Article
Pharmacology & Pharmacy
Tina Blazevic, Gottfried Reznicek, Limin Ding, Gangqiang Yang, Patricia Haiss, Elke H. Heiss, Verena M. Dirsch, Rongxia Liu
Summary: This study demonstrates that esterification is a promising approach to enhance the in vivo bioavailability of rosmarinic acid in rats and the in vitro biological activity in rat vascular smooth muscle cells. The optimal alkyl chain length for esterification is between C1 and C4, while longer alkyl chains may lead to cytotoxicity.
FRONTIERS IN PHARMACOLOGY
(2021)
Review
Biochemistry & Molecular Biology
Huaquan Guan, Wenbin Luo, Beihua Bao, Yudan Cao, Fangfang Cheng, Sheng Yu, Qiaoling Fan, Li Zhang, Qinan Wu, Mingqiu Shan
Summary: Rosmarinic acid is a widely occurring polyphenolic acid in herbal plants with various biological activities, such as anti-inflammation, anti-oxidation, and anti-diabetes. Its natural derivatives have also been extensively studied. Despite the advancements in research, there are still unresolved issues regarding its toxicity and bioavailability.
Article
Microbiology
Sinenhlanhla Mtshali, Byron A. Jacobs
Summary: Physiologically based pharmacokinetic models have gained popularity in drug development and regulatory science. This study validates the model's effectiveness in predicting drug-drug interaction and the pharmacokinetics of antiretroviral and anti-TB drugs through mathematical solving and sensitivity analysis.
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY
(2022)
Review
Plant Sciences
Maja Hitl, Nebojsa Kladar, Neda Gavaric, Biljana Bozin
Summary: Rosmarinic acid, a phenolic compound commonly found in Lamiaceae plants, has various biological and pharmacological activities and beneficial health effects when ingested orally. Metabolized mainly by gut microflora and excreted through the kidneys, herbal remedies containing this compound have shown positive effects in skin diseases, allergies, and osteoarthritis. Future studies should focus on the long-term dynamics of its application in patients.
Article
Chemistry, Medicinal
Hyewon Chung, Jin-Woo Park, Dai-Hyun Kim, Soo-Hong Seo, Kyoung-Ah Kim, Woo-Shun Lee, Ji-Young Park
Summary: This study investigated the pharmacokinetics, pharmacodynamics, and safety/tolerability of MT921, an injectable cholic acid, in healthy volunteers after a single subcutaneous administration. The results showed that systemic exposure to cholic acid increased with dose escalation, while blood lipid profiles and deoxycholic acid levels were unaffected by MT921 treatment. Adverse events such as injection site pain and edema were mild and resolved without treatment.
Article
Pharmacology & Pharmacy
Yun Ju Kang, Chul Haeng Lee, Soo-Jin Park, Hye Suk Lee, Min-Koo Choi, Im-Sook Song
Summary: The study found that OAT1 and OAT3 are important transporters that may regulate the pharmacokinetic properties of rosmarinic acid and potentially cause herb-drug interactions with the compound.
Article
Engineering, Chemical
Muzaffar Iqbal, Mohammad Raish, Ajaz Ahmad, Essam A. Ali, Yousef A. Bin Jardan, Mushtaq A. Ansari, Mudassar Shahid, Abdul Ahad, Khalid M. Alkharfy, Fahad I. Al-Jenoobi
Summary: The study found that when Ibrutinib interacts with Sinapic acid, it may influence the pharmacokinetics of Ibrutinib and result in increased bioavailability. This may be due to the inhibition of IBR metabolism in the liver and intestines by SA.
Article
Infectious Diseases
Pierre Chauvelot, Celine Dupieux-Chabert, Lelia Abad, Aubin Souche, Tristan Ferry, Jerome Josse, Frederic Laurent, Florent Valour
Summary: The study demonstrated that dalbavancin has the ability to effectively eradicate intraosteoblastic reservoir of Staphylococcus aureus in bone and joint infections. It showed significant reduction in bacterial inoculum at both low concentration and standard therapeutic doses, with similar efficacy to vancomycin but less efficient than rifampicin. Dalbavancin was found to be the only molecule significantly active at a low concentration.
JOURNAL OF ANTIMICROBIAL CHEMOTHERAPY
(2021)
Article
Endocrinology & Metabolism
Ki Young Huh, Jun Gi Hwang, Wonjung Shin, Seungjae Baek, JaeDuk Choi, Nora Lee, Young Min Cho, Howard Lee
Summary: HM15136, a novel long-acting glucagon analogue, was shown to be safe and well tolerated in doses ranging from 10-120 μg/kg in a randomized, double-blind, placebo-controlled study. It increased blood glucose levels and suppressed the secretion of endogenous glucagon.
DIABETES OBESITY & METABOLISM
(2022)
Review
Pharmacology & Pharmacy
Li Zhou, Micaela B. Reddy, Rajendar K. Mittapalli, Jing Yang, Donghua Yin
Summary: Combination therapies are commonly evaluated in the clinical development of oncology investigational agents, and the design needs to consider factors such as drug interactions and benefit/risk to study participants. This report proposes application scenarios for different trial designs and emphasizes the importance of generating robust exposure-response data for optimal dose selection.
CLINICAL PHARMACOLOGY & THERAPEUTICS
(2023)
Article
Pharmacology & Pharmacy
Ana Alarcia-Lacalle, Helena Barrasa, Javier Maynar, Andres Canut-Blasco, Carmen Gomez-Gonzalez, Maria Angeles Solinis, Arantxazu Isla, Alicia Rodriguez-Gascon
Summary: This study developed a rapid, simple and reproducible HPLC-UV method for quantifying ceftaroline in plasma samples, which was accurate and stable, successfully applied in two critically ill patients.
Review
Infectious Diseases
Cornelia B. Landersdorfer, Amanda Gwee, Roger L. Nation
Summary: Traditionally, ongoing i.v. antibiotic therapy has been believed to be superior to early i.v. to oral switch for severe infections. However, this belief may not be based on robust data and contemporary clinical studies. This review examines the rationale for an early switch and discusses barriers and perceptions related to this practice.
CLINICAL MICROBIOLOGY AND INFECTION
(2023)
Article
Biochemical Research Methods
Shujie Fu, Qinglang Zhang, Shiyu Zhang, Weizhe Jiang, Minjie Jiang
Summary: The concentration of rosmarinic acid (RA) and its analog (E)-3-(3,4-dihydroxyphenyl)-2-(3-(3,4-dihydroxyphenyl)acrylamido)propanoic acid (A1) in rat plasma following oral administration was determined using liquid chromatography-tandem mass spectrometry. The developed method exhibited a linear relationship within the concentration ranges of 5-750 ng/ml for both RA and A1. This study is the first to concentrate on determining A1 and RA in rat plasma through oral administration, and the developed method provides a rapid, sensitive, and alternative approach for their accurate quantification and identification in vivo.
RAPID COMMUNICATIONS IN MASS SPECTROMETRY
(2023)
Article
Hematology
Julie Kanter, R. Clark Brown, Cynthia Norris, Santosh M. Nair, Abdullah Kutlar, Deepa Manwani, Nirmish Shah, Chiaki Tanaka, Shankaranand Bodla, Gessami Sanchez-Olle, Urs Albers, Darla Liles
Summary: This study analyzed the pharmacokinetics, pharmacodynamics, safety, and efficacy of crizanlizumab in patients with sickle cell disease. The results demonstrated the sustained efficacy and long-term safety of the drug in treating sickle cell disease.
Review
Plant Sciences
Xu-Ping Qian, Xue-Hui Zhang, Lu-Ning Sun, Wei-Fan Xing, Yu Wang, Shi-Yu Sun, Meng-Yuan Ma, Zi-Ping Cheng, Zu-Dong Wu, Chen Xing, Bei-Ning Chen, Yong-Qing Wang
Summary: This systematic review summarized and compared the medical applications of corosolic acid (CA) and its structural analogues, highlighting their activities in lowering blood sugar, anti-inflammation, and anti-tumor effects. Structural modification and formulation design can improve their oral absorption and bioavailability, making them promising lead compounds for further development and mechanistic studies.