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Drug Discoveries & Therapeutics

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https://www.readbyqxmd.com/read/29081455/evaluation-of-the-innate-immune-stimulating-activity-of-amazake-using-a-silkworm-muscle-contraction-assay
#1
Hiroko Maruki-Uchida, Masahiko Sai, Kazuhisa Sekimizu
We evaluated the innate immune-stimulating activity of amazake using a silkworm muscle contraction assay. Sake cake, a raw material used to make amazake, had high innate immunity-stimulating activity, whereas rice malt, another raw material used to make amazake, did not, even after fermentation. These results suggest that the silkworm muscle contraction assay is a useful tool to screen foods with high innate immune-stimulating activity and that amazake made from sake cake has immunomodulatory potential.
October 30, 2017: Drug Discoveries & Therapeutics
https://www.readbyqxmd.com/read/29081439/isolation-of-antibiotic-producing-pseudomonas-species-with-low-temperature-cultivation-of-temperate-soil
#2
Shuhei Mitsutomi, Kazuhisa Sekimizu, Chikara Kaito
We performed low-temperature cultivation of soil samples in Tokyo, Japan, and isolated 30 bacterial strains that formed colonies at 4°C. All the culture supernatants of these bacteria exhibited antibacterial activity against Escherichia coli. The 16S rDNA sequences of 29 strains showed similarity to that of the Pseudomonas genus, whereas the 16S rDNA sequence of one strain showed similarity to that of the Janthinobacterium genus. We classified the 29 strains into 10 groups according to the 16S rDNA sequence similarities, and performed two phylogenetic analyses using the 16S rDNA and rpoD gene sequences...
October 29, 2017: Drug Discoveries & Therapeutics
https://www.readbyqxmd.com/read/29081438/two-spotted-cricket-as-an-animal-infection-model-of-human-pathogenic-fungi
#3
Yuto Kochi, Yasuhiko Matsumoto, Kazuhisa Sekimizu, Chikara Kaito
Invertebrate infection models that can be evaluated at human body temperature are limited. In this study, we utilized the two-spotted cricket, a heat-tolerant insect, as an animal infection model of human pathogenic fungi. Injection of human pathogenic fungi, including Candida albicans, Candida glabrata, and Cryptococcus neoformans killed crickets within 48 h at both 27˚C and 37˚C. The median lethal dose values (LD50 values) of C. albicans and C. glabrata against crickets were decreased at 37˚C compared to that at 27˚C, whereas the LD50 value of C...
October 29, 2017: Drug Discoveries & Therapeutics
https://www.readbyqxmd.com/read/29070744/glycyrrhizin-inhibits-human-parainfluenza-virus-type-2-replication-by-the-inhibition-of-genome-rna-mrna-and-protein-syntheses
#4
Kae Sakai-Sugino, Jun Uematsu, Miyuki Kamada, Hiroe Taniguchi, Saori Suzuki, Yumiko Yoshimi, Sahoko Kihira, Hidetaka Yamamoto, Mitsuo Kawano, Masato Tsurudome, Myles O'Brien, Makoto Itoh, Hiroshi Komada
The effect of glycyrrhizin on the replication of human parainfluenza virus type 2 (hPIV-2) was examined. Cell fusion induced by hPIV-2 was inhibited by glycyrrhizin, and glycyrrhizin reduced the number of viruses released from the cells. Glycyrrhizin did not change cell morphology at 1 day of culture, but caused some damage at 4 days, as determined by the effect on actin microfilaments. However, it affected the cell viability at 1 day: about 20% of the cells were not alive by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay at 1 day of culture...
October 24, 2017: Drug Discoveries & Therapeutics
https://www.readbyqxmd.com/read/29021505/skin-permeability-of-tulobuterol-in-two-transdermal-formulations-and-their-followability
#5
Yuichi Takizawa, Takeshi Goto, Shuji Sato, Naoya Ohmori, Kenji Mori, Yayoi Shimada, Kuei Chen, Takamitsu Miyagi, Fumio Fukai
Various generic transdermal formulations of tulobuterol containing rubber and acrylate base polymers are commercially available in Japan. However, none of the formulations have been compared directly with respect to the skin permeability of tulobuterol and to their follow ability. Tulobuterol Tape Sawai of rubber base and Tulobuterol Tape NP of acrylate base were used to conduct the in vitro 24-hour skin permeability test of tulobuterol at receiver solution temperatures of 32°C, 37°C, and 40°C. Furthermore, the followability of these tapes were examined by measuring the depth of the pores that were formed in their adhesive layer...
October 11, 2017: Drug Discoveries & Therapeutics
https://www.readbyqxmd.com/read/29021504/ethanol-extracts-of-aster-yomena-kitam-honda-inhibit-adipogenesis-through-the-activation-of-the-ampk-signaling-pathway-in-3t3-l1-preadipocytes
#6
Min Ho Han, Ji-Suk Jeong, Jin-Woo Jeong, Sung Hyun Choi, Sung Ok Kim, Su Hyun Hong, Cheol Park, Byung Woo Kim, Yung Hyun Choi
The leaves of Aster yomena (Kitam.) Honda have long been used as a traditional herb for treating disorders including coughs, asthma, and insect bites. According to recent studies, A. yomena leaf extracts have several pharmacological properties, including anti-inflammatory, antioxidant, and anti-asthmatic activities. However, little information is available regarding their anti-obesity effect. In this study, we investigated the inhibitory effect of the ethanol extracts of A. yomena leaves (EEAY) on adipocyte differentiation and adipogenesis using 3T3-L1 preadipocytes...
October 11, 2017: Drug Discoveries & Therapeutics
https://www.readbyqxmd.com/read/29021503/characterization-of-the-chemical-structure-and-innate-immune-stimulating-activity-of-an-extracellular-polysaccharide-from-rhizobium-sp-strain-m2-screened-using-a-silkworm-muscle-contraction-assay
#7
Makoto Urai, Tomoko Aizawa, Katsutoshi Imamura, Hiroshi Hamamoto, Kazuhisa Sekimizu
We screened innate immunostimulant-producing bacteria using a silkworm muscle contraction assay, and isolated Rhizobium sp. strain M2 from soil. We purified the innate immunostimulant from strain M2, and characterized the chemical structure by nuclear magnetic resonance spectroscopy and chemical analyses. The innate immunostimulant (M2 EPS) comprised glucose, galactose, pyruvic acid, and succinic acid with a molar ratio of 6.8:1.0:0.9:0.4, and had a succinoglycan-like high molecular-weight heteropolysaccharide structure...
October 11, 2017: Drug Discoveries & Therapeutics
https://www.readbyqxmd.com/read/29021502/structural-analysis-of-an-innate-immunostimulant-from-broccoli-brassica-oleracea-var-italica
#8
Makoto Urai, Keiko Kataoka, Satoshi Nishida, Kazuhisa Sekimizu
Vegetables are eaten as part of a healthy diet throughout the world, and some are also applied topically as a traditional medicine. We evaluated the innate immunostimulating activities of hot water extracts of various vegetables using the silkworm muscle contraction assay system, and found that broccoli, Brassica oleracea var. italica, contains a strong innate immunostimulant. We purified the innate immunostimulant from broccoli, and characterized the chemical structure by chemical analyses and NMR spectroscopy...
October 11, 2017: Drug Discoveries & Therapeutics
https://www.readbyqxmd.com/read/29021501/early-small-bowel-perforation-due-to-aflibercept
#9
Toufic Moussallem, Chetana Lim, Michael Osseis, Francesco Esposito, Eylon Lahat, Liliana Fuentes, Chady Salloum, Daniel Azoulay
In patients with malignancy who receive aflibercept based chemotherapy, gastrointestinal perforation is among the reported adverse events with a prevalence of 1.9%. This complication may lead to mortality up to 10.8%. We here report a case of small bowel perforation that occurred fifteen days after the first cycle of aflibercept in a 58-year old female who had metachronous colorectal liver metastases. Emergency laparotomy was performed and revealed a small bowel perforation without any anastomotic dehiscence...
October 11, 2017: Drug Discoveries & Therapeutics
https://www.readbyqxmd.com/read/28626112/experience-with-long-term-administration-of-tolvaptan-to-patients-with-acute-decompensated-heart-failure
#10
Shunsuke Kiuchi, Takahiro Fujii, Shinji Hisatake, Takayuki Kabuki, Oka Takashi, Shintaro Dobashi, Takanori Ikeda
Tolvaptan (TLV) is an oral selective vasopressin type 2 receptor antagonist. Long-term use of TLV is not recommended in patients with heart failure (HF) if fluid retention disappears and/or body weight is within the target range. However, some patients require long-term use of TLV. The current study investigated the efficacy and safety of long-term use of TLV. Subjects were 258 consecutive patients with HF who received TLV during hospitalization from January 2011 to March 2015. The rate of continuing administration of TLV was evaluated...
July 31, 2017: Drug Discoveries & Therapeutics
https://www.readbyqxmd.com/read/28652512/chryseobacterium-indolegenes-infection-in-a-patient-with-chronic-obstructive-pulmonary-disease
#11
Sevda Soydan, Seyda Ignak, Ozlem Unay Demirel, Gülkan Karadağ, Ayşen Aykent, Sinan Aslan
Chryseobacterium indolegenes is a rare pathogen that causes a variety of infections in inviduals who are mostly hospitalized with severe underlying diseases. Here we present a case of C. indolegenes in a 69-year-old male with chronic obstructive pulonary disease (COPD) who was admitted to the chest disease outpatient clinic with symptoms like cough, fever and sputum production and followed up on a suspicion of pneumonia. Despite the fact that our patient did not have any history of hospitalization for at least one year, pneumonia cause was due to C...
June 25, 2017: Drug Discoveries & Therapeutics
https://www.readbyqxmd.com/read/28652511/properties-of-induced-antimicrobial-activity-in-musca-domestica-larvae
#12
Kiyoshi Kawasaki, Minako Andoh
Insects produce antimicrobial molecules that contribute to their innate immune responses to eliminate invading microorganisms. To explore the potential utility of these antimicrobial molecules, we focused on larvae of the house fly Musca domestica, which is an efficient processor of organic waste and a good resource of protein and oil for animal feeding. The induction of hemagglutinating activity, which is usually accompanied by activation of innate immune responses in fly larvae, was observed in the hemolymph following needle injury...
June 25, 2017: Drug Discoveries & Therapeutics
https://www.readbyqxmd.com/read/28652510/beta-blocker-and-steroid-therapy-in-the-treatment-of-infantile-hepatic-hemangioendothelioma
#13
Zeynep Canan Özdemir, Yeter Düzenli Kar, Nurullah Cihan Şöhret, Mahmut Kebapçı, Özcan Bör
Infantile hepatic hemangioendothelioma (IHHE) is the most common benign vascular liver tumor and typically occurs during the first 6 months of life. A 4-month-old male patient presented with abdominal distention. A physical examination revealed massive hepatomegaly. Liver enzyme levels were normal. The alpha fetoprotein level was 1,323 mg/dL (6-1,000). Abdominal magnetic resonance imaging (MRI) showed multiple, well-defined and hyperintense nodular lesions in the liver. MRI findings suggested IHHE. The thyroid stimulating hormone (TSH) level was high (177...
June 25, 2017: Drug Discoveries & Therapeutics
https://www.readbyqxmd.com/read/28603180/intratumor-dihydropyrimidine-dehydrogenase-mrna-expression-levels-are-decreased-in-extramammary-paget-s-disease
#14
Yuki Nakamura, Ikko Kajihara, Yamada-Kanazawa Saori, Maeda-Otsuka Saki, Takamitsu Johno, Jun Aoi, Toshikatsu Igata, Shinichi Masuguchi, Satoshi Fukushima, Masatoshi Jinnin, Hironobu Ihn
S-1, a 5-fluorouracil (5-FU)-based anti-cancer agent, is an important drug for treating metastatic extramammary Paget's disease (EMPD). Although intratumor expression levels of 5-FU metabolism enzymes have been studied widely in many solid tumors, no studies have examined on the expression levels of thymidylate synthase (TS), orotate phosphoribosyl-transferase (OPRT) or dihydropyrimidine dehydrogenase (DPD) in skin cancers. The aim of this study was to estimate the intratumoral mRNA expression levels of these genes in EMPD by real time PCR...
June 11, 2017: Drug Discoveries & Therapeutics
https://www.readbyqxmd.com/read/28458299/genomic-analysis-of-vancomycin-resistant-staphylococcus-aureus-vrs3b-and-its-comparison-with-other-vrsa-isolates
#15
Suresh Panthee, Hiroshi Hamamoto, Atmika Paudel, Kazuhisa Sekimizu
High-level vancomycin resistance among Staphylococcus aureus poses a grave threat to global health as the treatment options for this pathogen are very limited. A detailed evaluation of the genetic background of vancomycin-resistant S. aureus (VRSA) is expected to facilitate the understanding of its origin and pathogenicity. In this study, we performed the genetic analysis of the clinical VRSA isolates and identified the genetic basis of resistance to multiple antibiotics among these strains, based on the available draft genome sequences...
May 30, 2017: Drug Discoveries & Therapeutics
https://www.readbyqxmd.com/read/28458298/biological-activities-and-antibacterial-biomarker-of-sesbania-grandiflora-bark-extract
#16
Pimporn Anantaworasakul, Hiroshi Hamamoto, Kazuhisa Sekimizu, Siriporn Okonogi
In the present study, the fractionated extracts of Sesbania grandiflora bark were prepared and evaluated for their biological activities. The ethyl acetate fractionate (EAF) showed high antioxidant activity along with free radical scavenging and reducing mechanisms. The free radical scavenging antioxidant activity of EAF was 69.3 ± 3.6% where its Trolox equivalent antioxidant capacity was 13.6 ± 0.7 mM/mg. EAF exhibited the reducing power equivalent to ferrous sulfate at 152 ± 2 mM/mg and equivalent to gallic acid at 1...
May 30, 2017: Drug Discoveries & Therapeutics
https://www.readbyqxmd.com/read/28458297/influence-of-clove-oil-and-eugenol-on-muscle-contraction-of-silkworm-bombyx-mori
#17
Kantaporn Kheawfu, Surachai Pikulkaew, Hiroshi Hamamoto, Kazuhisa Sekimizu, Siriporn Okonogi
Clove oil is used in fish anesthesia and expected to have a mechanism via glutamic receptor. The present study explores the activities of clove oil and its major compound, eugenol, in comparison with L-glutamic acid on glutamic receptor of silkworm muscle and fish anesthesia. It was found that clove oil and eugenol had similar effects to L-glutamic acid on inhibition of silkworm muscle contraction after treated with D-glutamic acid and kainic acid. Anesthetic activity of the test samples was investigated in goldfish...
May 30, 2017: Drug Discoveries & Therapeutics
https://www.readbyqxmd.com/read/28442678/frondoside-a-from-sea-cucumber-and-nymphaeols-from-okinawa-propolis-natural-anti-cancer-agents-that-selectively-inhibit-pak1-in-vitro
#18
Binh Cao Quan Nguyen, Kazuki Yoshimura, Shigenori Kumazawa, Shinkichi Tawata, Hiroshi Maruta
A sulfated saponin called "Frondoside A" (FRA) from sea cucumber and ingredients from Okinawa propolis (OP) have been previously shown to suppress the PAK1-dependent growth of A549 lung cancer as well as pancreatic cancer cells. However, the precise molecular mechanism underlying their anti-cancer action still remains to be clarified. In this study, for the first time, we found that both FRA and OP directly inhibit PAK1 in vitro in a selective manner (far more effectively than two other oncogenic kinases, LIMK and AKT)...
May 30, 2017: Drug Discoveries & Therapeutics
https://www.readbyqxmd.com/read/28442677/1-2-3-triazolyl-esterization-of-pak1-blocking-propolis-ingredients-artepillin-c-arc-and-caffeic-acid-ca-for-boosting-their-anti-cancer-anti-pak1-activities-along-with-cell-permeability
#19
Hideaki Takahashi, Binh Cao Quan Nguyen, Yoshihiro Uto, Md Shahinozzaman, Shinkichi Tawata, Hiroshi Maruta
Artepillin C (ARC) and caffeic acid (CA) are among the major anti-cancer ingredients of propolis, and block the oncogenic/melanogenic/ageing kinase PAK1. However, mainly due to their COOH moiety, cell-permeability of these herbal compounds is rather limited. Thus, in this study, in an attempt to increase their cell-permeability without any significant loss of their water-solubility, we have esterized both ARC and CA with the water-soluble 1,2,3-triazolyl alcohol through Click Chemistry. We found that this esterization boosts the anti-cancer activity of ARC and CA by 100 and over 400 folds, respectively, against the PAK-dependent growth of A549 lung cells, but show no effect on the PAK1-independent growth of B16F10 melanoma cells...
May 30, 2017: Drug Discoveries & Therapeutics
https://www.readbyqxmd.com/read/28442657/structural-characterization-and-biological-activities-of-a-novel-polysaccharide-from-phyllanthus-emblica
#20
Zihan Zeng, Wenjie Lv, Yongshuai Jing, Zhiyan Chen, Liyan Song, Ting Liu, Rongmin Yu
A novel water-soluble polysaccharide named PEPW80-1, with a molecular mass of 4.7 kDa, was isolated from the pulp tissues of Phyllanthus emblica, and purified by sephadex G-100 column and sephacryl S-300 HR chromatography. The structural features of PEPW80-1 were investigated by a combination of acid hydrolysis, periodate oxidation-Smith degradation, methylation analysis, gas chromatography-mass spectrometry, scanning electron microscope, Fourier transform infrared spectroscopy, and nuclear magnetic resonance spectroscopy...
May 30, 2017: Drug Discoveries & Therapeutics
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