Drug Discoveries & Therapeutics
Online ISSN : 1881-784X
Print ISSN : 1881-7831
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Showing 1-11 articles out of 11 articles from the selected issue
Original Articles
  • Masaki Ishii, Yasuhiko Matsumoto, Kazuhisa Sekimizu
    2018 Volume 12 Issue 4 Pages 185-188
    Published: August 31, 2018
    Released: September 18, 2018
    [Advance publication] Released: August 24, 2018
    JOURNALS FREE ACCESS

    Diabetes and obesity result from sucrose-induced hyperglycemia. Prevention of hyperglycemia contributes to inhibit the onset of these life-related diseases. Here we show that polysaccharides obtained from soil bacteria inhibit sucrose-induced hyperglycemia in an in vivo silkworm evaluation system. Ethanol precipitates of extracellular polysaccharides were prepared from viscous bacterial colonies. Among 24 samples obtained from different bacterial species, oral administration of 6 samples from Rhizobium altiplani, Cupriavidus sp., Paenibacillus polymyxa, Pantoea eucalypti, Variovorax boronicumulans, and Xanthomonas cynarae suppressed sucrose-induced hyperglycemia in silkworm insect larvae. The R. altiplani fraction treated further with DNase I, RNase A, and proteinase K, followed by phenol extraction also exhibited suppressive activity. Our results suggest that silkworms provide an efficient screening system of bacterial polysaccharides that inhibit sucrose-induced hyperglycemia.

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  • Temsiri Suwan, Sakornrat Khongkhunthian, Siriporn Okonogi
    2018 Volume 12 Issue 4 Pages 189-196
    Published: August 31, 2018
    Released: September 18, 2018
    JOURNALS FREE ACCESS

    Rice is staple food for people in many countries for centuries. It is therefore considered as safe and environmental friendly material for pharmaceutical formulations. In the present study, aqueous extracts of three different parts of rice grain; rice bran (RB), rice husk (RH), and rice germ (RG) were compared for their use as reducing agents in synthesis of silver nanoparticles (AgNPs). AgNPs from those three different parts of rice, RB-AgNPs, RH-AgNPs, and RG-AgNPs, respectively showed different reducing activity, which the highest capacity was RB. RG-AgNPs and RB-AgNPs showed the maximum absorption of AgNPs at 440 nm whereas that of RH-AgNPs was at 480 nm. FTIR spectra of all AgNPs indicated the presence of different functional groups from rice attached to the nanoparticles and these groups prevented the particle agglomeration. Size analysis using dynamic light scattering revealed that RB-AgNPs was the smallest particles (346.4 ± 36.8 nm) and possessed the highest negative zeta potential. Antimicrobial test showed that the AgNPs obtained from green synthesis mediated by rice extracts have great antimicrobial activity against Streptococcus mutans, the severe oral pathogenic bacteria causing dental caries. These results suggest that aqueous extracts of RB, RH, and RG have potential to be used as reducing agents in synthesis of silver nanoparticles.

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  • Rinrampai Puttipan, Sunee Chansakaow, Sakornrat Khongkhunthian, Siripo ...
    2018 Volume 12 Issue 4 Pages 197-205
    Published: August 31, 2018
    Released: September 18, 2018
    JOURNALS FREE ACCESS

    From the previous findings, the ethanolic fractionated extract of Caesalpinia sappan (F-EtOH) has high activity against Streptococcus mutans, the most severe cariogenic bacteria. The present study was aimed to isolate and identify the active compound of F-EtOH and compare its inhibitory activity against the biofilm of S. mutans as well as the cytotoxicity to oral fibroblast cells with F-EtOH. Compound isolation was done by column chromatography. The active compound was identified using liquid chromatography-mass spectrometry with electrospray ionization and nuclear magnetic resonance spectroscopy. It was found that the major compound of F-EtOH is brazilin. F-EtOH and brazilin were compared for inhibitory potential on the biofilms of three strains of S. mutans. The results exhibited that both F-EtOH and brazilin had potential on inhibiting biofilm formation and eradicating the preformed biofilms and their activity was dose dependent. F-EtOH showed significantly less toxic to normal periodontal ligament fibroblast than brazilin. At low concentration of 1- and 2-MBC, F-EtOH showed higher effective than brazilin. The results of our study suggest that the antibacterial activity of F-EtOH is according to the synergistic effects of the existing compounds including brazilin in F-EtOH.

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  • Siriporn Okonogi, Adchareeya Kaewpinta, Taepin Junmahasathien, Songwut ...
    2018 Volume 12 Issue 4 Pages 206-213
    Published: August 31, 2018
    Released: September 18, 2018
    JOURNALS FREE ACCESS

    The effects of variety and modification of rice on its antioxidant and anti-inflammatory activities were investigated. White rice varieties; Jasmine (JM) and Saohai (SH), and pigmented rice varieties; Doisket (DS) and Homnil (HN) were used. The modified rice samples were obtained from chemical modification using etherification reaction. The activities of the modified rice samples were compared with the ethanol extracts of the raw rice at the same rice concentration. Antioxidant activity was measured by the free radical scavenging activity tests and ferric reducing power assay. Results indicated that the ethanol extracts of raw rice had higher antioxidant activity than the modified rice. Among the raw rice tested, the pigmented rice showed higher antioxidant activity than white rice. Trolox equivalent antioxidant capacity values from free radical scavenging activity test were revealed that 50% ethanol extracts of HN and DS possessed the highest antioxidant activity. Ferric reducing power assay showed that 50% ethanol extracts of DS had the highest antioxidant activity. The anti-inflammatory activity was evaluated in vitro using a lipopolysaccharide-stimulated RAW264.7 macrophage cell model with enzyme-linked immunosorbent assay. Absolute ethanol extracts of HN reduced interleukin-6 secretion whereas that of DS suppressed interleukin-6 and tumor necrosis factor -α secretion. These results indicate that variety of rice, chemical modification, and extracting solvent were the factors that play an important role on antioxidant and anti-inflammatory activity. This study supports the potential use of the pigmented rice, especially DS, as a promising choice of a natural source because of its antioxidant and anti-inflammatory activities.

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  • Siddhartha Kumar, Arvind Kumar, Manisha Kaushal, Prince Kumar, Kasturi ...
    2018 Volume 12 Issue 4 Pages 214-223
    Published: August 31, 2018
    Released: September 18, 2018
    JOURNALS FREE ACCESS

    Staphylococcus aureus is an opportunistic pathogen, responsible for superficial and invasive infections both in nosocomial and community-acquired settings. The incidences of infection have become more problematic attributable to emerging drug resistance and biofilm formation. These challenges suggest the need for new antimicrobial agents against S. aureus. In present work, we purified a fungal xenobiotic (FI3) which elicits a potent antimicrobial activity against a list of tested microbes including methicillin sensitive (MSSA) and methicillin resistance (MRSA) S. aureus. The cell growth of MSSA and MRSA were completely ceased with the 1× minimum inhibitory concentration (MIC); 32 µg/mL and 128 µg/mL, respectively. The cell viability severely decreased within 90 min, due to disturbance of membrane homeostasis. This bactericidal effect was enhanced at lower pH (pH 4) with a speculation to retain positive charge. The FI3 potently disrupts biofilm adherence at 64 µg/mL and found to be a safe with no toxic effect on mammalian tissue. FI3 also leads to increase the potency of tested antibiotics. Taken together, we established that FI3 has a potent antimicrobial activity against tested microbes and safer to human tissue. It may be proven a leading molecule for the treatment of bacterial infections.

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  • Fuki Kurimoto, Satoko Hori, Yasufumi Sawada
    2018 Volume 12 Issue 4 Pages 224-232
    Published: August 31, 2018
    Released: September 18, 2018
    [Advance publication] Released: August 01, 2018
    JOURNALS FREE ACCESS

    Patients' experience of adverse reactions (ADR) and usability of drugs is important for proper use and post-marketing development of drugs, but it remains unclear whether and how patients are transmitting such information to others. The aim of this study was to explore differences in the ways in which bronchial asthma (BA) patients transmit experience of ADR to inhaled corticosteroids and usability of inhalers to others, including the reasons for these differences. A qualitative study involving focus-group interviews was conducted. Participants were fifteen Japanese BA patients treated with inhaled steroids who belonged to an association for BA patients. Data were analyzed using the constant comparative method. Almost all participants reported behavioral differences concerning ADR and usability. Participants actively expressed their doubts and anxieties about ADR to members of a patients' association and their attending physician. In contrast, information about patients' needs, including opinions and questions about the usability of steroids inhalers and anxieties regarding potential ADR to prolonged use of inhaled steroids, was shared only with members within the association and not disseminated outside, with some participants even choosing to keep it personal. Underlying this behavior was a mindset of perceiving efficacy and ADR to be more important than usability, and thinking "it is useless to inform anyone." In conclusion, behavioral differences of how BA patients transmit experience about ADR and usability was obvious, because benefit to inform usability was not perceived. It is necessary to make patients aware that transmitting their experience and comments about drugs is beneficial.

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  • Koichi Yabunaka, Gojiro Nakagami, Keiko Tabata, Junko Sugama, Masaru M ...
    2018 Volume 12 Issue 4 Pages 233-238
    Published: August 31, 2018
    Released: September 18, 2018
    JOURNALS FREE ACCESS

    This study aims to assess the fecal retention in elderly patients using colonic ultrasonography (US) in Japanese long-term care facility and determine the correlation between nutrition management methods and the fecal retention by US. This cross-sectional, single-center study was conducted in a long-term care facility in Japan. Patients with chronic constipation fulfilled the Rome III criteria for the diagnosis of functional constipation. US was performed on constipation patients with 4-day fecal retention before starting the standard management of constipation. After patients had defecated, nurses checked the outside of feces using King's Stool Chart and Bristol Stool Chart. All of 32 patients underwent the management of suppository laxative, the daily life independence level in grade C. In all cases, the King's Stool Chart did not detect > 200 g of fecal matter; the Bristol Stool Chart revealed type 5-7 in 56.2% of patients. The total parenteral nutrition and tube feeding did not completely detect type 1-2 in 0%. While the fecal retention groups comprised 15.6%, the non-fecal retention groups comprised 84.4%. The total parenteral nutrition did not completely detect the fecal retention in 0%. In the non-fecal retention groups, the King's Stool Chart indicated < 100 g in 81.8%, and the Bristol Stool Chart indicated type 5-7 in 100%. In conclusion, fecal properties of elderly constipation patients with the long-term parenteral nutrition should be assessed in follow-up examination by US, which is possible for personalized medical care by US, to avoid the administered regular management of constipation.

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  • Patrícia Lopes-Souza, Carla Fontoura Dionello, Danúbia da Cunha Sá-Cap ...
    2018 Volume 12 Issue 4 Pages 239-247
    Published: August 31, 2018
    Released: September 18, 2018
    JOURNALS FREE ACCESS

    The purpose of this systematic review was to investigate the effects of whole body vibration (WBV) exercise in the management of cancer therapy-related morbidities. The PubMED and PEDro databases were used to access publications published in English about the use of whole body vibration (WBV) exercises in cancer patients until February 22nd 2017. The studies included were classified according to the level of evidence (LE) by the National Health and Medical Research Council Hierarchy of evidence and the methodological quality (MQ) by the PEDro scale. The four included studies (2 of them with "high" LE-II and MQ) were performed in patients with different types of cancer (i.e. breast, lung, prostate, solid or hematological), treated with WBV exercise to counteract the cancer therapy-related morbidities. The variables evaluated were muscle activity, subjective rate of perceived exertion, exercise capacity, muscle strength, quality of life, resting urinary incontinence and severity of peripheral neuropathy. Although WBV exercise appears to be a potential treatment procedure of cancer therapy-related morbidities, further additional studies are required to determine specific and tailored protocols to be used in the different stages of the disease.

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  • Motoari Takata, Yuko Wada, Yurika Iwasawa, Miyuki Kumazawa, Ken-ichi S ...
    2018 Volume 12 Issue 4 Pages 248-253
    Published: August 31, 2018
    Released: September 18, 2018
    JOURNALS FREE ACCESS

    The physicochemical properties (pH, yield value, and squeeze force) of a drug for dermatomycosis, a terbinafine hydrochloride-containing cream (a brand-name product), and 12 over-the-counter drugs (OTCs) were measured and compared to ascertain the characteristics of each product. The pH of the brand-name product, Lamisil, was 4.1, and that of the OTC products ranged from 4.2 to 7.6; Lamisil Plus (7.6) had a significantly higher pH. Moreover, the yield value for Lamisil, as an index of cream ductility, was 128 dyn/cm2, and that for the OTC products ranged from 110 to 887 dyn/cm2. In particular, the OTC products Damalin (887 dyn/cm2), Barriact (512 dyn/cm2), and Exiv Deep (663 dyn/cm2) had a significantly higher yield value. In addition, the squeeze force was measured by attaching a HapLog® to the thumb and second finger. The squeeze force for Lamisil was 12.9 N, and that for the OTC products ranged from 1.8 to 14.6 N. The OTC product Bilumon (1.8 N) had a significantly lower squeeze force. These results indicated that there were marked differences in the pharmaceutical properties of brand-name and OTC products. External preparations are characterized by their feel during use. Based on the current results, the pharmaceutical characteristics of drugs resulted in differences in their feel during use, suggesting that products appropriate for individual patients can be recommended.

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Case Report
  • Parul Kodan, Nitin Gupta, Ankita Baidya, Ayan Basu, Abdul Razik, Ankit ...
    2018 Volume 12 Issue 4 Pages 254-258
    Published: August 31, 2018
    Released: September 18, 2018
    JOURNALS FREE ACCESS

    Filariasis can present in many different ways and pose significant dilemma to the clinician. We report four atypical cases of filariasis which presented as abdominal mass, cervical lymph node enlargement, fever in pregnancy and nosocomial febrile illness respectively. All the four cases were treated successfully with oral antifilarial agents. It is essential to be aware of such atypical presentations of filariasis so that prompt therapy can be initiated.

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