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https://www.readbyqxmd.com/read/29461053/research-progress-of-polycyclic-polyprenylated-acylphloroglucinols
#1
Xing-Wei Yang, Robert B Grossman, Gang Xu
Polycyclic polyprenylated acylphloroglucinols (PPAPs) are a class of hybrid natural products sharing the mevalonate/methylerythritol phosphate and polyketide biosynthetic pathways and showing considerable structure and bioactivity diversity. This review discusses the progress of research into the chemistry and biological activity of 421 natural PPAPs in the past 11 years as well as in-depth studies of biological activities and total synthesis of some PPAPs isolated before 2006. We created an online database of all PPAPs known to date at http://www...
February 20, 2018: Chemical Reviews
https://www.readbyqxmd.com/read/29442047/comprehensive-phytochemical-characterization-of-st-john-s-wort-hypericum-perforatum-l-oil-macerates-obtained-by-different-extraction-protocols-via-analytical-tools-applicable-in-routine-control
#2
M Heinrich, R Daniels, F C Stintzing, D R Kammerer
The aim of the present study was to investigate the impact of crucial process parameters, i.e. of light and temperature conditions, during the preparation of St. John's wort (SJW, Hypericum perforatum L.) Arachis oil macerates. Extracts were prepared according to a standardized protocol over a period of 28 days. For this purpose, flowering tops of H. perforatum were macerated with Arachis oil (drug extract ratio, DERnative 1:4) under different light and temperature conditions. Spectrophotometric measurements were carried out to quantitate naphthodianthrones and to characterize extract color in the CIE L*C*h° system...
March 1, 2017: Die Pharmazie
https://www.readbyqxmd.com/read/29440179/role-of-c-jun-n-terminal-kinase-in-pregnane-x-receptor-mediated-induction-of-human-cytochrome-p4503a4-in-vitro
#3
Guncha Taneja, Chun Chu, Paramahamsa Maturu, Bhagavatula Moorthy, Romi Ghose
Cytochrome P450 (CYP) 3A4 is the most abundant drug metabolizing enzyme and is responsible for the metabolism of ~50% of clinically available drugs. Induction of CYP3A4 impacts the disposition of its substrates and leads to harmful clinical consequences such as failure of therapy. In order to prevent such undesirable consequences, molecular mechanisms of regulation of CYP3A4 need to be fully understood. CYP3A4 induction is primarily regulated by the xenobiotic nuclear receptor, pregnane-X-receptor (PXR). After ligand binding, PXR is transported to the nucleus, where it binds to the CYP3A4 promoter and induces its gene expression...
February 12, 2018: Drug Metabolism and Disposition: the Biological Fate of Chemicals
https://www.readbyqxmd.com/read/29411879/understanding-drug-interactions-with-st-john-s-wort-hypericum-perforatum-l-impact-of-hyperforin-content
#4
REVIEW
Sigrun Chrubasik-Hausmann, Julia Vlachojannis, Andrew J McLachlan
OBJECTIVE: The aim of this study was to review herb-drug interaction studies with St John's wort (Hypericum perforatum L.) with a focus on the hyperforin content of the extracts used in these studies. METHODS: PUBMED was systematically searched to identify studies describing pharmacokinetic interactions involving St John's wort. Data on study design and the St John's wort extract or product were gathered to extract hyperforin content and daily dose used in interaction studies...
February 7, 2018: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/29382233/an-in-vivo-study-of-hypericum-perforatum-in-a-niosomal-topical-drug-delivery-system
#5
Mohamed Ali, Amira Abdel Motaal, Mohammed A Ahmed, Abdulrhman Alsayari, Omaima N El-Gazayerly
The active compounds present in Hypericum perforatum L. (Hypericaceae) include hyperforin, hypericins and flavonoids, which are assumed to be responsible for the activity of the extract in the treatment of wounds and scars. The present study aimed to incorporate H. perforatum extract standardized to a known content of phloroglucinols, naphthodianthrones and polyphenolic compounds into an effective transdermal drug delivery system capable of entrapping both lipophilic and hydrophilic constituents in the form of niosomal gels for wound treatment...
November 2018: Drug Delivery
https://www.readbyqxmd.com/read/29279803/wound-healing-potential-of-oil-of-hypercium-perforatum-in-excision-wounds-of-male-sprague-dawley-rats
#6
Shivananada B Nayak, Kubra Isik, Julien R Marshall
Objective: To evaluate the wound-healing activity of oil of Hypercium perforatum (St. John's wort), in excision wounds of male white rats. Approach: The current methods of wound management involve the use of antibiotic creams. The search for more natural materials for the purpose of healing of wounds has led to the discoveries of potential agents prepared from plant extracts. Hyperforin and Hypericin are important phytochemical constituents found in H. perforatum, which have been highlighted for their antimicrobial, antiviral, and anti-inflammatory properties in recent times...
December 1, 2017: Advances in Wound Care
https://www.readbyqxmd.com/read/29191717/improved-in-vitro-models-for-preclinical-drug-and-formulation-screening-focusing-on-2d-and-3d-skin-and-cornea-constructs
#7
REVIEW
Nicole Beißner, Antonio Bolea Albero, Jendrik Füller, Thomas Kellner, Lothar Lauterboeck, Jinghu Liang, Markus Böl, Birgit Glasmacher, Christel C Müller-Goymann, Stephan Reichl
The present overview deals with current approaches for the improvement of in vitro models for preclinical drug and formulation screening which were elaborated in a joint project at the Center of Pharmaceutical Engineering of the TU Braunschweig. Within this project a special focus was laid on the enhancement of skin and cornea models. For this reason, first, a computation-based approach for in silico modeling of dermal cell proliferation and differentiation was developed. The simulation should for example enhance the understanding of the performed 2D in vitro tests on the antiproliferative effect of hyperforin...
November 27, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/29141922/trpc6-contributes-to-lps-induced-inflammation-through-erk1-2-and-p38-pathway-in-bronchial-epithelial-cells
#8
Li-Fen Zhou, Qing-Zi Chen, Chun-Tao Yang, Zhao-Di Fu, Shen-Ting Zhao, Yan Chen, Shu-Ni Li, Li Liao, Yu-Bo Zhou, Jian-Rong Huang, Jian-Hua Li
Transient receptor potential canonical (TRPC) channels are currently an emerging target for airway disorders. Recent evidences have indicated that TRPC6 as a member of the TRPC family plays an important role in airway inflammation, but its precise function in bronchial epithelial cells remains unclear. The aim of this study was to investigate the role of TRPC6 in TLR4-mediated inflammation in human bronchial epithelial cells stimulated by endotoxin (lipopolysaccharide, LPS). Hyp9 is a simplified phloroglucinol derivative of Hyperforin which highly selective activates TRPC6 channels...
November 15, 2017: American Journal of Physiology. Cell Physiology
https://www.readbyqxmd.com/read/28990659/persistence-of-stat-1-inhibition-and-induction-of-cytokine-resistance-in-pancreatic-%C3%AE-cells-treated-with-st-john-s-wort-and-its-component-hyperforin
#9
Michela Novelli, Pascale Beffy, Alex Gregorelli, Svetlana Porozov, Fabrizio Mascia, Chiara Vantaggiato, Pellegrino Masiello, Marta Menegazzi
OBJECTIVES: St John's wort extract (SJW) and its component hyperforin (HPF) were shown to potently inhibit cytokine-induced STAT-1 and NF-κB activation in pancreatic β cells and protect them against injury. This study aimed at exploring the time course of STAT-1 inhibition afforded by these natural compounds in the β-cell line INS-1E. METHODS: INS-1E cells were pre-incubated with SJW extract (2-5 μg/ml) or HPF (0.5-2 μm) and then exposed to a cytokine mixture...
October 9, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/28982580/stimulation-of-transient-receptor-potential-m3-trpm3-channels-increases-interleukin-8-gene-promoter-activity-involving-ap-1-and-extracellular-signal-regulated-protein-kinase
#10
Sandra Rubil, Andrea Lesch, Naofumi Mukaida, Gerald Thiel
Stimulation of Ca(2+) permeable TRPM3 (transient receptor potential melastatin-3) channels with the steroid ligand pregnenolone sulfate activates stimulus-responsive transcription factors, including the transcription factor AP-1 (activator protein-1). As part of a search for AP-1-regulated target genes we analyzed the gene encoding interleukin-8 (IL-8) in HEK293 cells expressing TRPM3 channels. Here, we show that stimulation of TRPM3 channels activated transcription of an IL-8 promoter-controlled reporter gene that was embedded into the chromatin of the cells...
October 2, 2017: Cytokine
https://www.readbyqxmd.com/read/28961505/hyperforin-attenuates-aluminum-induced-a%C3%AE-production-and-tau-phosphorylation-via-regulating-akt-gsk-3%C3%AE-signaling-pathway-in-pc12-cells
#11
Wanyue Huang, Ping Cheng, Kaiyuan Yu, Yanfei Han, Miao Song, Yanfei Li
Aluminum (Al) is a neurotoxicant and cause β-amyloid (Aβ) peptides aggregation and tau hyperphosphorylation. Hyperforin (HF) is one of the major active constituents of the extracts of St. John's Wort (Hypericum perforatum), can treat Alzheimer's disease (AD) and other diseases involving peptide accumulation and cognition impairment. To determine the effects of HF on Al-induced Aβ formation and tau hyperphosphorylation, PC12 cells were cultured and treated with Al-malt (500μM) and/or HF (1μM). The results showed that HF treatment significantly attenuated Al-malt-induced Aβ1-42 production by reducing the expressions of APP, BACE1 and PS1, while increasing the expressions of sAPPα, ADAM9/10/17, and tau phosphorylation in PC12 cells...
September 26, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28943862/the-chemical-and-antibacterial-evaluation-of-st-john-s-wort-oil-macerates-used-in-kosovar-traditional-medicine
#12
James T Lyles, Austin Kim, Kate Nelson, Angelle L Bullard-Roberts, Avni Hajdari, Behxhet Mustafa, Cassandra L Quave
Hypericum perforatum L. (Hypericaceae), or St. John's Wort, is a well-known medicinal herb often associated with the treatment of anxiety and depression. Additionally, an oil macerate (Oleum Hyperici) of its flowering aerial parts is widely used in traditional medicine across the Balkans as a topical wound and ulcer salve. Other studies have shown that Oleum Hyperici reduces both wound size and healing time. Of its active constituents, the naphthodianthrone hypericin and phloroglucinol hyperforin are effective antibacterial compounds against various Gram-positive bacteria...
2017: Frontiers in Microbiology
https://www.readbyqxmd.com/read/28885074/clinical-risks-of-st-john-s-wort-hypericum-perforatum-co-administration
#13
REVIEW
Samaneh Soleymani, Roodabeh Bahramsoltani, Roja Rahimi, Mohammad Abdollahi
St. John's wort (SJW) is a common medicinal herb used for the treatment of mild to moderate depression. Hyperforin, one of the chief components of SJW, plays an important role in the induction of cytochrome P450 enzymes (CYP) and P-glycoprotein transporter (P-gp), and therefore, affects the pharmacokinetics of various drugs. There are several clinical studies demonstrating the interaction of SJW with the metabolism of conventional drugs which may cause life-threatening events. Areas covered: This review focuses on human studies that have evaluated pharmacokinetic alterations of conventional drugs in concomitant use with different SJW preparations...
October 2017: Expert Opinion on Drug Metabolism & Toxicology
https://www.readbyqxmd.com/read/28870826/hyperforin-protects-against-acute-cerebral-ischemic-injury-through-inhibition-of-interleukin-17a-mediated-microglial-activation
#14
Li Ma, Xia Pan, Fang Zhou, Kang Liu, Long Wang
Hyperforin, a pharmacologically active component of the medicinal plant Hypericum perforatum (St. John's wort), has been shown to be neuroprotective against acute ischemic stroke. However, the underlying mechanisms are still unclear and need to be fully elucidated. C57BL/6 wildtype (WT) mice or interleukin (IL)-17A knock-out mice were subjected to middle cerebral artery occlusion (60 minutes) followed by reperfusion for 72 hours. Hyperforin (0.5 μg) was injected slowly into the right ventricle of WT mice 1, 24 and 48 hours after middle cerebral artery occlusion (MCAO) onset...
September 1, 2017: Brain Research
https://www.readbyqxmd.com/read/28870756/stabilization-of-hyperforin-dicyclohexylammonium-salt-with-dissolved-albumin-and-albumin-nanoparticles-for-studying-hyperforin-effects-on-2d-cultivation-of-keratinocytes-in-vitro
#15
J Füller, T Kellner, M Gaid, L Beerhues, C C Müller-Goymann
Due to the limited chemical stability of the natural hyperforin molecule, a more stable form of hyperforin, i.e., the hyperforin dicyclohexylammonium salt (HYP-DCHA) has been used for ex vivo and in vitro experiments in recent years, but its actual stability under typical cell culture conditions has never been studied before. In this contribution the stability of HYP-DCHA was examined under typical cell culture conditions. Different cell culture media with and without fetal calf serum (FCS) supplementation were studied with regard to further stabilization of HYP-DCHA determined with HPLC analysis...
September 1, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28722156/chemometric-evaluation-of-hypericin-and-related-phytochemicals-in-17-in-vitro-cultured-hypericum-species-hairy-root-cultures-and-hairy-root-derived-transgenic-plants
#16
Katarína Nigutová, Souvik Kusari, Selahaddin Sezgin, Linda Petijová, Jana Henzelyová, Miroslava Bálintová, Michael Spiteller, Eva Čellárová
OBJECTIVES: The objective of this study was to ascertain the presence and correlations among eight important secondary metabolites viz. hypericin, pseudohypericin, emodin, hyperforin, rutin, hyperoside, quercetin and quercitrin in different organs of 17 in vitro cultured Hypericum species, along with H. tomentosum and H. tetrapterum hairy root cultures, and hairy root-derived transgenic plants of H. tomentosum. METHODS: Samples were extracted and analysed by LC-MS...
July 19, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/28696436/reduced-trpc6-mrna-levels-in-the-blood-cells-of-patients-with-alzheimer-s-disease-and-mild-cognitive-impairment
#17
R Lu, J Wang, R Tao, J Wang, T Zhu, W Guo, Y Sun, H Li, Y Gao, W Zhang, C J Fowler, Q Li, S Chen, Z Wu, C L Masters, C Zhong, N Jing, Y Wang, Y Wang
Transient receptor potential canonical 6 (TRPC6) inhibits β-amyloid (Aβ) production. Hyperforin, the TRPC6 agonist, reduces Aβ levels and improves cognitive performance in Alzheimer's disease (AD) models. However, it's unknown whether TRPC6 expression is changed in AD patients. In this case-control study, we measured TRPC6 expression levels in the peripheral blood cells of four independent AD sets from five hospitals and one mild cognitive impairment (MCI) set from a local community (229 AD, 70 MCI, 40 Parkinson disease and 359 controls from China, total n=698) using quantitative real-time PCR assay...
July 11, 2017: Molecular Psychiatry
https://www.readbyqxmd.com/read/28669795/downstream-processing-of-hyperforin-from-hypericum-perforatum-root-cultures
#18
Paul Haas, Mariam Gaid, Ajmal Zarinwall, Ludger Beerhues, Stephan Scholl
Hyperforin is a major metabolite of the medicinal plant Hypericum perforatum (St. John's Wort) and has recently been found in hormone induced root cultures. The objective of this study is to identify a downstream process for the production of a hyperforin-rich extract with maximum extraction efficiency and minimal decomposition. The maximum extraction time was found to be 60min. The comparison of two equipment concepts for the extraction and solvent evaporation was performed employing two different solvents...
June 29, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28472287/optimized-and-validated-hplc-analysis-of-st-john-s-wort-extract-and-final-products-by-simultaneous-determination-of-major-ingredients
#19
Konstantina Zeliou, Nikos I Kontaxis, Evangelia Margianni, Christos Petrou, Fotini N Lamari
Aim of this work was to develop a validated high performance liquid chromatography method for the analysis of extracts and final products of St. John's wort, according to international guidelines for bioanalytical method validation. Chromatographic separation was performed on a C18 column with a combination of gradient and isocratic steps; the mobile phase composed of ammonium acetate solution (pH 4.5; 10 mM), acetonitrile and methanol. Quantification and method validation was performed using extract spiked with external reference standards of chlorogenic acid, rutin, hyperoside, isoquercitrin, quercetin and hypericin...
September 1, 2017: Journal of Chromatographic Science
https://www.readbyqxmd.com/read/28432535/exploring-the-carbamazepine-interaction-with-human-pregnane-x-receptor-and-effect-on-abcc2-using-in-vitro-and-in-silico-approach
#20
Gurpreet K Grewal, Khuraijam D Singh, Neha Kanojia, Chitra Rawat, Samiksha Kukal, Ajay Jajodia, Anshika Singhal, Richa Misra, Selvaraman Nagamani, Karthikeyan Muthusamy, Ritushree Kukreti
PURPOSE: Over expression of ATP-binding cassette transporters is considered one of the major reasons for non-responsiveness to antiepileptic drugs. Carbamazepine (CBZ), one of first line antiepileptic drug is known to influence ABCC2 expression but its exact molecular mechanism is unknown. METHODS: We investigated the effect of CBZ on expression of ABCC2 and pregnane X receptor (PXR) in HepG2 cell line and compared with hyperforin (agonist of PXR) and ketoconazole (antagonist of PXR) through realtime PCR and western blot assay...
July 2017: Pharmaceutical Research
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