• Journal of Microbiology and Biotechnology
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• v.25 no.9
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• pp.1510-1518
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• 2015

In this work, we wanted to develop a probiotic from famous longevity villages in Korea. We visited eight longevity villages in Korea to collect fecal samples from healthy adults who were aged above 80 years and had regular bowel movements, and isolated lactic-acid-producing bacteria from the samples. Isolated colonies that appeared on MRS agar containing bromophenol blue were identified by means of 16S rRNA sequencing, and 102 of the isolates were identified as lactic-acid-producing bacteria (18 species). Lactobacillus fermentum was the most frequently found species. Eight isolates were selected on the basis of their ability to inhibit the growth of six intestinal pathogens (Escherichia coli O157:H7, Salmonella enterica subsp. enterica Typhimurium, Salmonella enterica subsp. enterica Enteritidis, Enterococcus faecalis, Staphylococcus aureus, and Listeria monocytogenes) and their susceptibility to 15 antimicrobial agents. Among these eight isolates, four Lactobacillus fermentum isolates were found not to produce any harmful enzymes or metabolites. Among them, Lactobacillus fermentum isolate no. 24 showed the strongest binding to intestinal epithelial cells, the highest immune-enhancing activity, anti-inflammation activity, and anti-oxidation activity as well as the highest survival rates in the presence of artificial gastric juice and bile solution. This isolate, designated Lactobacillus fermentum PL9988, has all the characteristics for a good probiotic.

• Journal of Pharmaceutical Investigation
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• v.38 no.4
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• pp.255-259
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• 2008

The present study aimed to investigate the in-vitro characteristics of N4-amino acid derivatives of cytarabine for the oral delivery of cytarabine. After the synthesis of L-Ile-cytarabine, L-Leu-cytarabine and L-Arg-cytarabine, the gastrointestinal stability of each prodrug was examined using artificial gastric juice and intestinal fluids. The cellular uptake characteristics of prodrugs were also examined in Caco-2 cells. While L-Ile-cytarabine and L-Leu-cytarabine appeared to be stable in all the tested biological media during 4-hr incubation, L-Arg-cytarabine was rapidly disappeared within 5 min. Accordingly, the cellular uptake of L-Ile-cytarabine and L-Leu-cytarabine was significantly higher than that of its parent drug, cytarabine in Caco-2 cells but the cellular uptake of L-Arg-cytarabine was similar to that from its parent drug. The cellular uptake of L-Ile-cytarabine and L-Leu-cytarabine appeared to be saturable as drug concentration increased from 0.4 to 4 mM. Collectively, L-Ile-cytarabine and L-Leu-cytarabine could be promising candidates to improve the oral absorption of cytarabine via a saturable transport pathway.

• Journal of Pharmaceutical Investigation
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• v.17 no.1
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• pp.1-14
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• 1987

To increase the bioavailability of norfloxacin, inclusion complex of antimicrobial agent norfloxacin with ${\beta}-Cyclodextrin$ was prepared and studied by the solubility method, spectrophotometric methods(UV, IR, $^1H-NMR$), differential thermal analysis, powder X-ray diffractometry, the physical properties, the antimicrobial activity, DNA binding and in situ recirculation technique. The conclusions are summerized as following; 1) The inclusion complexation was identified by means of solubility, spectrophotometry(UV, IR, NMR), DTA and X-ray diffraction. 2) The molar ratio of $norfloxacin-{\beta}-cyclodextrin$ complex was 1 : 1. 3) The stability constant of $norfloxacin-{\beta}-cyclodextrin$ complex was $21.5\;M^{-1}$, and both true and apparent partition coefficients of the inclusion complex were larger than those of norfloxacin. 4) The time required to dissolve 60% $(T_{60}%)$ of the inclusion complex was 120 min. in distilled water and in the artificial intestinal juice, while norfloxacin did not reach to 60% dissolution within 120 min. 5) The antimicrobial activity of the inclusion complex against Pseudomonas aeruginosa, Klebsiella pneumoniae and Staphylococcus aureus showed no significant difference compared to that of norfloxacin alone. 6) Studies on binding properties between the inclusion complex and norfloxacin alone to DNA according to equilibrium dialysis showed no significant differency. 7) In situ absorption rates (Ka) of inclusion complex and norfloxacin alone were 0.229 and $0.102hr^{-1}$, respectively.

• Journal of Pharmaceutical Investigation
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• v.15 no.2
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• pp.53-62
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• 1985

Pivampicillin hydrochloride is a kind of broad spectrum antibiotics with bactericidal action, and is used in many countries, although it has bitter taste, unpleasant odour and side effects of irritating gastric mucosa, nausea, penicillin allergy, etc. For the improvement of such side effects of pivampicillin hydrochloride, microcapsules, with wall of ethylcellulose, have been prepared by coacervation method. The shape was observed through the scanning electron microscope, the release of the drug into an aqueous medium was studied and the effects of core: ethylcellulose ratio were interpreted as well as making sensory evaluation of taste and odour. There was decreasing trend in dissolution rate of the drug with the increase of core: ethylcellulose ratios, and the smaller microcapsules released their contents more rapidly. A linear relationship was established between the amount of ethylcellulose and the time for 60% release of the drug, and the release pattern was found to have similar characteristics to the release of the drug from an insoluble porous matrix. The release of the drug in the artificial intestinal fluids (pH 6.8) was found to be similar to that in water, while the release in the artificial gastric juice (pH 1.2) was slightly slower. Bioavailability of microcapsule was compared with that of pivampicillin hydrochloride in rabbits using serum concentration and urinary excretion measurements. Microcapsule gave showed slightly higher serum level than pivampicillin hydrochloride from 2 hours after administration, while no significant difference was observed in the accumulated urinary excretion rate between pivampicillin hydrochloride and microcapsule. The ulcer index of pivampicillin hydrochloride administered group was 2.6, and microcapsule administered group was 1.5, while control group was 0.8. Therefore it may be concluded that microencapsulation of pivampicillin hydrochloride is a useful pharmaceutical approach to protect the gastrointestinal tract from being injured by direct contact of pivampicillin hydrochloride without any significant difference of bioavailability.

• Microbiology and Biotechnology Letters
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• v.30 no.4
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• pp.359-366
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• 2002

Bacillus polyfermenticus SCD which is commonly called as Bisroot strain is being used for functional foods through the treatment of long-term intestinal disorders, since the live strains in the form of active endospores can successfully reach the target intestine in humans. The cells of B. polyfermenticus SCD were treated for 4h in artificial gastric juice (pH 2.0,3.0) and bile acid. Final viability of the strain in artificial gastric Juice (pH 2.0, 3.0) is reached to 62.8% and 81.2% respectively B. polyfermenticus SCD is resistant to antibiotics such as streptomycin, rifampicin, nystatin and ampicilin. B. polyfermenticus SCD is well known supplies the nutrients by synthesizing vitamin $B_1$, $B_2$, C and K. B. polyfermenticus SCD produces various digestive enzymes and the enzymes enable to completely digest diets in our body. Above all, $\alpha$-amylase and pretense activities are very higher than B. subtilis KCTC 1020, about two fold and twenty five fold respectively. B. polyfermenticus SCD is very stable during long-term storage period in phosphate buffers of wide-range pH, solutions of various concentrations of sodium chloride, 5% glucose solution and water.

• Journal of Pharmaceutical Investigation
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• v.26 no.1
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• pp.1-11
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• 1996

Biphenyldimethyldicarboxylate (PMC), which has been used to treat hepatitis, is insoluble in water, therefore it has low bioavailability after oral administration. For the purpose of increasing the dissolution rate of PMC, the physical mixtures and inclusion complexes of PMC and $dimethyl-{\beta}-cyclodextrin\;(DM\;{\beta}CD)\;or\;hydroxypropyl-{\beta}-cyclodextrin\;(HP{\beta}CD)$ in molar ratio of 1 : 1 and 1 : 2 were prepared by solvent evaporation method. Mixed micelles of PMC were prepared by reacting PMC with bile salts [sodium cholate(NaC), sodium glycocholate (NaGC)] and oleic acid (OA) or palmitoylcarnitine chloride(PCC). Chloroform/water partition coefficient (PC) of PMC was 36.14 in artificial gastric juice (AGJ) and 33.47 in artificial intestinal juice (AIJ), respectively, on the other hand octanol/water PC was 63.36. PMC formulation was prepared by reacting PMC with PEG400-glycerin system(95 : 5, 90 : 10, respectively) and PEG400-PEG4000-glycerin system (70 : 25 : 5, 65 : 25 : 10, respectively). Dissolution test was performed in AGJ and AIJ by paddle method at $37{\pm}0.5^{\circ}C$. The dissolution rates of PMC tablets on the market were 5.74% and 8.26% at AGJ and AIJ, respectively and marketed PMC capsules were 22.14% and 28.64% at AGJ and AIJ, respectively. The dissolution rates of inclusion complexes of PMC with $DM{\beta}CD$ and $HP{\beta}CD$ in a molar ratio of 1 : 1 were more fast than those of corresponding physical mixtures. The decreasing order of dissolution rates was as follows; PMC-PEG400-PEG4000-glycerin formulation > PMC-PEG400-glycerin formulation > mixed micelles > CD inclusion complexes. The dissolution rates of PMC-PEG400-glycerin and PMC-PEG400-PEG4000-glycerin formulation were most fast and the percentage of dissolution was almost 100% within 20 minutes. And their dissolution rates after 120 minutes were markedly increased as compared with capsules on the market (4.0-fold and 3.2-fold in PMC-PEG400-glycerin formulation at AGJ and AIJ, respectively, and 4.8-fold and 3.7-fold in PMC-PEG400-PEG4000-glycerin formulation at AGJ and AIJ, respectively).

• Korean Journal of Food Science and Technology
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• v.33 no.5
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• pp.567-573
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• 2001

Lactobacilli have been generally recognized as an important lactic acid bacteria present in the normal human intestinal flora. Fifty two Lactobacillus isolates were recovered from the feces of healthy Koreans whose age ranged from thirteen days after birth to 37 years. Among the isolates above, 17 isolates were tentatively identified as strains of Lactobacillus acidophilus and 3 isolates as strains of Lactobacillus casei. For their characterization, these twenty isolates were subjected to the experiments for the resistance to the artificial gastric juice, pH2.5 and bile salt. Interestingly, 3 strains survived pH 2.5 after 3 hour incubation in the artificial gastric juice with more than 75% of survival rate. L. acidophilus a-4 had the highest survival rate of 100%. Four strains including L. acidophilus a-3 grew gradually in MRS broth in the presence of the artificial bile salt. Cholesterol assimilation was also tested for the 20 isolates. The result showed that cholesterol concentration of the medium was reduced by 10 Lactobacillus isolates with more than 60%, as compared to the control. L. acidophilus a-2 had the highest reduction rate of 77%. Judging from these data obtained in vitro, some isolates ware likely to reach the lower small intestine after consumption without a significant loss of viability, suggesting that they had the potential to be developed as a probiotic culture which might lower the cholesterol level in human.

• Journal of the Korean Applied Science and Technology
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• v.37 no.6
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• pp.1535-1544
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• 2020

The primary objective of this study was to isolate and identify amine oxidase-producing probiotic Bacillus strains from traditional fermented soybean paste. Biogenic amines (BA)-forming bacteria isolated from the samples were identified as Bacillus sp. TS09, Bacillus licheniformis TS17, Bacillus subtilis TS19, Bacillus cereus TS23, Bacillus sp. TS30, Bacillus megaterium TS31, B. subtilis TS44, Bacillus coagulans TS46 and Bacillus amyloliquefaciens TS59. Meanwhile, B. subtilis TS04 and TS50 isolated from the same samples exhibited good probiotic properties, including the tolerance to artificial gastric juice and bile salts, the adhesion to intestinal epithelial cells, and the production of bacteriocin(s) active against BA-forming bacteria (Bacillus sp. TS30 and B. subtilis TS44). In addition, the amine oxidase produced by B. subtilis TS04 and TS50 significantly decreased the formation of BA, especially cadaverine, putrescine, and tyramine, therefore, these strains could be considered good potential probiotic candidates to prevent or reduce BA accumulation in food products.

• Journal of the Korean Society of Food Science and Nutrition
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• v.43 no.5
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• pp.749-755
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• 2014

Exopolysaccharides (EPSs) have been widely used in the food industry as viscofying, stabilizing, and emulsifying agents as well as in the pharmaceutical industry for their immunomodulatory, anti-tumor, and anti-inflammatory effects. A total of 458 lactic acid bacteria (LAB) strains isolated from several kinds of soybean pastes were screened for the production of homo-EPS (HoPS). LAB isolates were primarily screened using thin layer chromatography (TLC) and further screened polymerase chain reaction (PCR) targeting genes involved in HoPS production. Six LAB isolates producing high amounts of HoPS were identified by TLC. Among these isolates, glucansucrase gene was amplified in two strains (JSA57, JSB22), whereas the fructansucrase gene was detected in three strains (JSA57, JSB22, JSB66). After isolating the strains, their morphological characteristics and 16S rDNA sequences were determined. Six species were identified as L. alimentarius HSB15, L. plantarum JSA22, L. pentosus JSA57, L. brevis JSB22, L. alimentarius JSB66, and L. parabrevis JSB89. To evaluate the potential probiotic properties of these LAB, their survival rates against a simulated intestinal environment were determined. After 2 hr of incubation in artificial gastric juice, survival rates of JSA57, JSB90, JSB22, and JSB66 were all greater than 50%. After 2 hr of incubation in bile juice, viable cell count of JSB22 was similar with initial vial cell counts. Growth of the six LAB was screened in arabino-oligosaccharide (AOS)-containing MRS broth. Results showed that growth of the isolates selectively increased after culture in AOS-containing media. Strain JSB22 (6 hr), JSB66 (6 hr), HSB15 (20 hr), and JSA22 (29 hr) showed maximum growth rate. Especially, JSB22 showed the highest growth rate. These results suggest that EPS-producing LAB isolated from Deonjang could be applied as synbiotics.

• Korean Journal of Food Science and Technology
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• v.34 no.1
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• pp.73-78
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• 2002

Bacillus polyfermenticus SCD, which is commonly called as Bisroot strain, is being used for functional foods through the treatment of long-term intestinal disorders, since the live strains in the form of active endospores can successfully reach the target intestine in both humans and animals. The cells of B. polyfermenticus SCD were treated for 24 h in artifical bile after incubation for 2 h in artificial gastric juice and final number of the strain was reached to around $3.3{times}10^7\;CFU/mL$. In test of API ZYM kit, ${\beta}-glucuronidase$ or ${\beta}-glucosidase$ was not produced by B. polyfermenticus SCD. B. polyfermenticus SCD was resistant to antibiotics, such as nisin, streptomycin, tetracycline, and rifamycin. B. polyfermenticus SCD was also affected by alcohol concentration up to 4%, but more than 8%, their growth was not affected significantly. Finally, B. polyfermenticus SCD was shown to inhibit the growth of Listeria monocytogenes ATCC 19111 completely within 24 h of incubation, which indicated its bactericidal nature.