• 한방비만학회지
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• 제11권2호
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• pp.41-68
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• 2011

Objectives: After organizing segmentations related to obesity from classics and each studies, we would like to examine the value of wild ginseng, bovis calculus, ursi fel and moschus as a obesity medicine. Methods: We found out 4 drugs which are wild ginseng, bovis calculus, ursi fel and moschus from the classics, such as "Shin-Nong-Bon-Cho-Kyung", "Myoung-Eui-Byul-Lok", "Bon-Cho-Gang-Mok", "Bon-Cho-Jong-Shin", "Bon-Cho-Bi-Yo", "Bon-Cho-Gu-Jin" and "Deuk-Bae-Bon-Cho", we searched websites such as RISS, Korean traditional knowledge portal, the society of Korean medicine for obesity research, Korean pharmacopuncture institute, the Korean academy of oriental rehabilitation medicine and Korean acupuncture & moxibustion society as well. Results: 1. We couldn't find the contents related to the efficacy of improving obesity through wild ginseng, bovis calculus, ursi fel and moschus from the classics. 2. Wild ginseng had a study dealing with the efficacy of anticancer, obesity, toxicity, immunity, sulfation, diabetes, plasma proteins, depression, hypertension, endometriosis and hair loss. Especially among 6 studies related to obesity, apart from the study that treated extract of wild ginseng directly to the cell or oral administration to the animals, also have studies that had an efficacy of improving obesity through injecting pharmacopuncture to acupuncture point and vein, etc. 3. Bovis calculus had a study about efficacy related to arthritis, liver, inflammation of cornea, obesity, anticancer, immunity, antacid, heart, lumbar pain, hypertension, toxicity, a digestive organ and sasang constitution, especially in case of obesity, had each studies about oral administration of complex prescription and about cell unit experiment of pharmacopuncture. 4. Ursi fel had a study about efficacy related to liver, arthritis, inflammation of cornea, immunity, obesity, anticancer, antacid, lumbar pain, digestive organ, toxicity, cell protection, skin ailment, etc. Especially in case of obesity, had each studies about oral administration of animal experiment and about cell unit experiment of pharmacopuncture. 5. Moschus had a study about efficacy related to liver, the central nervous system, arthritis, inflammation of cornea, immunity, obesity, anticancer, hypertension, heart, lumbar pain, etc. Especially in case of obesity, had one study about oral administration of complex prescription. Conclusion: Through the result of probability as a obesity medicine of wild ginseng, bovis calculus, ursi fel and moschus, we could identify the possibility of each drug as a obesity medicine. Also in the future, it is considered that studies about one or complex prescription and pharmacopuncture as a obesity medicine will be needed.

• The Korean journal of internal medicine
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• 제33권6호
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• pp.1182-1193
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• 2018

Background/Aims: Elderly patients (${\geq}80years$) with colorectal cancer (CRC) tend to avoid active treatment at the time of diagnosis despite of recent advances in treatment. The aim of this study was to determine treatment propensity of elderly patients aged ${\geq}80years$ with CRC in clinical practice and the impact of anticancer treatment on overall survival (OS). Methods: Medical charts of 152 elderly patients (aged ${\geq}80years$) diagnosed with CRC between 1998 and 2012 were retrospectively reviewed. Patients' clinical characteristics, treatment modalities received, and clinical outcome were analyzed. Results: Their median age was 82 years (range, 80 to 98). Of 152 patients, 148 were assessable for the extent of the disease. Eighty-two of 98 patients with localized disease and 28 of 50 patients with metastatic disease had received surgery or chemotherapy or both. Surgery was performed in 79 of 98 patients with localized disease and 15 of 50 patients with metastatic disease. Chemotherapy was administered in only 24 of 50 patients with metastatic disease. Patients who received anticancer treatment according to disease extent showed significantly longer OS compared to untreated patients (localized disease, 76.2 months vs. 15.4 months, p = 0.000; metastatic disease, 9.9 months vs. 2.6 months, p = 0.001). Along with anticancer treatment, favorable performance status (PS) was associated with longer OS in multivariate analysis of clinical outcome. Conclusions: Elderly patients aged ${\geq}80years$ with CRC tended to receive less treatment for metastatic disease. Nevertheless, anticancer treatment in patients with favorable PS was effective in prolonging OS regardless of disease extent.

• 셀메드
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• 제10권2호
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• pp.16.1-16.8
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• 2020

Standardization of drug deals with confirmation of drug identity and determination of drug quality and purity. Unani herbal formulations are used in traditional medicine for the treatment of various diseases. Cancer is a disease which causes abnormal, uncontrolled growth of body tissue or cells, which tend to proliferate in an uncontrolled way. Spread of cancer from site of origin to other organs of the body is called metastasis. It is a hyper proliferative disorder involving, transformation, dysregulation of apoptosis, invasion and angiogenesis. The present study aimed to standardize a classical Unani formulation (CUF) described as anticancer properties. The CUF has been used for anti-cancerous activity (Dāfi'-i-saraṭān) in human population by Unani physicians for centuries. The standardization parameters carried out for classical Unani formulation are pharmacognostical studies, physicochemical parameters, high-performance thin layer chromatography (HPTLC), microbial load, aflatoxins, and heavy metals revealing specific identities and to evaluate Pharmacopoeial standards. Experiment and the data obtained established the Pharmacopoeial standards for this formulation for identification and quality control purpose. The CUF has been successfully standardized and standard operating procedures (SOPs) for its preparation has been laid down which may serve as a standard reference in future. The standardization data of this formulation may be used as a standard guideline for preparation of the formulation in future.

• 약학회지
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• 제36권6호
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• pp.591-597
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• 1992

The organ distribution of $[^3H]$-methotrexate-lactosaminated bovine serum albumin conjugates ($[^3H]$-MTX-LBSA) was investigated to examine their role as a liver-specific anticancer drug. Synthesis of lactosaminated bovine serum albumin(LBSA) with BSA, lactose and sodium cyanoborohydride through reductive amination was followed by its conjugation with methotrexate (MTX) and 1-ethyl-3-(3-dimethylaminopropyl) carbodiimide hydrochloride (EDC), thereby synthesizing [$[^3H]$-MTX-LBSA conjugates. Organ distribution and plasma elimination profiles were studied in male Wistar rats after intravenous injection of [$[^3H]$-MTX-LBSA conjugates. The fates of $[^3H]$-MTX and the $[^3H]$-MTX-BSA conjugates´fates were also investigated for comparison. The results showed that the plasma level of $[^3H]$-MTX-LBSA conjugates declined more rapidly than those of $[^3H]$-MTX-BSA and their liver concentration was significantly higher than those of other treatment (p<0.01). In addition, their uptake compared to the amount taken up by the liver (1 : 33.1 at 10 min, 1 : 24.1 at 120 min). All these suggested that MTX-LBSA conjugate is one of the drug delivery system (DDS) that is advanced in concentrating MTX in the liver and minimizing the renal toxicity of MTX.

• Biomolecules & Therapeutics
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• 제26권6호
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• pp.591-598
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• 2018

Epigenetic silencing is considered to be a major mechanism for loss of activity in tumor suppressors. Reversal of epigenetic silencing by using inhibitors of DNA methyltransferase (DNMT) or histone deacetylases (HDACs) such as 5-Aza-CdR and FK228 has shown to enhance cytotoxic activities of several anticancer agents. This study aims to assess the combinatorial effects of genesilencing reversal agents (5-Aza-CdR and FK228) and oxaliplatin in gastric cancer cells, i.e., Epstein-Barr virus (EBV)-negative SNU-638 and EBV-positive SNU-719 cells. The doublet combinatorial treatment of 5-Aza-CdR and FK228 exhibited synergistic effects in both cell lines, and this was further corroborated by Zta expression induction in SNU-719 cells. Three drug combinations as 5-Aza-CdR/FK228 followed by oxaliplatin, however, resulted in antagonistic effects in both cell lines. Simultaneous treatment with FK228 and oxaliplatin induced synergistic and additive effects in SNU-638 and SNU-719 cells, respectively. Three drug combinations as 5-Aza-CdR prior to FK228/oxaliplatin, however, again resulted in antagonistic effects in both cell lines. This work demonstrated that efficacy of doublet synergistic combination using DNMT or HDACs inhibitors can be compromised by adding the third drug in pre- or post-treatment approach in gastric cancer cells. This implies that the development of clinical trial protocols for triplet combinations using gene-silencing reversal agents should be carefully evaluated in light of their potential antagonistic effects.

• Journal of Microbiology and Biotechnology
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• 제17권10호
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• pp.1712-1716
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• 2007

To generate new scaffold candidates as highly selective and potent cyelin-dependent kinase (CDK) inhibitors, structure-based drug screening was performed utilizing 3D pharmacophore conformations of known potent inhibitors. As a result, CR229 (6-bromo-2,3,4,9-tetrahydro-carbolin-1-one) was generated as the hit-compound. A computational docking study using the X-ray crystallographic structure of CDK2 in complex with CR229 was evaluated. This predicted binding mode study of CR229 with CDK2 demonstrated that CR229 interacted effectively with the Leu83 and Glu81 residues in the ATP-binding pocket of CDK2 for the possible hydrogen bond formation. Furthermore, biochemical studies on inhibitory effects of CR229 on various kinases in the human cervical cancer HeLa cells demonstrated that CR229 was a potent inhibitor of CDK2 ($IC_{50}:\;3\;{\mu}M$), CDKI ($IC_{50}:\;4.9\;{\mu}M$), and CDK4 ($IC_{50}:\;3\;{\mu}M$), yet had much less inhibitory effect ($IC_{50}:>20\;{\mu}M$) on other kinases, such as casein kinase 2-${\alpha}1$ (CK2-${\alpha}1$), protein kinase A (PKA), and protein kinase C (PKC). Accordingly, these data demonstrate that CR229 is a potent CDK inhibitor with anticancer efficacy.

• Asian Pacific Journal of Cancer Prevention
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• 제16권9호
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• pp.3753-3758
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• 2015

Background: Polymeric nanoparticles are attractive materials that have been widely used in medicine for drug delivery, with therapeutic applications. In our study, polymeric nanoparticles and the anticancer drug, chrysin, were encapsulated into poly (D, L-lactic-co-glycolic acid) poly (ethylene glycol) (PLGA-PEG) nanoparticles for local treatment. Materials and Methods: PLGA: PEG triblock copolymers were synthesized by ring-opening polymerization of D, L-lactide and glycolide as an initiator. The bulk properties of these copolymers were characterized using 1H nuclear magnetic resonance spectroscopy and Fourier transform infrared spectroscopy. In addition, the resulting particles were characterized by scanning electron microscopy. Results: The chrysin encapsulation efficiency achieved for polymeric nanoparticles was 70% control of release kinetics. The cytotoxicity of different concentration of pure chrysin and chrysin loaded in PLGA-PEG ($5-640{\mu}M$) on T47-D breast cancer cell line was analyzed by MTT-assay. Conclusions: There is potential for use of these nanoparticles for biomedical applications. Future work should include in vivo investigation of the targeting capability and effectiveness of these nanoparticles in the treatment of breast cancer.

• Integrative Medicine Research
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• 제3권2호
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• pp.67-73
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• 2014

Background: The transcription factor signal transducer and activator of transcription 3 (Stat3)is constitutively activated in many human cancers. It promotes tumor cell proliferation,inhibits apoptosis, induces angiogenesis and metastasis, and suppresses antitumor hostimmune responses. Therefore, Stat3 has emerged as a promising molecular target for cancertherapies. In this study, we evaluated the Stat3-suppressive activity of 38 herbal medicinestraditionally used in Korea.Methods: Medicinal herb extracts in 70% ethanol were screened for their ability to suppressStat3 in the A549 human lung cancer cell line. A Stat3-responsive reporter assay system wasused to detect intracellular Stat3 activity in extract-treated cells, and Western blot analyseswere performed to measure the expression profiles of Stat3-regulated proteins.Results: Fifty percent of the 38 extracts possessed at least mild Stat3-suppressive activities(i.e., activity less than 75% of the vehicle control). Ethanol extracts of Bupleurum falcatumL., Taraxacum officinale Weber, Solanum nigrum L., Ulmus macrocarpa Hance, Euonymus alatusSieb., Artemisia capillaris Thunb., and Saururus chinensis (Lour.) Baill inhibited up to 75% of thevehicle control Stat3 activity level. A549 cells treated with these extracts also had reducedBcl-xL, Survivin, c-Myc, and Mcl-1 expression.Conclusion: Many medicinal herbs traditionally used in Korea contain Stat3 activity-suppressing substances. Because of the therapeutic impact of Stat3 inhibition, these resultscould be useful when developing novel cancer therapeutics from medicinal herbs.

• Asian Pacific Journal of Cancer Prevention
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• 제15권17호
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• pp.7363-7369
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• 2014

The present study aimed to prepare and evaluate polymeric micelles conjugated with folic acid through ${\alpha}$- or ${\gamma}$-carboxyl groups for antitumor efficacy. The isomeric block copolymers, ${\alpha}$- and ${\gamma}$-folate-polyethyleneglycol-distearoyl phosphatidylethanolamine (${\alpha}$- and ${\gamma}$-Fol-PEG-DSPE), were produced by solid phase peptide synthesis. Three types of doxorubicin (DOX)-loaded polymeric micelles (MPEG-DSPE-DOX and ${\alpha}$- / ${\gamma}$-Fol-PEG-DSPEDOX micelles) were prepared via the film formation method. Compared with MPEG-DSPE-DOX micelles, the ${\alpha}$- / ${\gamma}$-Fol-PEG-DSPE-DOX micelles presented a higher cellular uptake behavior in the live cell study. Cell viability percentages were 81.8%, 57.3%, 56.6% at 2 hours for MPEG-DSPE-DOX, ${\alpha}$- and ${\gamma}$-Fol-PEG-DSPE-DOX micelles, respectively (p<0.05). Using the KB xenograft tumor model, both ${\alpha}$- and ${\gamma}$-folate-conjugated micelles were found to have better antitumor effects with lower toxicity in comparison with MPEG-DSPE-DOX micelles. No difference in in vivo antitumor efficacy was found between ${\alpha}$- and ${\gamma}$-Fol-PEG-DSPE-DOX micelles. The folate-conjugated micelles might be a potentially useful strategy for tumor targeting of therapeutic agents, whether grafting with folic acid through ${\alpha}$- or ${\gamma}$-carboxyl groups.

• 생명과학회지
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• 제33권8호
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• pp.663-679
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• 2023

본 리뷰 논문은 2010년부터 2022년까지의 인공지능을 활용한 신약개발 관련 연구동향을 분석하여 정리하였다. 이러한 분석을 통해 2,421개 연구의 초록을 코퍼스로 구성하고, 전처리를 거쳐 빈도가 높고 연결 중심성이 높은 단어를 추출하였다. 분석 결과 2010-201년과 2020-2022년 단어빈도 추이는 비슷한 것으로 구분되어 나타났다. 연구 방법으로는 2010년부터 2020년까지 머신 러닝을 활용한 연구가 많이 진행되었고, 2021년부터는 딥러닝을 활용한 연구가 증가하고 있다. 이러한 연구를 통해 이루어지고 있는 인공지능 활용연구 동향에 대해 분야별로 살펴보고 관련 연구의 장점, 문제점, 도전과제 등을 살펴보았다. 파악되어진 연구 동향은 2021년 이후로 약물의 재배치를 인공지능 활용 연구, 항암제 개발을 위한 컴퓨터 활용 연구, 임상시험에 인공지능 적용 연구 등과 같이 인공지능 적용 분야가 확대되고 있다는 점이다. 이러한 과정을 통해 향후 이루어질 것으로 예상되는 인공지능 활용 신약개발 연구의 전망에 대해 간략히 제시하였다. 위의 인공지능 기술 발전과 함께 바이오와 의료데이터의 신뢰성과 안전성이 확보되어진다면 인공지능 활용 신약개발의 방향이 개인 맞춤형 의료와 정밀의료 분야로 진행되어질 것으로 판단하기에 이에 대한 지속적인 노력이 필요하리라 본다.