• Title/Summary/Keyword: Anticancer drug

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Flavonoids: An Emerging Lead in the P-glycoprotein Inhibition

  • Gadhe, Changdev G.;Cho, Seung Joo
    • Journal of Integrative Natural Science
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    • v.5 no.2
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    • pp.72-78
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    • 2012
  • Multidrug resistance is a major obstacle in cancer chemotherapy. Cancer cells efflux chemotherapeutic drug out of cell by means of transporter and reduce the active concentration of it inside cell. Such transporters are member of the ATP binding cassettes (ABC) protein. It includes P-gp, multiple resistant protein (MRP), and breast cancer resistant protein (BCRP). These proteins are widely distributed in the human cells such as kidney, lung, endothelial cells of blood brain barrier etc. However, there are number of drugs developed for it, but most of them are getting transported by it. So, still there is necessity of a good modulator, which could effectively combat the transport of chemotherapeutic agents. Natural products origin modulators were found to be effective against transporter such as flavonoids, which belongs to third generation modulators. They have advantage over synthetic inhibitor in the sense that they have simple structure and abundant in nature. This review focuses on the P-gp structure its architecture, efflux mechanism, herbal inhibitors and their mechanism of action.

Stability of antineoplaston A10 in Aqueous Solution

  • Oh, In-Joon;Lee, Jeong-Min;Lee, Yong-Bok;Shin, Sang-Chul;Choi, Bo-Gil
    • Archives of Pharmacal Research
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    • v.18 no.2
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    • pp.75-78
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    • 1995
  • The analysis method nad stability test of antineoplaston A10, a new anticancer drug candidate, were established. A10 and phenylacetyl- L-glutamine, one of the degradation products, can be detected by high-performance liquid chromatography. The degradation kinetics of antineoplaston A10 in aqueous solutions from pH 1 to 10 buffers were carried out at 40, 50 and 60.deg.C. Pseudo-first order kinetics were obtained throughout the entire pH ranges studied. The pH-rate profiles showed that antineoplaston A10 was very unstable in alkaline conditions and most stable at pH 4.

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Zingiber officinale: A Simple Spice with Health Benefits & Some Modern Researches

  • Abbasi, Hana;Khatoon, Rizwana;Kabir, Hifzul
    • CELLMED
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    • v.9 no.2
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    • pp.3.1-3.5
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    • 2019
  • Zingiber officinale is a spice which is having a strong historical medicinal background and used by different systems of medicine for various ailments. It is also used to maintain the characteristic sharpness and tangy essence of food and beverages and used in carbonated drinks, as a conserve in sugar syrup. Ginger considered as an incredible drug for inflammation, gastrointestinal problems, pain and sexual problems since centuries. There are many studies carried out in recent years, which proves that the active constituents of ginger shows a variety of pharmacological effects like antiemetic, hepatoprotective, anti hyperlipidemic and antibacterial. The most momentous among all the nutraceutical aspects of ginger are its positive control on gastrointestinal tract including digestive stimulant action, anticancer effect and anti-inflammatory effect.

Crystallization and preliminary X-ray analysis of API5-FGF2 complex

  • Bong, Seoung Min;Lee, Byung Il
    • Biodesign
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    • v.6 no.4
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    • pp.92-95
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    • 2018
  • API5 is a unique oncogenic, non-BIR type IAP nuclear protein and is up-regulated in several cancers. It exerts several functions, such as apoptosis inhibition, cell cycle progression, cancer immune escape, and anticancer drug resistance. Although structural studies of API have revealed that API5 mediates protein-protein interactions, its detailed molecular functions remain unknown. Since FGF2 is one of API5's major interacting proteins, structural studies of the API5-FGF2 complex will provide insight into both proteins' molecular function. We overexpressed and purified API5 and FGF2 in Escherichia coli and crystallized the API-FGF2 complex using polyethylene glycol (PEG) 6000 as a precipitant. Diffraction data were collected to a $2.7{\AA}$ resolution using synchrotron X-rays. Preliminary diffraction analysis revealed that the API5-FGF2 complex crystal belongs to the space group $P2_12_12_1$ with the following unit cell parameters: a = 46.862, b = 76.523, $c=208.161{\AA}$. One asymmetric unit with 49.9% solvent contains one API5-FGF2 complex. Molecular replacement calculation, using API5 and FGF2 coordinates, provided a clear electron density map for an API5-FGF2 complex.

Induction of cell death by 2,4,3',5'-tetramethoxystilbene in human acute promyelocytic leukemia (HL-60) cells and its mechanism.

  • Lee, Sang-Kwang;Kim, Mie-Young;Chun, Young-Jin
    • Proceedings of the PSK Conference
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    • 2003.10b
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    • pp.149.1-149.1
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    • 2003
  • We have previously shown that 2,4,3',5'-tetramethoxystilbene (TMS), a synthetic trans-stilbene analogue, is one of the most potently selective inhibitor of human cytochrome P450 1B1 in vitro and in vivo. In the present studies, the apoptotic effects of TMS were investigated in HL-60 cells. The effects of TMS on the proliferation of HL-60 cells were determined with MTT assay. TMS exhibited cytotoxicity with an $IC_50$ value of 37 nM. Cotreatment with TMS and etoposide, a well-known anticancer drug significantly enhanced the cytotoxicity. (omitted)

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Modulation of P-glycoprotein Activity by Flavonoids and Organic Isothiocyanates in Human Uterine Cells.

  • Chung, Soo-Yeon;Go, Eun-Jung;Lee, Hwa-Jeong
    • Proceedings of the PSK Conference
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    • 2003.10b
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    • pp.231.2-231.2
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    • 2003
  • One of the possible mechanisms of multi-drug resistance found in cancer cells is the over-expression of P-glycoprotein (P-gp). Studies have shown that compounds found in plants including vegetables and fruits not only have anticancer activities but may also modulate P-gp activity. The effect of flavonoids and organic isothiocyanates on P-gp activity was studied in human uterine sarcoma cell lines, MES-Sa (sensitive) and MES-SD/DX5 (resistant). The accumulation of daunomycin (DNM), a P-gp substrate, was approximately 10 times greater in the sensitive cell as compared to the resistant cells over the entire time course (up to 2 hrs). (omitted)

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Chemotherapy of Mammary Comedocarcinoma with Doxorubicin in a Dog

  • Kim, Yeonsoo;Seo, Kyoungwon;Song, Kunho
    • Journal of Veterinary Clinics
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    • v.38 no.6
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    • pp.274-278
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    • 2021
  • An 11-year-old, intact female, Miniature Poodle presented with an abdominal mass. The abdominal mass was located around the right fifth mammary gland. The surgically removed mammary mass was subjected to histopathological examination. Based on the microscopic interpretation, a final diagnosis of an intermediate grade infiltrative mammary comedocarcinoma was established. Computed tomography for metastasis evaluation after surgical resection of the tumor showed enlarged right medial iliac and right inguinal lymph nodes, and a micronodule in the accessory lung lobe, suggesting metastasis of the mammary gland tumor. Doxorubicin, a chemotherapeutic drug, was administered six times at three week intervals. However, despite chemotherapy, the masses around the fourth and fifth mammary gland on the right side enlarged in size, and the treatment was discontinued at the request of the owner. The anticancer response to mammary comedocarcinoma is poor and the patient is in hospice management. This is the first attempt to treat a case of canine mammary comedocarcinoma in South Korea.

Analgesic Effect of Poria cocos Extract on a Rat Model of Adjuvant-induced Arthritis

  • Lee, Gil-Hyun;Yoon, Hae-Gyung;Choi, Go-Eun;Hyun, Kyung-Yae
    • Biomedical Science Letters
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    • v.28 no.2
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    • pp.137-144
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    • 2022
  • Poria cocos is a natural substance known to have anticancer, antioxidant and anti-inflammatory effects. The aim of this study is to investigate the analgesic effects of Poria cocos extract (PCE). We evaluated the analgesic effects of PCE using adjuvant induced arthritis rat model. Male SD rats were administered intra-orally with PCE according to prescribed dosage, during 6 days. After 6 days later, serum TNF-α, IL-1β, and IL-6 levels were measured by ELISA. In our experiment, administration of PCE decreased TNF-α, IL-1β, IL-6 and PGE2 level in serum. Furthermore, it was confirmed that allodynia was relieved in evaluation of pain behavior. It was confirmed that administration of PCE reduces nociceptive pain by reducing nociceptive stimuli by acting as an anti-inflammatory drug.

Stress granules dynamics: benefits in cancer

  • Jeong In, Lee;Sim, Namkoong
    • BMB Reports
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    • v.55 no.12
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    • pp.577-586
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    • 2022
  • Stress granules (SGs) are stress-induced subcellular compartments, which carry out a particular function to cope with stress. These granules protect cells from stress-related damage and cell death through dynamic sequestration of numerous ribonucleoproteins (RNPs) and signaling proteins, thereby promoting cell survival under both physiological and pathological condition. During tumorigenesis, cancer cells are repeatedly exposed to diverse stress stimuli from the tumor microenvironment, and the dynamics of SGs is often modulated due to the alteration of gene expression patterns in cancer cells, leading to tumor progression as well as resistance to anticancer treatment. In this mini review, we provide a brief discussion about our current understanding of the fundamental roles of SGs during physiological stress and the effect of dysregulated SGs on cancer cell fitness and cancer therapy.

Physico-phytochemical Evaluation of Raw Material and CO2 extract of Fruits of Terminalia chebula

  • Chandil, Shachi;Bamoriya, Harikishan
    • CELLMED
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    • v.12 no.1
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    • pp.4.1-4.13
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    • 2022
  • The present communication attempts to evaluate the physicochemical and preliminary phytochemical studies on the fruit of Terminalia chebula Retz. Combretaceae family. Haritaki is one of the most celebrated herbs in the Indian traditional medicine system, Ayurveda. Terminalia chebula is known to exhibit different properties like anticancer, anti-inflammatory, anti-protozoal, antimicrobial, antioxidant, hepato and renal protective activities, and in the management of metabolic syndrome. As there is no detailed standardisation work reported on fruit, the physicochemical parameters, preliminary phytochemical constants, heavy metals, analysis are carried out. The phytochemical screening indicated the presence Tannin, Alkaloid, Phenol, Carbohydrate, Steroids, Protein and Resin compounds in CO2 extract of Haritaki. The present investigation will helpful in assessing the quality and purity of a crude drug. Thus, the study provides facts that CO2 extract of Haritaki contains medicinally important bioactive phytochemical compounds which justifies the use of plant species as conventional medicine for treatment of many diseases.