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Drug Discoveries & Therapeutics

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https://www.readbyqxmd.com/read/28320984/investigation-of-antiaromatase-activity-using-hepatic-microsomes-of-nile-tilapia-oreochromis-niloticus
#1
Tanongsak Sassa-Deepaeng, Wasana Chaisri, Surachai Pikulkaew, Siriporn Okonogi
Microsomal aromatase enzymes of humans and rats have been used in antiaromatase assays, but enzyme activity is species-specific. The current study extracted hepatic microsomes of Nile tilapia (Oreochromis niloticus) to investigate and compare the antiaromatase activity of chrysin, quercetin, and quercitrin. This activity was evaluated using a dibenzylfluorescein (DBF) assay. Results revealed that the age and body weight of Nile tilapia affected the yield of extracted microsomes. Extraction of hepatic microsomes of Nile tilapia was most effective when using a reaction medium with a pH of 8...
March 19, 2017: Drug Discoveries & Therapeutics
https://www.readbyqxmd.com/read/28320983/levetiracetam-and-topiramate-poisoning-two-overdoses-on-those-drugs-with-no-lasting-effects
#2
Moaziz Sarfaraz, Rana Hasan Syeda
Levetiracetam and topiramate are newer anticonvulsants, which is why international data on overdoses of these drugs are lacking. Only a few mild adverse reactions have been noted. These anticonvulsants have been the drug of choice for neurologists. Despite their wide usage, there is a dearth of literature on symptoms and signs of their toxicity. Presented here is the case of a 21-year-old female who overdosed twice on levetiracetam and topiramate. The woman was admitted and discharged after the first overdose...
March 19, 2017: Drug Discoveries & Therapeutics
https://www.readbyqxmd.com/read/28320982/comparison-of-three-acute-stress-models-for-simulating-the-pathophysiology-of-stress-related-mucosal-disease
#3
Bhagawati Saxena, Sanjay Singh
Stress-related mucosal disease (SRMD) is highly prevalent in intensive care patients leading to increasing treatment cost and mortality. SRMD is a disease elusive of ideal treatment. Evaluation of drugs is very pertinent for the efficient and safe treatment of SRMD. It relies mainly on in vivo screening models. There are various stress models, and till date, none of them is validated for simulating the SRMD pathophysiology. The present study aims to choose the best model, which reproduce pathophysiology of SRMD, among previously established stress models...
March 19, 2017: Drug Discoveries & Therapeutics
https://www.readbyqxmd.com/read/28228617/silkworm-fungal-infection-model-for-identification-of-virulence-genes-in-pathogenic-fungus-and-screening-of-novel-antifungal-drugs
#4
Masaki Ishii, Yasuhiko Matsumoto, Ikuko Nakamura, Kazuhisa Sekimizu
The silkworm infection model has the potential to replace conventional animal models for evaluation of the efficacy and toxicity of investigational antifungal agents. Silkworms are relatively inexpensive, can be simply grown in large numbers and can be easily infected with pathogenic fungi, including mutant strains. Antifungal agents can then be injected into the silkworm either via the hemolymph to mimic intravenous administration or directly into the gut for oral administration, and their antifungal effect can be evaluated...
February 21, 2017: Drug Discoveries & Therapeutics
https://www.readbyqxmd.com/read/28202883/decreased-sugar-concentration-in-vegetable-and-fruit-juices-by-growth-of-functional-lactic-acid-bacteria
#5
Masaki Ishii, Yasuhiko Matsumoto, Satoshi Nishida, Kazuhisa Sekimizu
Leuconostoc carnosum #7-2, L. gelidum #4-2, and L. mesenteroides 8/11-3, which were isolated from fermented plant foods, are lactic acid bacteria. We previously reported that these bacteria are functional lactic acid bacteria whose innate immunity-stimulating activities are high based on a silkworm muscle contraction assay. The concentrations of these three lactic acid bacteria increased to more than 1 × 10(6) colony forming units (cfu)/mL in various vegetable and fruit juices when the pH values were appropriately adjusted...
February 14, 2017: Drug Discoveries & Therapeutics
https://www.readbyqxmd.com/read/28202882/lactic-acid-bacteria-of-the-leuconostoc-genus-with-high-innate-immunity-stimulating-activity
#6
Masaki Ishii, Satoshi Nishida, Keiko Kataoka, Yayoi Nishiyama, Shigeru Abe, Kazuhisa Sekimizu
We screened lactic acid bacteria that exhibited high innate immunity-stimulating activity by monitoring muscle contraction activity in silkworms. Heat-treated fractions of lactic acid bacteria, Leuconostoc carnosum #7-2, Leuconostoc gelidum #4-2, and Leuconostoc mesenteroides 8/11-3, had high (250-460 units/mg) innate immunity-stimulating activity. These lactic acid bacteria proliferated in milk to concentrations of 1 × 10(6) colony forming unit/mL. The present findings suggest that the silkworm muscle contraction assay is useful for screening lactic acid bacteria with high innate immunity-stimulating activity, and that the assay can be used for the production of fermented foods made from milk...
February 14, 2017: Drug Discoveries & Therapeutics
https://www.readbyqxmd.com/read/28202881/the-exercise-paradox-may-be-solved-by-measuring-the-overall-thrombotic-state-using-native-blood
#7
Hideo Ikarugi, Junichiro Yamamoto
While exercise is widely believed to prevent atherothrombotic diseases, it occasionally causes sudden death. This exercise paradox may be due to the inadequate testing of the thrombotic and thrombolytic status. A recently developed shear-induced thrombosis/endogenous fibrinolysis test performed with non-anticoagulated blood samples allows the assessment of the thrombotic state of an individual both at rest and after exercise. This sensitive and physiologically relevant test may help to solve the aforementioned exercise paradox...
February 14, 2017: Drug Discoveries & Therapeutics
https://www.readbyqxmd.com/read/28190800/cocoon-carcinomatosa-an-unusual-cause-of-intestinal-obstruction
#8
Jimil Shah, Amit Kumar, Harjeet Singh, Roshan Agarwala, Vishal Sharma, Surinder S Rana
Abdominal cocoon, also termed sclerosing encapsulating peritonitis, is an uncommon entity associated with formation of a fibro-collagenous membrane around intestinal loops resulting in intestinal obstruction. Most reported cases are idiopathic, but many other causes have been implicated in cocoon formation, including use of continuous ambulatory peritoneal dialysis, peritoneal tuberculosis, and connective tissue disease. However, peritoneal carcinomatosis is a rarely reported entity that causes this condition...
February 13, 2017: Drug Discoveries & Therapeutics
https://www.readbyqxmd.com/read/28190799/short-lived-non-coding-transcripts-slits-clues-to-regulatory-long-non-coding-rna
#9
Hidenori Tani
Whole transcriptome analyses have revealed a large number of novel long non-coding RNAs (lncRNAs). Although the importance of lncRNAs has been documented in previous reports, the biological and physiological functions of lncRNAs remain largely unknown. The role of lncRNAs seems an elusive problem. Here, I propose a clue to the identification of regulatory lncRNAs. The key point is RNA half-life. RNAs with a long half-life (t1/2 > 4 h) contain a significant proportion of ncRNAs, as well as mRNAs involved in housekeeping functions, whereas RNAs with a short half-life (t1/2 < 4 h) include known regulatory ncRNAs and regulatory mRNAs...
February 13, 2017: Drug Discoveries & Therapeutics
https://www.readbyqxmd.com/read/28179604/ability-of-community-pharmacists-to-promote-self-care-and-self-medication-by-local-residents-i-improvements-in-bone-mineral-density
#10
Yoshiko Wada, Yuko Wada, Satoko Ennyu, Ken-Ichi Shimokawa, Fumiyoshi Ishii
This study was conducted in order to establish a health management method for the elderly in a community through follow-ups of bone mineral density (BMD) measurement results over a 1-year period based on BMD measurements performed by pharmacists and a guidance program. Regarding BMD measurement results, the percent young adult mean (%YAM: mean BMD in healthy persons of the same sex aged between 51 and 82 years old) significantly increased in Period I, during which the intervention by pharmacists was performed (6 months after the start of measurements), but significantly decreased in Period II, during which this intervention was not performed (between 7 and 12 months after the start of measurements)...
February 8, 2017: Drug Discoveries & Therapeutics
https://www.readbyqxmd.com/read/28123157/olive-and-ginkgo-extracts-as-potential-cataract-therapy-with-differential-inhibitory-activity-on-aldose-reductase
#11
Diaaeldin Mohamed Abdelkawi Elimam, Ahmed Salah Uddin Ibrahim, Gregory Ing Liou, Farid Abd-Elrehim Abd-Elaziz Badria
Aldose reductase (AR) has been the leading target in the treatment of diabetic cataract. Although numerous synthetic AR inhibitors (ARI) have been identified, their adverse side effects currently preclude their use. Olive leaf extract (OLE) as well as ginkgo leaf extract (GLE) are natural supplements that have wide therapeutic indices and a plethora of salutary effects during diabetes that so far untested on sugar cataract progression. As such, the present study sought to evaluate the AR-inhibiting properties of OLE and GLE using the isolated enzyme from rabbit lens...
January 26, 2017: Drug Discoveries & Therapeutics
https://www.readbyqxmd.com/read/28123156/scientific-evidence-for-therapeutic-effects-of-chinese-prescription-kangen-karyu-from-pre-clinical-animal-experiments
#12
Takako Yokozawa, Chan Hum Park, Kinzo Matsumoto
Chinese prescription Kangen-karyu, comprised of six crude drugs, has received much attention due to its numerous biological activities. The present study reports therapeutic evidence for Kangen-karyu from pre-clinical animal experiments related to human diseases. Kangen-karyu showed beneficial effects on type 1 diabetes and related complications through the suppression of protein expression related to advanced glycation endproducts and oxidative stress. Kangen-karyu reduced oxidative stress via the regulation of dyslipidemia, and also exerted a renoprotective effect mainly through its antioxidant properties during the development of diabetic nephropathy in type 2 diabetes...
January 26, 2017: Drug Discoveries & Therapeutics
https://www.readbyqxmd.com/read/28123155/rivaroxaban-induced-chest-wall-spontaneous-expanding-hematoma
#13
Nikolaos S Salemis
Rivaroxaban is an oral direct Factor Xa inhibitor approved in the European Union and the United Sates for the single-drug treatment of several thromboembolic diseases in adults. Ιt has been evaluated in large phase III clinical trials and has been found to have similar efficacy and safety with standard therapy. Herein, is described a very rare case of a rivaroxaban-induced spontaneous expanding chest wall hematoma, that required surgical intervention, in a breast cancer patient. Use of the Naranjo adverse drug reaction probability scale indicated a probable relationship (score of 7) between the patient's development of hematoma and treatment with rivaroxaban...
January 26, 2017: Drug Discoveries & Therapeutics
https://www.readbyqxmd.com/read/27990007/a-newborn-with-hemorrhagic-meningoencephalitis-due-to-proteus-mirabilis
#14
Yesim Coskun, Ipek Akman, Canan Yildirim, Mustafa Kemal Demir
Neonatal meningoencephalitis is a severe condition for the developing brain of a newborn. Radiologic findings of necrosis and liquefaction due to hemorrhagic meningoencephalitis may be confused with brain abcess. In this article, we report a neonate having liquefaction necrosis due to hemorrhagic meningoencephalitis mimicing intracranial abscess due to Proteus mirabilis. We would like to describe the clinical course and evolution of brain imaging and emphasize the importance of the serial MR imaging (MRI).
December 18, 2016: Drug Discoveries & Therapeutics
https://www.readbyqxmd.com/read/27990006/nitric-oxide-donor-hybrid-compounds-as-promising-anticancer-agents
#15
Qin-Ge Ding, Jie Zang, Shuai Gao, Qianwen Gao, Wenwen Duan, Xiaoyang Li, Wenfang Xu, Yingjie Zhang
Nitric oxide (NO) plays important roles in cardiovascular regulation, nerve transmission delivery and immune responses. In the last semicenturry, it has been proved that though low concentration of NO is tumor-promoting, high concentration of NO could exhibit multiple antitumor effects, which led to the research and development of kinds of NO donors and NO donor hybrid compounds as antitumor agents. Herein, the recent development of NO donor hybrid compounds is briefly reviewed.
December 18, 2016: Drug Discoveries & Therapeutics
https://www.readbyqxmd.com/read/27890872/effect-of-astigmatism-on-refraction-in-children-with-high-hyperopia
#16
Hao Hu, Jinhui Dai, Minjie Chen, Lanting Chen, Lingli Jiang, Ran Lin, Ling Wang
The aim of this study was to evaluate primitively whether the extent and component of astigmatism influences regression in degree of spherical (DS) and the best corrected visual acuity (BCVA) of children with hyperopia of +5.00 diopters (D) or greater. Children were screened from the outpatient refraction database in the Wenling No. 1 People's Hospital in Zhejiang province and in Eye & ENT Hospital of Fudan University between June 2005 and December 2015. Eligible eyes were divided into three groups according to the extent of astigmatism: group of astigmatism ≤ -2 D of cylinder, group without astigmatism or with astigmatism ≥ -0...
November 27, 2016: Drug Discoveries & Therapeutics
https://www.readbyqxmd.com/read/27795481/gene-delivery-systems-by-the-combination-of-lipid-bubbles-and-ultrasound
#17
Yoichi Negishi, Yoko Endo-Takahashi, Kazuo Maruyama
Gene therapy is promising for the treatment of many diseases including cancers and genetic diseases. From the viewpoint of safety, ultrasound (US)-mediated gene delivery with nano/ microbubbles was recently developed as a novel non-viral vector system. US-mediated gene delivery using nano/microbubbles are able to produce transient changes in the permeability of the cell membrane after US-induced cavitation while reducing cellular damage and enables the tissue-specific or the site-specific intracellular delivery of gene both in vitro and in vivo...
October 28, 2016: Drug Discoveries & Therapeutics
https://www.readbyqxmd.com/read/27773889/nucleic-acid-drugs-and-dna-based-delivery-systems
#18
Makiya Nishikawa
Nucleic acids are biologically active materials, and chemically modified nucleic acids are now being used in nucleic acid drugs. DNA, one of the two types of nucleic acids, can also be used as a material to construct DNA-based delivery systems, such as DNA hydrogel, for therapeutic compounds. Use of chemically modified nucleic acids would greatly increase the therapeutic potency of such DNA-based delivery systems. However, attention should be paid to the differences in the physicochemical properties of natural and chemically modified nucleic acids...
October 23, 2016: Drug Discoveries & Therapeutics
https://www.readbyqxmd.com/read/27746419/the-serum-pdgf-dependent-melanogenic-role-of-the-minute-level-of-the-oncogenic-kinase-pak1-in-melanoma-cells-proven-by-the-highly-sensitive-kinase-assay
#19
Pham Thi Be Tu, Binh Cao Quan Nguyen, Shinkichi Tawata, Cheong-Yong Yun, Eung Gook Kim, Hiroshi Maruta
We previously demonstrated that the oncogenic kinase PAK4, which both melanomas and normal melanocytes express at a very high level, is essential for their melanogenesis. In the present study, using the highly sensitive "Macaroni-Western" (IP-ATP-Glo) kinase assay, we investigated the melanogenic potential of another oncogenic kinase PAK1, which melanoma (B16F10) cells express only at a very minute level. After transfecting melanoma cells with PAK1-shRNA for silencing PAK1 gene, melanin content, tyrosinase activity, and kinase activity of PAK1 were compared between the wild-type and transfectants...
October 17, 2016: Drug Discoveries & Therapeutics
https://www.readbyqxmd.com/read/27746418/smart-polymeric-nanocarriers-for-small-nucleic-acid-delivery
#20
Kanjiro Miyata
In recent decades, nucleic acid therapeutics have been attracting much attention because of their potential as treatments for various diseases that require high target specificity. Nevertheless, the number of approved nucleic acid drugs is very limited due to substantially poor bioavailability, thereby generating the need for nucleic acid delivery carriers. A variety of delivery formulations have been reported so far. This review particularly describes polymer-based delivery carriers for systemic administration, highlighting the potential of biological environment-responsive chemistry for overcoming the biological barriers to nucleic acid delivery...
October 17, 2016: Drug Discoveries & Therapeutics
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