53,283 results match your criteria medicinal drugs

Arsenic compounds: The wide application and mechanisms applied in acute promyelocytic leukemia and carcinogenic toxicology.

Eur J Med Chem 2021 May 4;221:113519. Epub 2021 May 4.

School of Chinese Materia Medica, Beijing University of Chinese Medicine, Beijing, 100029, China. Electronic address:

Arsenic (As), as well as its various compounds have been widely used for nearly 4000 years either as drugs or poisons. These compounds are valuable in the treatment of various diseases ranging from dermatosis to cancer, thereby emphasizing their important roles as therapeutic agents. The ability of As compounds, especially arsenic trioxide (ATO) in the treatment of acute promyelocytic leukemia (APL), has fundamentally altered people's understanding of the poison, and has become a major factor in the re-emergence of Western medicine candidates to treat leukemia and other solid tumors. Read More

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Design, synthesis, and biological evaluation of novel tetrahydroprotoberberine derivatives to reduce SREBPs expression for the treatment of hyperlipidemia.

Eur J Med Chem 2021 May 5;221:113522. Epub 2021 May 5.

State Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing, 210009, China; Department of Medicinal Chemistry, School of Pharmacy, China Pharmaceutical University, Nanjing, 210009, China. Electronic address:

Statins play an important role in the treatment of hyperlipidemia, but drug resistance and adverse effects greatly limits their application. To discover new lipid-lowering drugs, three different series of tetrahydroprotoberberine derivatives (THPBs) were designed and synthesized. These compounds were first tested for their effects on viability of HepG2 cells and 21 compounds with the percent of cell viability over 90% were further screened to evaluate their ability to reduce total cholesterol (TC) and triglyceride (TG) levels. Read More

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Small Molecule with Bridged Carbonyl and Tri-fluoro-aceto-phenone Groups Impedes Microtubule Dynamics and Subsequently Triggers Cancer Cell Apoptosis.

ChemMedChem 2021 May 13. Epub 2021 May 13.

Indian Institute of Technology Jodhpur, Depepartment of Biosecience and Bioengineeering, NH 62, Nagaur Road, 342037, Jodhpur, INDIA.

We identified a new class of microtubule targeted small molecule, which showed significant anticancer activity and induces apoptotic death of cancer cells. Precisely the central bridged carbonyl group and trifluoro-acetophenone group of a bis-benzothiazole molecule (BBT) interacts with tubulin close to the curcumin site and perturbs microtubule dynamics as well as causes microtubule depolymerization. We observed a significant enhancement of fluorescence while BBT interacts with the tubulin through bridged carbonyl moiety, a similar phenomenon to colchicine. Read More

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[Development of clinical trial of new drugs of traditional Chinese medicines].

Zhongguo Zhong Yao Za Zhi 2021 Apr;46(7):1691-1695

Shuguang Hospital Affiliated to Shanghai University of Traditional Chinese Medicine Shanghai 201203, China.

The relevant laws and regulations of drug clinical trials were introduced in this paper. It is pointed out that with drug re-gulatory laws and technological advances, clinical trials have become an important link in the development of new drugs of traditional Chinese medicines(TCM). Clinical trials of new drugs of TCM must comply with the requirement of "Good Clinical Practice for Trial on Medicinal Products". Read More

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[Critical quality attribute assessment of big brand traditional Chinese medicine: quality control of Tongren Niuhuang Qingxin Pills in texture and sensory attributes].

Zhongguo Zhong Yao Za Zhi 2021 Apr;46(7):1598-1605

School of Chinese Materia Medica, Beijing University of Chinese Medicine Beijing 102488, China Engineering Research Center of Chinese Medicine Production and New Drug Development, Ministry of Education Beijing 102488, China.

Texture sensory attributes are the key items in quality control of Chinese medicinal honeyed pills. The purpose of this study is to develop a quality control method for assessing the texture sensory attributes of Chinese medicinal honeyed pills based on real-world Tongren Niuhuang Qingxin pilular masses and finished products. First, parameters of texture profile analysis(TPA) were optimized through single factor and central composite design(CCD) experiments to establish a detection method for texture sensory attri-butes of Tongren Niuhuang Qingxin Pills. Read More

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Micro-nano particulate compositions of Hypericum perforatum L in ultra high diluted succussed solution medicinal products.

Heliyon 2021 Apr 19;7(4):e06604. Epub 2021 Apr 19.

Department of Materials Science and Engineering, School of Chemical Engineering, NTUA, GR15780 Athens, Greece.

The fact that many patients all over the world use homeopathic ultra high diluted succussed medicinal products, makes very interesting an explanation about the structure of them since until now only unconfirmed hypotheses are made. The present study focuses on the still unanswered questions about what happens with the chemical composition and the physicochemical properties of these products using Hypericum Perforatum L as a representative paradigm. All samples were prepared according to manufacturing procedures described mainly in S. Read More

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Icariside II: Anticancer Potential and Molecular Targets in Solid Cancers.

Front Pharmacol 2021 26;12:663776. Epub 2021 Apr 26.

Department of Neurology, Affiliated Hospital of Shandong University of Traditional Chinese Medicine, Jinan, China.

Icariside II, an active flavonoid, is extracted from the traditional Chinese medicinal herb . It possesses multiple biological and pharmacological properties, including anti-inflammatory, anticancer, and anti-osteoporotic properties. In recent years, apoptosis has become the hot spot in anticancer therapies. Read More

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L. Regulates Glutathione Redox Stress and Normalizes Ggt1/Anpep Signaling to Alleviate OVX-Induced Kidney Dysfunction.

Front Pharmacol 2021 26;12:628651. Epub 2021 Apr 26.

Shaanxi Province Key Laboratory of New Drugs and Chinese Medicine Foundation Research, Shaanxi Collaborative Innovation Center Medicinal Resources Industrialization, Shaanxi University of Chinese Medicine, Xianyang, China.

Menopause and associated renal complications are linked to systemic redox stress, and the causal factors remain unclear. As the role of L. (HPL) in menopause-induced kidney disease therapy is still ambiguous, we aim to explore the effects of HPL on systemic redox stress under ovariectomy (OVX)-induced kidney dysfunction conditions. Read More

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Therapeutic Potentials of Antiviral Plants Used in Traditional African Medicine With COVID-19 in Focus: A Nigerian Perspective.

Front Pharmacol 2021 26;12:596855. Epub 2021 Apr 26.

Department of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Ibadan, Ibadan, Nigeria.

The coronavirus disease 2019 (COVID-19) pandemic is caused by an infectious novel strain of coronavirus known as severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) which was earlier referred to as 2019-nCoV. The respiratory disease is the most consequential global public health crisis of the 21st century whose level of negative impact increasingly experienced globally has not been recorded since World War II. Up till now, there has been no specific globally authorized antiviral drug, vaccines, supplement or herbal remedy available for the treatment of this lethal disease except preventive measures, supportive care and non-specific treatment options adopted in different countries via divergent approaches to halt the pandemic. Read More

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Discovery of genes involved in anthocyanin biosynthesis from the rind and pith of three sugarcane varieties using integrated metabolic profiling and RNA-seq analysis.

BMC Plant Biol 2021 May 12;21(1):214. Epub 2021 May 12.

Institute of Medicinal Plant Development, Chinese Academy of Medical Sciences, Peking Union Medical College, 100193, Beijing, P. R. China.

Background: Sugarcane (Saccharum officinarum) is one of the most valuable feedstocks for sugar production. In addition to the production of industrial raw materials such as alcohol, papermaking, the fiber of livestock feed, respectively, sugarcane can produce bioactive compounds such as anthocyanins. Elucidation of the anthocyanin biosynthesis pathway is critical for the molecular breeding of sugarcane varieties with favorable traits. Read More

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Design, synthesis and anti-HIV evaluation of novel 5-substituted diarylpyrimidine derivatives as potent HIV-1 NNRTIs.

Bioorg Med Chem 2021 May 5;40:116195. Epub 2021 May 5.

Department of Medicinal Chemistry, Key Laboratory of Chemical Biology, Ministry of Education, School of Pharmaceutical Sciences, Cheeloo College of Medicine, Shandong University, Ji'nan 250012, China; China-Belgium Collaborative Research Center for Innovative Antiviral Drugs of Shandong Province, 44 West Culture Road, 250012 Jinan, Shandong, PR China. Electronic address:

Non-nucleoside reverse transcriptase inhibitors (NNRTIs) are widely used in combination therapies against HIV-1. As a continuation of our efforts to discover and develop "me-better" drugs of DAPYs, novel diarylpyrimidine derivatives were designed, synthesized and evaluated for their anti-HIV activities in MT-4 cells. All the compounds demonstrated strong inhibition activity against wide-type HIV-1 strain (III) with EC values in the range of 2. Read More

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Mechanism-Guided Development of Transition-Metal-Catalyzed C-N Bond-Forming Reactions Using Dioxazolones as the Versatile Amidating Source.

Acc Chem Res 2021 May 12. Epub 2021 May 12.

Center for Catalytic Hydrocarbon Functionalizations, Institute for Basic Science (IBS), Daejeon 34141, Korea.

ConspectusCatalytic reactions that construct carbon-nitrogen bonds are one of central themes in both synthetic and medicinal chemistry since the obtainable nitrogen-containing motifs are commonly encountered in natural products and have also seen a growing prominence as key structural features in marketed drugs and preclinical candidates. Pd-catalyzed cross-couplings, such as Buchwald-Hartwig amination, are at the forefront of such synthetic methods in practical settings. However, they require prefunctionalized substrates such as (hetero)aryl halides that must be prepared independently, often by multiple operations. Read More

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Structural recognition of the MYC promoter G-quadruplex by a quinoline derivative: insights into molecular targeting of parallel G-quadruplexes.

Nucleic Acids Res 2021 May 12. Epub 2021 May 12.

Purdue University, College of Pharmacy, Medicinal Chemistry and Molecular Pharmacology, 575 W Stadium Ave., West Lafayette, IN 47907, USA.

DNA G-Quadruplexes (G4s) formed in oncogene promoters regulate transcription. The oncogene MYC promoter G4 (MycG4) is the most prevalent G4 in human cancers. However, the most studied MycG4 sequence bears a mutated 3'-residue crucial for ligand recognition. Read More

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S-SIL of PCSK9-Active Oligonucleotide as Tools for Accurate Quantification by Mass Spectrometry.

Nucleic Acid Ther 2021 May 11. Epub 2021 May 11.

Oligonucleotide Discovery, Discovery Sciences, BioPharmaceuticals R&D, AstraZeneca, Gothenburg, Sweden.

Stable isotope labeling (SIL) of active pharmaceutical ingredients (API) is a well-established technique for the accurate quantification of small-molecule drugs. As the scope of active ingredients is expanding into areas of larger molecules, such as oligonucleotides (ONs), the development of new quantification techniques is critical. Herein, we describe the analysis of a S-SIL anti-PCSK9 gapmer-type antisense ON. Read More

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Potential beneficial effects of kefir and its postbiotic, kefiran, on child food allergy.

Food Funct 2021 May;12(9):3770-3786

Laboratory of Pharmaceutical and Medicinal Chemistry (PharMedChem), Federal University of Amapá, Macapá, Brazil.

Food allergies are known as the public health problem, affecting people of all age groups, but more commonly in babies and children, with consequences for nutritional status and quality of life. The increase in the consumption of healthy foods has consequently led to an increased demand for functional foods with specific health benefits. Thus, the pharmaceutical industry's interest in natural products has grown every time and is therefore considered as an alternative to synthetic drugs. Read More

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Utilizing Xenogeneic Cells As a Therapeutic Agent for Treating Diseases.

Cell Transplant 2021 Jan-Dec;30:9636897211011995

Sex Hormone Research Center, Department of Medical Laboratory Science and Biotechnology, China Medical University and Hospital, Taichung, Taiwan.

The utilization of biologically produced cells to treat diseases is a revolutionary invention in modern medicine after chemically synthesized small molecule drugs and biochemically made protein drugs. Cells are basic units of life with diverse functions in mature and developing organs, which biological properties could be utilized as a promising therapeutic approach for currently intractable and incurable diseases. Xenogeneic cell therapy utilizing animal cells other than human for medicinal purpose has been studied as a new way of treating diseases. Read More

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Integrated gut microbiota and fecal metabolomics reveal the renoprotective effect of Rehmanniae Radix Preparata and Corni Fructus on adenine-induced CKD rats.

J Chromatogr B Analyt Technol Biomed Life Sci 2021 Apr 24;1174:122728. Epub 2021 Apr 24.

Jiangsu Collaborative Innovation Center of Chinese Medicinal Resources Industrialization, Nanjing University of Chinese Medicine, 138 Xianlin Road, Nanjing 210023, PR China. Electronic address:

Rehmanniae Radix Preparata (RR) and Corni Fructus (CF), well-known traditional Chinese medicines (TCMs), were generally used together in the clinical practices to treat chronic kidney disease (CKD) with synergistic effects for thousands of years, but their combination mechanism remains largely unknown so far. Recent evidences have implicated intestinal flora as potential targets for the therapy of CKD. In this study, the CKD rat model was induced by adenine. Read More

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An overview on the role of plant-derived tannins for the treatment of lung cancer.

Phytochemistry 2021 May 8;188:112799. Epub 2021 May 8.

Department of Biochemistry, ICMR-National Institute for Research in Environmental Health, Bhopal, Madhya Pradesh, India. Electronic address:

Lung cancer is the leading cause of cancer-related death globally. Despite many advanced approaches to treat cancer, they are often ineffective due to resistance to classical anti-cancer drugs and distant metastases. Currently, alternative medicinal agents derived from plants are the major interest due to high bioavailability and fewer adverse effects. Read More

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The selective 5-HT receptor biased agonists, F15599 and F13714, show antidepressant-like properties after a single administration in the mouse model of unpredictable chronic mild stress.

Psychopharmacology (Berl) 2021 May 10. Epub 2021 May 10.

Department of Pharmacodynamics, Faculty of Pharmacy, Jagiellonian University Medical College, Krakow, Poland.

Rationale: The prevalence of depression is ever-increasing throughout the population. However, available treatments are ineffective in around one-third of patients and there is a need for more effective and safer drugs.

Objectives: The antidepressant-like and procognitive effects of the "biased agonists" F15599 (also known as NLX-101) which preferentially targets postsynaptic 5-HT receptors and F13714, which targets 5-HT autoreceptors, were investigated in mice. Read More

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From Precision Metapharmacology to Patient Empowerment: Delivery of Self-Care Practices for Epilepsy, Pain, Depression and Cancer Using Digital Health Technologies.

Front Pharmacol 2021 23;12:612602. Epub 2021 Apr 23.

Department of Pharmacotherapy, Skaggs Pharmacy Institute, University of Utah, Salt Lake City, UT, United States.

To improve long-term outcomes of therapies for chronic diseases, health promotion and lifestyle modifications are the most promising and sustainable strategies. In addition, advances in digital technologies provide new opportunities to address limitations of drug-based treatments, such as medication non-adherence, adverse effects, toxicity, drug resistance, drug shortages, affordability, and accessibility. Pharmaceutical drugs and biologics can be combined with digital health technologies, including mobile medical apps (digital therapeutics), which offer additional clinical benefits and cost-effectiveness. Read More

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Characterization of pharmaco-EEG fingerprint and sleep-wake profiles of Lavandula angustifolia Mill. essential oil inhalation and diazepam administration in rats.

J Ethnopharmacol 2021 May 7:114193. Epub 2021 May 7.

Division of Biological Science, Faculty of Science, Prince of Songkla University, Hat Yai, Songkhla 90110, Thailand; Biosignal Research Center for Health, Faculty of Science, Prince of Songkla University, Hat Yai, Songkhla, 90110, Thailand. Electronic address:

Ethnopharmacological Relevance: Lavandula angustifolia Mill. essential oil (Lavender EO) has a long history of medicinal use and is particularly claimed to possess anxiolytic and sedative properties. Lavender EO aromatherapy has been used to reduce distress and improve insomnia naturally. Read More

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Design, synthesis, structural and molecular characterization, toxicity, psychotropic activity and molecular docking evaluation of a novel phenytoin derivative: 3-decyl-5,5-diphenylimidazolidine-2,4-dione.

J Biomol Struct Dyn 2021 May 10:1-18. Epub 2021 May 10.

Laboratory of Medicinal Chemistry, Drug Sciences Research Center, Faculty of Medicine and Pharmacy, Mohammed V University in Rabat, Rabat, Morocco.

The hydantoin scaffold is of substantial importance and it is commonly used in drug discovery. Herein, we report the synthesis of a novel phenytoine (a hydantoin derivative) with high yield by the reaction of phenytoin with 1-bromodecyl agent. Namely, 3-decyl-5,5- diphenylimidazolidine-2,4-dione (3DDID). Read More

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Fabrication of versatile targeted lipopolymersomes for improved camptothecin efficacy against colon adenocarcinoma and .

Expert Opin Drug Deliv 2021 May 10. Epub 2021 May 10.

Pharmaceutical Research Center, Pharmaceutical Technology Institute, Mashhad University of Medical Sciences, Mashhad, Iran.

: Hybrid vesicular systems (lipopolymersomes) are promising platforms for minimizing the liposomes and polymersomes disadvantages in terms of chemotherapeutic transportation. In this regard, lipopolymersome has been designed to integrate the advantage of both polymersomes and liposomes to enable better structural integrity of the bilayer after encapsulation of hydrophobic drugs while maintaining the soft nature of liposomes, superior serum stability, and high encapsulation efficiency of cargos in the bilayer segment.: In the present study, we reported preparation and characterization of five camptothecin (CPT)-loaded lipopolymersomal formulations composed of poly (ethylene glycol)-poly (lactic acid) (PEG-PLA) and dipalmitoylphosphatidylcholine (DPPC) at different molar ratios using film rehydration method. Read More

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Kinase Inhibitors as Underexplored Antiviral Agents.

J Med Chem 2021 May 10. Epub 2021 May 10.

Centro de Investigaciones Biológicas Margarita Salas (CSIC), Ramiro de Maeztu 9, 28040 Madrid, Spain.

Viral infections are a major health problem; therefore, there is an urgent need for novel therapeutic strategies. Antivirals used to target proteins encoded by the viral genome usually enhance drug resistance generated by the virus. A potential solution may be drugs acting at host-based targets since viruses are dependent on numerous cellular proteins and phosphorylation events that are crucial during their life cycle. Read More

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Safe Polycationic Dendrimers as Potent Oral In Vivo Inhibitors of : A New Therapy to Take Down Tuberculosis.

Biomacromolecules 2021 May 10. Epub 2021 May 10.

Laboratoire de Chimie de Coordination du CNRS, 205 Route de Narbonne, BP 44099, 31077 Toulouse Cedex 4, France.

The long-term treatment of tuberculosis (TB) sometimes leads to nonadherence to treatment, resulting in multidrug-resistant (MDR) and extensively drug-resistant (XDR) tuberculosis. Inadequate bioavailability of the drug is the main factor for therapeutic failure, which leads to the development of drug-resistant cases. Therefore, there is an urgent need to design and develop novel antimycobacterial agents minimizing the period of treatment and reducing the propagation of resistance at the same time. Read More

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SUMOylation Wrestles With the Occurrence and Development of Breast Cancer.

Front Oncol 2021 21;11:659661. Epub 2021 Apr 21.

Key Laboratory of the Ministry of Education for Medicinal Resources and Natural Pharmaceutical Chemistry, National Engineering Laboratory for Resource Developing of Endangered Chinese Crude Drugs in Northwest of China, College of Life Sciences, Shaanxi Normal University, Xi'an, China.

Breast cancer has the highest incidence among cancers and is the most frequent cause of death in women worldwide. The detailed mechanism of the pathogenesis of breast cancer has not been fully elucidated, and there remains a lack of effective treatment methods for the disease. SUMOylation covalently conjugates a large amount of cellular proteins, and affects their cellular localization and biological activity to participate in numerous cellular processes. Read More

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Hypnotic Effect of . Hydroalcoholic Extract in Pentobarbital-Treated Mice.

Neurol Res Int 2021 21;2021:5521019. Epub 2021 Apr 21.

Neuroscience Research Center, Mashhad University of Medical Sciences, Mashhad, Iran.

Background: Current drugs used in the management of insomnia are associated with side effects. The use of medicinal herbs for insomnia treatment has recently been suggested.

Objective: The present study aimed to determine the hypnotic activity of the hydroalcoholic extract of . Read More

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Therapeutic Potential of Bioactive Compounds in Honey for Treating Osteoarthritis.

Front Pharmacol 2021 21;12:642836. Epub 2021 Apr 21.

Facultad de Ciencias de La Salud, Universidad Anáhuac México Sur, Ciudad de México, Mexico.

Dysregulation of joint tissue homeostasis induces articular degenerative changes and musculoskeletal diseases such as osteoarthritis. This pathology represents the first cause of motor disability in individuals over 60 years of age, impacting their quality of life and the costs of health systems. Nowadays, pharmacological treatments for cartilage disease have failed to achieve full tissue regeneration, resulting in a functional loss of the joint; therefore, joint arthroplasty is the gold standard procedure to cure this pathology in severe cases of Osteoarthritis. Read More

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The burden of cannabis-attributed pediatric and adult emergency department visits.

Acad Emerg Med 2021 May 9. Epub 2021 May 9.

Oregon Health and Science University, Department of Emergency Medicine, Center for Policy and Research in Emergency Medicine, Portland, Oregon, United States.

States that have legalized cannabis for medicinal or retail use have noted increases in emergency department (ED) visits associated with cannabis-associated harms. However, most studies are retrospective and identify cannabis-related visits using diagnosis codes or THC-positive urine drug immunoassays. These identification methods are limited. Read More

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Potential new targets and drugs related to histone modifications in glioma treatment.

Bioorg Chem 2021 Apr 24;112:104942. Epub 2021 Apr 24.

Graduate School, Shandong First Medical University & Shandong Academy of Medical Sciences, Taian, Shandong, China; Department of Neurology, Linyi People's Hospital, Shandong University, Linyi, Shandong, China; Central Laboratory, Linyi People's Hospital, Shandong University, Linyi, Shandong, China; Key Laboratory of Neurophysiology, Key Laboratory of Tumor Biology, Linyi, Shandong, China. Electronic address:

Glioma accounts for 40-50% of craniocerebral tumors, whose outcome rarely improves after standard treatment. The development of new therapeutic targets for glioma treatment has important clinical significance. With the deepening of research on gliomas, recent researchers have found that the occurrence and development of gliomas is closely associated with histone modifications, including methylation, acetylation, phosphorylation, and ubiquitination. Read More

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