Latest ArticlesPolysaccharides as one of the most common drug delivery materials have the excellent advantages, such as diverse natural sources, high biocompatibility and multi-functions. Polysaccharides have been investigated and widely used in food industry, pharmaceutical and medical fields especially in the targeted oral drug delivery for colonic diseases treatment with important research values and great potential applications. Inspired by the unique properties of polysaccharides, researchers around the world have developed the cross-linked nanoparticles, self-assembled nanoparticles and hydrogels, focusing on various drug delivery strategies such as pH-sensitive, microbial enzyme-responsive, reactive oxygen species-responsive, mucoadhesive and receptor-targeted. Exhilaratingly, the polysaccharides-based therapeutics have shown high efficacy for the treatment of digestive tract diseases, such as colitis or colonic cancer. Herein, we summarized the research progress of polysaccharides-based targeted oral drug delivery systems for colonic diseases treatment, and discussed the perspectives of the researches and application development in future.
The heat shock protein 20 (Hsp20) gene family plays an important role in regulating the stress response and plant development. The characteristics of Hsp20 in Cannabis sativa (CsHsp20), however, are still unclear. We systematically analyzed the CsHsp20 family based on the whole-genome and transcriptome database of Cannabis sativa using a series of bioinformatical tools. A total of 35 CsHsp20 genes (CsHsp20-1-CsHsp20-35) were identified in Cannabis sativa; they distribute onto 9 chromosomes and belong to 10 subfamilies, each with similar protein motifs. The promoter region of the CsHsp20 genes contains a variety of hormone-responsive and stress-responsive cis-elements, indicating that CsHsp20 genes are involved in plant growth and development and various stress responses. Protein interaction analysis showed that CsHsp20 proteins interacted with other members of the Hsp family and were regulated by transcription factors Hop and HSFA2. Transcriptome data showed that the expression levels of CsHsp20 genes were different among different tissues of Cannabis sativa and across different developmental stages. CsHsp20 genes were highly expressed mainly in hemp seed and its maturation stage, suggesting that CsHsp20 gene family members regulate the growth and development of hemp seed. Our research lays a foundation for the studying the function of CsHsp20 gene family and the directional cultivation of high-quality non-psychoactive medicinal cannabis.
To explore the protective effects and pharmacophore of verbascoside against oxygen-glucose deprivation/reperfusion (OGD/R)-induced neuronal cells injury, we used OGD/R-induced PC12 cells as a neuronal injury model. We investigated the neuroprotective effects of verbascoside and its structural fragments (caffeic acid 3, 4-dihydroxyphenethyl ester, caffeic acid, and 3, 4-dihydroxyphenylethanol) by MTT and crystal violet staining analysis. Moreover, we studied the protection of verbascoside and its structural fragments on mitochondria by Hoechst33258 staining, JC-1 staining and transmission electron microscope analysis. The neuroprotective mechanisms of verbascoside and its major active fragment caffeic acid were investigated by detecting B cell lymphoma 2 (Bcl 2)/Bcl 2 associated X protein (Bax)-dependent mitochondrial cysteinyl aspartate specific proteinase 3 (caspase 3)/poly ADP-ribose polymerase (PARP) apoptosis pathway by Western blot. The results showed that verbascoside, caffeic acid 3, 4-dihydroxyphenethyl ester and caffeic acid significantly improved cell viability and maintained normal PC12 cells morphology. These compounds also significantly reversed OGD/R-induced PC12 cells apoptosis, inhibited cell mitochondria depolarization, and maintained normal mitochondria structure. Furthermore, verbascoside and its major active fragment caffeic acid markedly inhibited the cleavage of mitochondrial apoptotic proteins caspase 3 and PARP, down-regulated Bax, and increased Bcl 2 expression. These results indicate that verbascoside protects OGD/R-induced neuronal cells injury via mitochondrial caspase 3/PARP apoptosis pathway, and caffeic acid may function as the major pharmacophore structure.
Tuberculosis (TB) is an enduring threat to global health. The epidemic persists with growing drug resistance, especially for extensively drug-resistant TB. Therefore, the treatment for TB and its associated multidrug resistance has been an ongoing challenge. Due to the greater attention and investment in the elimination of this disease, significant progress has been achieved. Bedaquiline, delamanid, and pretomanid have been approved for the clinical use. In addition, two dozens new anti-TB drugs are currently in clinical testing. China has contributed four new drugs TBI-223, TBI-166, aulimanid, and WX-081. The aim of this review is to summarize the recent advances in anti-TB drug development. Based on the different clinical stages of these anti-TB drugs, we mainly focus on mechanism of action, in vitro and in vivo pharmacological studies, pharmacokinetics and clinical studies.
The success of new drug discovery in 2021 can be affirmative, although the whole world is still suffering from COVID-19 pandemic. 50 new drugs were approved by the FDA's Center for Drug Evaluation and Research (CDER) last year. Among them, 27 were defined as first-in-class drugs, accounting for the highest number in the past decade. Notably, small molecule drugs still occupy a dominant position in first-in-class drugs with 15 drugs approved. Some of them were regarded as milestones for the drug discovery including sotorasib, a first small molecular covalent inhibitor targeting the "undruggable" target of the KRAS G12C; asciminib, a first small molecular allosteric inhibitor targeting the allosteric pocket of BCR-ABL1; belzutifan, a first small molecular inhibitor to inhibit HIF-2α; and vericiguat, a first small molecular sGC agonist for the treatment of chronic heart failure (CHF). First-in-class drugs rely on the discovery of novel targets and biological mechanisms, thus requiring different drug design approaches and being important guidance. In this review, we expect to provide research ideas and methods for more first-in-class drugs based on the research background, development process and therapeutic application of 3 first-in-class small molecule drugs in 2021.
As a kind of tumor immunotherapy, tumor vaccine provides a new strategy for cancer treatment. With nano-biomimetic materials to encapsulate the tumor antigens, the construction of nano-biomimetic tumor vaccine can target the tumor and release antigens, with high efficiency and safety. Therefore, nano-biomimetic vaccine has become a hot research topic. Based on this review, several new nano-biomimetic nanoparticles are summarized, and the clinical applications of the nano-biomimetic vaccine combined with other therapeutic strategies are introduced.
Sesterterpenoids, composed of five isoprene units and biosynthetically derived from geranylfarnesyl diphosphate (GFDP), are a class of the precious terpenoids with approximately 1 300 natural products known to date. Natural sesterterpenoids are widely distributed and possess extreme structural complexity and diversity and remarkable biological activity. In recent decades, a series of important progresses have been made in sesterterpenoid biosynthesis with the development of genome mining and heterogeneous expression technologies. This paper mainly focuses on the advances in sesterterpenoid biosynthesis, including the biochemical functions and catalytic mechanisms of GFDP synthases, sesterterpene synthases and oxidases. This review would lay the foundation for in-depth investigation on the biosynthesis, biological activities and synthetic biology of sesterterpenoids.
Recombinant human granulocyte colony stimulating factor (rhG-CSF) has been in clinical use for the adjuvant therapy of cancer patients with neutropenia caused by radiotherapy/chemotherapy. However, it does have some drawbacks such as poor stability and short half-life, and needs to be administered repeatedly, which is easy to cause adverse reactions such as drug tolerance and immune rejection. Therefore, it is necessary to develop long-acting rhG-CSF to improve its clinical efficacy. In this review, we summarize the research progress on the development of long-acting rhG-CSF using the strategies such as PEGylation, fusion protein and new dosage forms in recent years, and discuss its future development trend.
Inflammatory bowel disease (IBD) is a disease characterized by chronic and progressive inflammation of the intestinal tract, which seriously affects the quality of life of patients because it is difficult to cure and easy to recur. As the main organ of substance absorption, the changes of intestinal drug transporters will lead to changes in the behavior of endogenous and exogenous substances in vivo. Changes in the expression and function of a variety of drug transporters have also been observed in intestinal inflammatory tissues of patients with IBD. This paper reviews the changes of intestinal drug transporters in IBD and its related mechanisms, which provides a theoretical basis for finding new strategies for the treatment of IBD and clinical rational drug use.
Coronavirus disease 2019 (COVID-19) continues to be prevalent all over the world and mutant strains are constantly appearing, the application of vaccine is still an important method of epidemic prevention and control. Mucosal immunity plays an important role in preventing severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) invasion. The currently marketed injectable COVID-19 vaccine mainly activates humoral immunity, but it is difficult to induce effective mucosal immunity, and it is unable to prevent pathogen invasion in the early stage of virus infection. Compared with injection vaccination, inoculation of the COVID-19 vaccine through mucosal routes such as nasal or oral can closely imitate the natural infection pathway of the virus and induce a comprehensive immune response. It is an ideal choice for rapid and extensive vaccination because it has the advantages of simple and convenient use, easy to achieve self-management of vaccinators, reduced demand for professional medical personnel and so on. In this paper, we summarized and analyzed the products and technical platforms of COVID-19 vaccine inoculated by oral route, in order to provide reference for related research work.
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