Drug Discoveries & Therapeutics
Online ISSN : 1881-784X
Print ISSN : 1881-7831
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Volume 9 , Issue 6
Showing 1-8 articles out of 8 articles from the selected issue
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Review
  • Qi Tang, Xueqin Li, Peipei Song, Lingzhong Xu
    Volume 9 (2015) Issue 6 Pages 380-385
    Released: January 18, 2016
    JOURNALS FREE ACCESS
    Diabetes mellitus (DM) appears to be increasing rapidly, threatening to reduce life expectancy for humans around the globe. The International Diabetes Federation (IDF) has estimated that there will be 642 million people living with the disease by 2040 and half as many again who will be not diagnosed. This means that pre-DM screening is a critical issue. Insulin resistance (IR) has emerged as a major pathophysiological factor in the development and progression of DM since it is evident in susceptible individuals at the early stages of DM, and particularly type 2 DM (T2DM). Therefore, assessment of IR via the homeostasis model assessment of IR (HOMA-IR) is a key index for the primary prevention of DM and is thus found in guidelines for screening of high-risk groups. However, the cut-off values of HOMA-IR differ for different races, ages, genders, diseases, complications, etc. due to the complexity of IR. This hampers the determination of specific cut-off values of HOMA-IR in different places and in different situations. China has not published an official index to gauge IR for primary prevention of T2DM in the diabetic and non-diabetic population except for children and adolescents ages 6-12 years. Hence, this article summarizes developments in research on IR, HOMA-IR, and pre-DM screening in order to provide a reference for optimal cut-off values of HOMA-IR for the diagnosis of DM in the Chinese population.
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Original Articles
  • Kazumi Hayama, Miki Takahashi, Satoru Yui, Shigeru Abe
    Volume 9 (2015) Issue 6 Pages 386-390
    Released: January 18, 2016
    JOURNALS FREE ACCESS
    We examined the effect of 5 saturated fatty acids and their related alcohols on the growth of Candida albicans. The inhibitory effects of these compounds against the yeast and hyphal growth forms of C. albicans were examined using the modified NCCLS method and crystal violet staining, respectively. Among these compounds, capric acid inhibited both types of growth at the lowest concentration. The IC80, i.e., the concentration at which the compounds reduced the growth of C. albicans by 80% in comparison with the growth of control cells, of capric acid for the hyphal growth of this fungus, which is indispensable for its mucosal invasion, was 16.7 μM. These fatty acids, including capric acid, have an unpleasant smell, which may limit their therapeutic use. To test them at reduced concentrations, the combined effect of these fatty acids and oligonol, a depolymerized polyphenol, was evaluated in vitro. These combinations showed potent synergistic inhibition of hyphal growth [fractional inhibitory concentration (FIC) index = 0.319]. Our results demonstrated that capric acid combined with oligonol could be used as an effective anti-Candida compound. It may be a candidate prophylactic or therapeutic tool against mucosal Candida infection.
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  • Rezeng Caidan, Limao Cairang, Jiumei Pengcuo, Li Tong
    Volume 9 (2015) Issue 6 Pages 391-396
    Released: January 18, 2016
    JOURNALS FREE ACCESS
    Rubus amabilis, Rubus niveus Thunb., and Rubus sachalinensis are three Rubus species that are alternatively found in Manubzhithang, a Tibetan medicine, in different areas of China. The current study analyzed HPLC/UV chromatograms and it compared compounds of these three Rubus species in contrast to reference substances such as 2,6-dimethoxy-4-hydroxyphenol-1-O-β-D-glucopyranoside, procyanidin B4, and isovitexin-7-O-glucoside. The three Rubus species produced similar peaks in chromatograms. The antioxidant activity of the three Rubus species was determined using an assay for DPPH free radical scavenging activity. Results indicated that the three Rubus species extracts had almost the same level of free radical scavenging activity. Thus, findings indicated the rationality of substituting these species for one another as an ingredient in Manubzhithang.
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  • Siriporn Okonogi, Adchareeya Kaewpinta, Songwut Yotsawimonwat, Sakornr ...
    Volume 9 (2015) Issue 6 Pages 397-403
    Released: January 18, 2016
    JOURNALS FREE ACCESS
    The objective of the present study was to prepare buccal anesthetic gels using rice as gelling agent. Rice grains of four rice varieties, Jasmine (JM), Saohai (SH), Homnil (HN), and Doisket (DS) were chemically modified. Buccal rice gels, containing lidocaine hydrochloride as local anesthetic drug were formulated using the respective modified rice varieties. The gels were evaluated for outer appearance, pH, color, gel strength, foaming property, adhesion, in vitro drug release and in vivo efficacy. It was found that the developed rice gels possessed good texture. Rice varieties showed influence on gel strength, color, turbidity, adhesive property, release property, and anesthetic efficacy. JM gel showed the lowest turbidity with light transmission of 86.76 ± 1.18% whereas SH gel showed the highest gel strength of 208.78 ± 10.42 g/cm2. Lidocaine hydrochloride can cause a decrease in pH and adhesive property but an increase in turbidity of the gels. In vitro drug release profile within 60 min of lidocaine SH gel and lidocaine HN gel showed that lidocaine could be better released from SH gel. Evaluation of in vivo anesthetic efficacy in 100 normal volunteers indicates that both lidocaine rice gels have high efficacy but different levels. Lidocaine SH gel possesses faster onset of duration and longer duration of action than lidocaine HN gel.
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  • Tushar Sehgal, Jasbir Kaur Hira, Jasmina Ahluwalia, Reena Das, Rajesh ...
    Volume 9 (2015) Issue 6 Pages 404-410
    Released: January 18, 2016
    JOURNALS FREE ACCESS
    Coumarin derivatives such as warfarin and acenocoumarol are used in various disorders such as deep venous thrombosis, pulmonary embolism, atrial fibrillation and artificial heart valves. They have improved prognosis of patients with thromboembolic disease. An individual's response to coumarins depends on several factors. The non-genetic factors include age, gender, body mass index, diet and interacting drugs. Among the genetic factors, the cytochrome P450 system and vitamin K epoxide reductase complex subunit 1 play a key role in drug metabolism. This was a prospective hospital based study in which allele and genotypic frequencies of CYP2C9 gene polymorphisms; 430C>T and 1075A>C and VKORC1 gene polymorphisms; 1639G>A, 9041G>A and 6009C>T in 106 alleles of north Indian patients with valve replacement on acenocoumarol were determined and their effect on acenocoumarol dosing was studied. To the best of our knowledge, this is first report of VKORC1 9041G>A and 6009C>T gene polymorphisms and their effect on acenocoumarol dosing from north India. In 53 patients with valve replacement on acenocoumarol with stable INR, the allele frequency of CYP2C9*2 and CYP2C9*3 gene polymorphisms was 0.05 and 0.17 respectively and that of VKORC1 *2,*3 and *4 gene polymorphisms was 0.15, 0.72 and 0.11 respectively. The presence of CYP2C9*3 or VKORC1*2 gene polymorphism were associated with decrease in acenocoumarol dose requirements (p values 0.03 and 0.02 respectively).This study confirmed the association of lower mean weekly dosages of acenocoumarol in patients with CYP2C9*3 and VKORC1*2 gene polymorphisms. An unusually high frequency of 9041A polymorphism in VKORC1 was found in study population.
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  • Zhipeng Sun, Yubing Zhu, Guangzhong Xu, Aminbuhe, Nengwei Zhang
    Volume 9 (2015) Issue 6 Pages 411-416
    Released: January 18, 2016
    JOURNALS FREE ACCESS
    Nosocomial infection is a common complication after abdominal oncology surgery. Aimed at finding its independent risk factors for prevention, all the patients who underwent abdominal oncology surgery were summarized from March 1st, 2010 to March 1st, 2013 from the oncology surgery department, Beijing Shijitan Hospital. The investigated variances were patients’ information including admission number, sex, age, diabetes, diagnosis, length of stay, American society of anesthesiologists (ASA) grade, surgery time, number of drainage tubes. Comparisons were taken between the infected cases and non-infected cases for retrospective logistic regression analysis. 4 variances including diabetes, preoperative hospitalization time ≥ 6 days, surgery time ≥ 230 minutes, ASA grade ≥ III were found out to be related to nosocomial infection after surgery. The 4 variances mentioned above were risk factors for nosocomial infection after surgery.
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Brief Report
  • Munehiro Nakata, Shota Kawaguchi, Ayami Oikawa, Akito Inamura, Shunki ...
    Volume 9 (2015) Issue 6 Pages 417-421
    Released: January 18, 2016
    JOURNALS FREE ACCESS
    An aqueous extract from toad skin, cinobufacini, has been known to possess anticancer ability. The present study examined effect of toad skin extract on activity of gelatinases including matrix metalloproteinases-2 and -9 which play an important role in invasion of carcinoma cells. Gelatinase activities derived from fetal serum albumin and culture medium of human breast carcinoma cell line MDA-MB-231 were significantly prevented in the presence of toad skin extract. The inhibitory activity was found in water-soluble fraction of the extract prepared by the Bligh & Dyer method but not in CHCl3-soluble lipid fraction. These results suggest that an aqueous extract from toad skin contains a water-soluble substance possessing a potent ability to prevent gelatinase activity. In conclusion, the water-soluble substance in toad skin extract cinobufacini may be able to regulate cancer cell migration accelerated by matrix metalloproteinases.
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Case Report
  • Michael Osseis, Chetana Lim, Eylon Lahat, Alexandre Doussot, Chady Sal ...
    Volume 9 (2015) Issue 6 Pages 422-423
    Released: January 18, 2016
    JOURNALS FREE ACCESS
    In Clozapine users constipation is among the reported side effects including agranulocytosis and myocarditis with prevalence rates ranging from 14% to 60%. In extreme cases this may lead to bowel obstruction and paralytic ileus which, if not detected and treated early, may lead to mortality up to 30%. We report the first case of hepatic outflow block secondary to compression of the liver by a distended colon upstream an impacted fecaloma in a 47-year old schizophrenic man treated by clozapine. Emergency sub-total colectomy was performed for pan-colonic ischemia. Surgery relieved the liver outflow block and was followed by uneventful outcome. Patients receiving clozapine should undergo routine laxatives and monitoring in order to limit the risk of clozapine-related ileus and bowel ischemia.
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