for other pharmacokinetic assessments. Male SD rats were housed in Medicilon animal facility. The animal experiments of the present study were approved by IACUC of Medicilon and were carried out in accordance with the SOPs of the facility.

Jul 06,2023

4-正丁基間苯二酚是一種高效的酪氨酸酶抑制劑，可用于化妝品中以達到脫色的目的。其中經皮吸收和皮膚分布研究通過尊龍凱時進行

4-n-butyl resorcinol (4-nBR) is a highly effective tyrosinase inhibitor, and can be used in cosmetic product for depigmentation purpose. Its efficacy correlates with 4-nBR that absorbed by skin. In this study, skin distribution of 4-nBR within either human or pig skin ex vivo was studied and compared by three independent laboratories. Good agreement was observed in each compartment considering usual inter-lab variability. The percutaneous absorption and skin distribution studies were carried out by L'Oréal (lab A), Fudan University (lab B), and Medicilon (lab C).

Jul 06,2023

Columbin具有多種藥理活性，包括體內抗炎和抗腫瘤活性，此實驗中動物研究通過尊龍凱時進行

Columbin is an important component isolated from Radix Tinosporae. Columbin possesses many pharmacological activities, including anti-inflammation, and antitumor activity in vivo. The purpose of the present study was to examine in vivo pharmacokinetics and bioavailability of Columbin in rats using a high-performance liquid chromatography coupled with tandem mass spectrometry quantitative detection method. This is the first study demonstrating the bioanalytical method and pharmacokinetic of Columbin. Animal studies were carried out in Medicilon.

Jul 06,2023

PTX-HSN是一種高效納米系統，具有較高耐受劑量，可將PTX遞送至卵巢癌并增強主動腫瘤靶向性。此研究中所有體內實驗均通過尊龍凱時進行

Paclitaxel-loaded hyaluronan solid nanoemulsions (PTX-HSNs) were successfully fabricated for the delivery of PTX to improve ovarian cancer treatment via active tumor targeting. The in vivo toxicity, in vivo antitumor effects, and pharmacokinetics of PTX-HSNs and Taxol were evaluated in nude mice and rats. PTX-HSN is a highly effective nanosystem with a high maximum tolerated dose (MTD) for delivering PTX to ovarian cancers characterized by CD44 overexpression, enhanced active tumor targeting, and low toxicity. All in vivo experiments were conducted with the approval of the Association for Assessment and Accreditation of Laboratory Animal Care (AAALAC) International (tested at Medicilon/MPI Preclinical Research).

Jul 06,2023

開發一種簡單準確的液相色譜串聯質譜法，用于大鼠血漿中牡荊素鼠李糖苷的測定和體內PK研究。此研究中動物研究通過尊龍凱時進行

A simple and accurate liquid chromatography coupled with tandem mass spectrometry method was developed for determination and in vivo pharmacokinetic studies of vitexin rhamnoside in rat plasma. Practical utility of this new LC/MS/MS method was confirmed in pilot pharmacokinetic studies in rats following both intravenous and oral administration. Animal studies were carried out in Medicilon.

Jul 06,2023

AD80是一種多激酶抑制劑，在多種肝細胞癌臨床前動物模型中具有抗腫瘤活性，AD80在血漿中的含量通過尊龍凱時進行LC-MS/MS測定

Liver cancer is the fourth greatest cause of cancer related mortality. AD80 is a multi-kinase inhibitor with anti-tumoral activity across a variety of hepatocellular carcinoma (HCC) preclinical models, including mouse xenografts. AD80 is highly active in a tumor xenograft model. Experimental dosing for AD80 was determined from maximum tolerated dosage (MTD) studies and pharmacokinetic (PK) analysis. Quantities of AD80 in blood plasma were determined by LC-MS/MS at Medicilon.

Jul 06,2023

以PROTAC為代表的靶向蛋白質降解是藥物發現的新興策略，研究人員設計并合成了多種PROTAC，此研究中所有PK研究均通過尊龍凱時進行

Targeted protein degradation (TPD) exemplified by PROTACs is an emerging strategy for next generation drug discovery. Threonine tyrosine kinase (TTK) is a dual-specific protein kinase that catalyzes phosphorylation of both serine/threonine and tyrosine residues. Researchers designed and synthesized TTK PROTACs, which demonstrated reasonable pharmacokinetic profiles. All the pharmacokinetic studies were carried out by Medicilon, according to the protocols and guidelines of the institutional care and use committee.

Jul 06,2023

氯磺丙脲對蠕蟲和人肺成纖維細胞MRC-5細胞具有抗衰老作用，氯磺丙脲在小鼠中的生物利用度測定通過尊龍凱時進行

Sulfonylureas exert their anti-diabetic effects by inhibiting K-ATP channels in the plasma membrane of islet β-cells. Chlorpropamide acts on complex II directly or indirectly via mitoK-ATP to produce mtROS as a pro-longevity signal. Chlorpropamide has an anti-aging effect on worms and human lung fibroblast MRC-5 cells. Determination of Chlorpropamide bioavailability in mice was performed by Medicilon.

Jul 06,2023

BRD4抑制劑可用于治療腎纖維化，ZLD2218可有效抑制BRD4活性，對ZLD2218的PK研究通過尊龍凱時進行

Uncovering new therapeutics for kidney fibrosis hold promise for chronic kidney disease (CKD). BRD4 inhibition ameliorated kidney injury and fibrosis. ZLD2218 exhibited the potent inhibitory activity against BRD4, with the IC50 value of 107?nM. Pharmacokinetic analysis of of ZLD2218 were analyzed by noncompartmental methods using Phoenix WinNonlin 7.0 (Accomplished by Medicilon).

Jul 06,2023

免疫檢查點阻斷療法改變了癌癥治療的范式，此研究中通過尊龍凱時在23 個同源腫瘤模型中進行了抗PD-1抗體的體內研究

Immune checkpoint blockade therapies have changed the paradigm of cancer therapies. Reseachers performed in vivo screening for anti-PD-1 therapy across 23 syngeneic tumor models and found that CT-26 and Colon 26, which are murine colorectal carcinoma derived from BALB/c mice, showed different sensitivity to anti-PD-1. In vivo studies for anti-PD-1 antibody across 23 syngeneic tumor models were performed by Medicilon.