220,974 results match your criteria pharmacological activities


Synthesis and pharmacological evaluation of choroquine derivatives bearing long aminated side chains as antivirus and anti-inflammatory agents.

Bioorg Chem 2021 Sep 11;116:105346. Epub 2021 Sep 11.

School of Chinese Materia Medica, Nanjing University of Chinese Medicine, Nanjing 210023 China; State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica (SIMM), Chinese Academy of Sciences, Shanghai 201203, China; Pharm-X Center, School of Pharmaceutical Sciences, Shanghai Jiao Tong University, Shanghai 200240, China; University of Chinese Academy of Sciences, Beijing 100049, China; School of Life Science and Technology, ShanghaiTech University, Shanghai 201210, China. Electronic address:

Starting from the antimalarial drugs chloroquine and hydroxychloroquine, we conducted a structural optimization on the side chain of chloroquine by introducing amino substituted longer chains thus leading to a series of novel aminochloroquine derivatives. Anti-infectious effects against SARS-Cov2 spike glycoprotein as well as immunosuppressive and anti-inflammatory activities of the new compounds were evaluated. Distinguished immunosuppressive activities on the responses of T cell, B cell and macrophages upon mitogen and pathogenic signaling were manifested. Read More

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September 2021

Progress in structure, synthesis and biological activity of natural cephalotane diterpenoids.

Phytochemistry 2021 Sep 15;192:112939. Epub 2021 Sep 15.

Key Laboratory of Structure-Based Drug Design & Discovery, Ministry of Education, and School of Traditional Chinese Materia Medica, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenyang, 110016, PR China. Electronic address:

The Cephalotaxus genus is well-known owing to the numerous complex, biologically relevant natural products that can be obtained from its constituent species. The successful identification of various Cephalotaxus alkaloids and natural, structurally diverse cephalotane diterpenoids that exhibit antitumor activities and excellent pharmacological properties has encouraged the discovery of previously undescribed compounds from this genus. The present review summarizes the different strategies for the total synthesis of cephalotane diterpenoids as well as their diverse chemical structures, antitumor activities, structure-activity relationships (SARs), and biosynthetic pathways. Read More

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September 2021

Rimonabant ameliorates hepatic ischemia/reperfusion injury in rats: Involvement of autophagy via modulating ERK- and PI3K/AKT-mTOR pathways.

Int Immunopharmacol 2021 Sep 15;100:108140. Epub 2021 Sep 15.

Department of Pharmacology and Toxicology, Faculty of Pharmacy, Zagazig University, Egypt.

Hepatic ischemia/reperfusion (HIR), which can result in severe liver injury and dysfunction, is usually associated with autophagy and endocannabinoid system derangements. Whether or not the modulation of the autophagic response following HIR injury is involved in the hepatoprotective effect of the cannabinoid receptor 1(CB1R) antagonist rimonabant remains elusive and is the aim of the current study. Rats pre-treated with rimonabant (3 mg/kg) or vehicle underwent 30 min hepatic ischemia followed by 6 hrs. Read More

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September 2021

Plant isoquinoline alkaloids: Advances in the chemistry and biology of berberine.

Eur J Med Chem 2021 Sep 9;226:113839. Epub 2021 Sep 9.

Phytochemistry Division, CSIR-Central Institute of Medicinal and Aromatics Plants (CSIR-CIMAP) P.O. CIMAP, Lucknow, 226015, India; Academy of Scientific and Innovative Research (AcSIR), Ghaziabad, 201002, India. Electronic address:

Alkaloids are one of the most important classes of plant bioactives. Among these isoquinoline alkaloids possess varied structures and exhibit numerous biological activities. Basically these are biosynthetically produced via phenylpropanoid pathway. Read More

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September 2021

Compound Tongluo Decoction inhibits endoplasmic reticulum stress-induced ferroptosis and promoted angiogenesis by activating the Sonic Hedgehog pathway in cerebral infarction.

J Ethnopharmacol 2021 Sep 15:114634. Epub 2021 Sep 15.

Department of Neurology, Nanjing Hospital of Chinese Medicine Affiliated to Nanjing University of Chinese Medicine, Nanjing, 210001, Jiangsu province, PR China. Electronic address:

Ethnopharmacological Relevance: Cerebral infarction is one of the most common types of cerebrovascular diseases that threaten people's health. Compound Tongluo Decoction (CTLD), a traditional Chinese medicine formula, has various pharmacological activities, including the alleviation of cerebral infarction symptoms.

Aim Of The Study: This study aims to explore the potential mechanism by which CTLD alleviates cerebral infarction. Read More

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September 2021

Neuroprotective effects of curcumin-loaded nanophytosome on ketamine-induced schizophrenia-like behaviors and oxidative damage in male mice.

Neurosci Lett 2021 Sep 15:136249. Epub 2021 Sep 15.

Faculty of Herbs, Amol University of Special Modern Technologies, Amol, Iran.

Curcumin as an antioxidant natural herb has shown numerous pharmacological effects. However, the poor bioavailability of curcumin is a significant pharmacological barrier for its antioxidant activities. The present study was conducted to develop curcumin-loaded nanophytosome (CNP) and explore their therapeutic potential in a ketamine (KET)-induced schizophrenia (SCZ) model. Read More

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September 2021

Photocrosslinkable gelatin/collagen based bioinspired polyurethane-acrylate bone adhesives with tunable elasticity and biodegradability.

Int J Biol Macromol 2021 Sep 15. Epub 2021 Sep 15.

İnönü University, Science Faculty, Department of Chemistry, Malatya, Turkey. Electronic address:

Hard or soft tissue adhesives have been presented as a promising candidate to replace traditional wound closure methods. A series of hard tissue bioadhesive formulations based on natural polymers have recently been designed and investigated in our laboratory. In current work, we produced an UV-curable polyurethane-acrylate formulations as a bioadhesive. Read More

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September 2021

Visual art therapy and cognition: Effects on people with mild cognitive impairment and low education level.

J Gerontol B Psychol Sci Soc Sci 2021 Sep 18. Epub 2021 Sep 18.

Department of Psychiatry, School of Medicine and Dentistry, University of Dodoma, Tanzania.

Objectives: The aim of this study was to examine the effects of visual art therapy (VAT) on cognition, psychological and functional ability of people with mild cognitive impairment (MCI) and low education.

Method: A single-blinded randomized controlled trial was conducted among 127 older adults with MCI, mean age 73.6 years and level of education in years, (median (range)) = 0 (0 - 9). Read More

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September 2021

Therapeutic potential of Scutellaria baicalensis Georgi in lung cancer therapy.

Phytomedicine 2021 Sep 4:153727. Epub 2021 Sep 4.

Innovative Institute of Chinese Medicine and Pharmacy, Chengdu University of Traditional Chinese Medicine, Chengdu, 611137, China. Electronic address:

Background: Globally, lung cancer is the leading cause of cancer associated mortalities. The current conventional chemotherapy remains the preferred treatment option for lung cancer, as surgical resection plays little role in the treatment of over 75% of lung cancer patients. Therefore, there is a need to develop novel potential therapeutic drugs or adjuvants with a high efficiency and safety against lung cancer. Read More

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September 2021

Cancer and diabetes: the interlinking metabolic pathways and repurposing actions of antidiabetic drugs.

Cancer Cell Int 2021 Sep 17;21(1):499. Epub 2021 Sep 17.

Phytochemistry Research Center, Shahid Beheshti University of Medical Sciences, Tehran, Iran.

Cancers are regarded as one of the main causes of death and result in high health burden worldwide. The management of cancer include chemotherapy, surgery and radiotherapy. The chemotherapy, which involves the use of chemical agents with cytotoxic actions is utilised as a single treatment or combined treatment. Read More

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September 2021

Expanding the toolbox of exosome-based modulators of cell functions.

Biomaterials 2021 Sep 12;277:121129. Epub 2021 Sep 12.

Department of Pharmacology and Pharmaceutical Sciences, School of Pharmacy, University of Southern California, Los Angeles, CA, 90089, USA; Department of Chemistry, Dornsife College of Letters, Arts and Sciences, University of Southern California, Los Angeles, CA, 90089, USA; Norris Comprehensive Cancer Center, University of Southern California, Los Angeles, CA, 90089, USA; Research Center for Liver Diseases, University of Southern California, Los Angeles, CA, 90089, USA. Electronic address:

Exosomes are cell-derived extracellular vesicles and play important roles in mediating intercellular communications. Due to their unique advantages in transporting a variety of biomolecules, exosomes have been emerging as a new class of nanocarriers with great potential for therapeutic applications. Despite advancements in loading chemotherapeutics and interfering RNAs into exosomes, active incorporation of protein molecules into exosomes remains challenging owing to their distinctive physicochemical properties and/or a lack of knowledge of cargo sorting during exosome biogenesis. Read More

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September 2021

Biological and pharmacological activities of noscapine: Focusing on its receptors and mechanisms.

Biofactors 2021 Sep 17. Epub 2021 Sep 17.

Applied Biomedical Research Center, Mashhad University of Medical Sciences, Mashhad, Iran.

Noscapine has been mentioned as one of the effective drugs with potential therapeutic applications. With few side effects and amazing capabilities, noscapine can be considered different from other opioids-like structure compounds. Since 1930, extensive studies have been conducted in the field of pharmacological treatments from against malaria to control cough and cancer treatment. Read More

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September 2021

Verification of Thai ethnobotanical medicine "Kamlang Suea Khrong" driven by multiplex PCR and powerful TLC techniques.

PLoS One 2021 17;16(9):e0257243. Epub 2021 Sep 17.

Department of Pharmaceutical Sciences, Faculty of Pharmacy, Chiang Mai University, Mueang, Chiang Mai, Thailand.

Kamlang Suea Khrong (KSK) crude drug, a traditional Thai medicine used for oral tonic and analgesic purposes, is obtained from three origins: the inner stem bark of Betula alnoides (BA) or the stems of Strychnos axillaris (SA) or Ziziphus attopensis (ZA). According to the previous reports, SA contains strychnine-type alkaloids that probably cause poisoning; however, only organoleptic approaches are insufficient to differentiate SA from the other plant materials. To ensure the botanical origin of KSK crude drug, powerful and reliable tools are desperately needed. Read More

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September 2021

Spirulina platensis protects against microcystin-LR-induced toxicity in rats.

Environ Sci Pollut Res Int 2021 Sep 17. Epub 2021 Sep 17.

Department of Pharmaceutical Sciences, Pharmacy Program, Batterjee Medical College, P.O. Box 6231, Jeddah, 21442, Saudi Arabia.

Microcystis aeruginosa produces an abundant cyanotoxin (microcystins (MCs) in freshwater supplies. MCs have adverse health hazards to animals and humans. Microcystin-leucine-arginine (microcystin-LR or MC-LR) is the most studied among these MCs due to their high toxicity. Read More

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September 2021

Effects of Controlled Generator Fume Emissions on the Levels of Troponin I, C-Reactive Protein and Oxidative Stress Markers in Dogs: Exploring Air Pollution-Induced Cardiovascular Disease in a Low-Resource Country.

Cardiovasc Toxicol 2021 Sep 17. Epub 2021 Sep 17.

Department of Veterinary Medicine, Faculty of Veterinary Medicine, University of Nigeria, Nsukka, Enugu, Nigeria.

Exhaust fumes from petrol/diesel-powered electric generators contribute significantly to air pollution in many developing countries, constituting health hazards to both humans and animals. This study evaluated the serum concentrations of Troponin I (TnI), C-reactive protein (CRP) and serum levels/activities of oxidative stress markers: catalase (CAT), reduced glutathione (GSH), malondialdehyde (MDA), nitric oxide (NO) and superoxide dismutase (SOD) in dogs experimentally exposed to graded levels of petrol generator exhaust fume (PGEF). Sixteen (16) healthy and adult male Basenji dogs were randomly assigned into four groups (A-D). Read More

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September 2021

Why use nutraceutical strategies for the Irritable Bowel Syndrome.

Curr Med Chem 2021 Sep 16. Epub 2021 Sep 16.

Dept Systems Medicine, Policlinico Tor Vergata (PTV) Foundation, Rome, Italy.

Irritable bowel syndrome (IBS) is a chronic functional bowel disorder, often stress-related, identified by many abdominal symptoms, the most important of which is the chronic visceral abdominal pain. Therefore, IBS commonly impairs the quality of life of patients, moreover it is frequently linked to depressive and anxiety symptoms. The treatment of IBS primarily focuses on symptoms relief. Read More

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September 2021

Insight into Recent Drug Discoveries against Trypanosomatids and Plasmodium spp Parasites: New Metal-based Compounds.

Curr Med Chem 2021 Sep 16. Epub 2021 Sep 16.

Sao Paulo State University (UNESP), School of Pharmaceutical Sciences, Araraquara, SP, 14800-903, Brazil.

Scaffolds of metal-based compounds can act as pharmacophore groups in several ligands to treat various diseases, including tropical infectious diseases (TID). In this review article, we investigate the contribution of these moieties to medicinal inorganic chemistry in the last seven years against TID, including American trypanosomiasis (Chagas disease), human African trypanosomiasis (HAT, sleeping sickness), leishmania, and malaria. The most potent metal-based complexes are displayed and highlighted in figures, tables and graphics; according to their pharmacological activities (IC50 > 10µM) against Trypanosomatids and Plasmodium spp parasites. Read More

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September 2021

CREB regulates the expression of Type 1 Inositol 1,4,5-trisphosphate receptors.

J Cell Sci 2021 Sep 17. Epub 2021 Sep 17.

Department of Pharmacology and Physiology, University of Rochester, Rochester, NY, 14642, USA.

Inositol 1,4,5-trisphosphate (IP3) receptors (IP3Rs) play a central role in regulating intracellular calcium signals in response to a variety of internal/external cues. Dysregulation of IP3R signaling is the underlying cause for numerous pathological conditions. It is well established that the activities of IP3Rs are governed by several post-translational modifications including phosphorylation by protein kinase A (PKA). Read More

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September 2021

Alcohol use disorder in the COVID-19 era: Position paper of the Italian Society on Alcohol (SIA).

Addict Biol 2021 Sep 16:e13090. Epub 2021 Sep 16.

Department of Translational Medicine, University of Ferrara, Ferrara, Italy.

Coronavirus disease 2019 (COVID-19) first emerged in China in November 2019. Most governments have responded to the COVID-19 pandemic by imposing a lockdown. Some evidence suggests that a period of isolation might have led to a spike in alcohol misuse, and in the case of patients with alcohol use disorder (AUD), social isolation can favour lapse and relapse. Read More

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September 2021

Effects of nitro-butoxyl- and butyl-esters of non-steroidal anti-inflammatory drugs compared with parent compounds on the contractility of digital arterial smooth muscle from the fallow deer (Dama dama).

Inflammopharmacology 2021 Sep 16. Epub 2021 Sep 16.

Biomedical Research Centre, Sheffield Hallam University, Howard Street, Sheffield, S1 1WB, UK.

Background: Non-steroidal anti-inflammatory drugs (NSAIDs) are a major cause of upper gastro-intestinal (GI) ulceration and bleeding as well as cardiovascular (CV) diseases (e.g., myocardial infarction and stroke). Read More

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September 2021

Preclinical evaluation of MRG002, a novel HER2-targeting antibody-drug conjugate with potent antitumor activity against HER2-positive solid tumors.

Antib Ther 2021 Jul 28;4(3):175-184. Epub 2021 Aug 28.

Research and Development, Shanghai Miracogen, Suite 4E, Bldg. 3, No. 1238 Zhangjiang Road, Pudong District, Shanghai 201203, China.

Background: ERBB2 is a proto-oncogene of multiple cancers including breast and gastric cancers with HER2 protein overexpression or gene amplification and has been proven clinically as a valid target for these cancers. HER2-targeting agents such as Herceptin®, Kadcyla® and ENHERTU® have been approved by the FDA for the treatment of breast cancer, but these drugs still face the challenge of acquired resistance and/or severe adverse reactions in clinical use. Therefore, there is significant unmet medical need for developing new agents that are more effective and safer for patients with advanced HER2-positive solid tumors including breast and gastric cancers. Read More

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Dihydroartemisinin attenuates benign prostatic hyperplasia in rats by inhibiting prostatic epithelial cell proliferation.

Ann Transl Med 2021 Aug;9(15):1246

Department of Urology, Xiangya Hospital, Central South University, Changsha, China.

Background: Benign prostatic hyperplasia (BPH) is a common urological condition in aging men. While dihydroartemisinin (DHA) exhibits a wide range of pharmacological activities, to date, there have been no studies examining the effects of DHA on BPH.

Methods: An BPH model was constructed in rats via daily subcutaneous injection of testosterone propionate (TP) for 28 consecutive days. Read More

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Natural Coumarins: Exploring the Pharmacological Complexity and Underlying Molecular Mechanisms.

Oxid Med Cell Longev 2021 23;2021:6492346. Epub 2021 Aug 23.

Department of Clinical Oncology, Queen Elizabeth Hospital, Kowloon, Hong Kong.

Coumarins belong to the benzopyrone family commonly found in many medicinal plants. Natural coumarins demonstrated a wide spectrum of pharmacological activities, including anti-inflammatory, anticoagulant, anticancer, antibacterial, antimalarial, casein kinase-2 (CK2) inhibitory, antifungal, antiviral, Alzheimer's disease inhibition, neuroprotective, anticonvulsant, phytoalexins, ulcerogenic, and antihypertensive. There are very few studies on the bioavailability of coumarins; therefore, further investigations are necessitated to study the bioavailability of different coumarins which already showed good biological activities in previous studies. Read More

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Pharmacological Properties of 2,4,6-Trihydroxy-3-Geranyl Acetophenone and the Underlying Signaling Pathways: Progress and Prospects.

Front Pharmacol 2021 31;12:736339. Epub 2021 Aug 31.

Department of Biomedical Sciences, Faculty of Medicine and Health Sciences, Universiti Putra Malaysia, Serdang, Malaysia.

2,4,6-Trihydroxy-3-geranyl acetophenone (tHGA) is a bioactive phloroglucinol compound found in (Champ. ex Benth.) T. Read More

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Safety Assessment of Maxim. Water Extract: General Toxicity Studies in Sprague-Dawley Rats and Beagle Dogs With Re-evaluation of Genotoxic Potentials.

Front Pharmacol 2021 31;12:687261. Epub 2021 Aug 31.

Department of Experimental Animal Research, Biomedical Research Institute, Seoul National University Hospital, Seoul, South Korea.

Maxim., commonly known as Manchurian stripe maple, is a deciduous tree belonging to the family of Aceraceae and has been traditionally used in folk medicine for its remedial effects in liver diseases and traumatic bleedings. With a growing body of experimental evidence for its pharmacological efficacies, such as neuroprotective, hepatoprotective, antioxidant, and anti-inflammatory activities, has gradually gained popularity as a health supplement and functional food. Read More

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Towards a better understanding of Fagopyrum dibotrys: a systematic review.

Chin Med 2021 Sep 16;16(1):89. Epub 2021 Sep 16.

Key Laboratory of Coarse Cereal Processing of Ministry of Agriculture and Rural Affairs, Chengdu University, Chengdu, China.

Fagopyrum dibotrys (F. dibotrys) (D.Don) H. Read More

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September 2021

Insight into the Isolation, Synthesis and Structure-Activity Relationship of Piperine Derivatives for the Development of New Compounds: Recent Updates.

Curr Top Med Chem 2021 Sep 16. Epub 2021 Sep 16.

Department of Pharmaceutical Chemistry, Maharishi Arvind College of Pharmacy, Ambabari Circle, Jaipur, Rajasthan- 302039. India.

Currently, black pepper commands the leading position among all the spices as a spice of handsome commercial importance in all the world trade and finds its way into the dietary habits of millions of people worldwide. Black pepper is biologically known as Piper nigrum and contains Piperine as the main active chemical constituent. This paper highlights various general methods for extracting Piperine from the crude drug: maceration extraction, Hydrotropic extraction, Accelerated solvent extraction, Thin layer chromatography, and extraction with ethanol & dichloromethane Ionic fluid-based ultrasonic-assisted extraction, etc. Read More

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September 2021

Nanomaterials for fluorescent detection of curcumin.

Spectrochim Acta A Mol Biomol Spectrosc 2021 Sep 4;265:120359. Epub 2021 Sep 4.

School of Chemistry and Materials Science, Nanjing University of Information Science & Technology, Nanjing 210044, China.

Owing to the attractive biological and pharmacological activities, sensitive and selective detection of curcumin is of great significance. Nanomaterials possessing unique optical properties exhibit potential applications in the fluorescent detection of curcumin. This review first discussed the detection strategies of fluorescent nanosensors. Read More

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September 2021

Phytochemistry and pharmacology of Wild.: a nootropic drug.

Authors:
Mohd Aleem

J Complement Integr Med 2021 Sep 15. Epub 2021 Sep 15.

Department of Ilmul Advia (Pharmacology), National Institute of Unani Medicine, Bengaluru, Karnataka, India.

Objectives: Wild is an evergreen climbing shrub. The plant is of great significance in the traditional Indian System of Medicine, such as Ayurveda, Unani, and Siddha. The seeds and their oil are extensively used to treat neurological disorders such as cognitive dysfunction, paralysis, epilepsy, insomnia, and other ailments like rheumatism, arthritis, sciatica, and leprosy. Read More

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September 2021

Perception, magnitude, and implications of cancer-related fatigue in breast cancer survivors: Study from a developing country.

J Cancer Res Ther 2021 Jul-Sep;17(4):998-1002

Department of Surgical Oncology, Max Institute of Cancer Care, Max Super Specialty Hospital, New Delhi, India.

Background: We have analyzed perceptions, magnitude, interventions adopted, and overall implications of cancer-related fatigue (CRF) in breast cancer survivors (BCSs).

Methodology: BCSs who attended follow-up clinic at our institute between January and June 2018 were asked to fill a questionnaire focused on assessing an individual's perception, severity, potential causes, implications on quality of life, and measures taken to deal with CRF.

Results: Sixty-five patients were included. Read More

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September 2021