• Natural Product Sciences
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• v.29 no.2
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• pp.98-103
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• 2023

Sphaeranthus africanus is commonly used as a traditional remedy for sore throats and pain treatment in Vietnam. The aerial parts have been studied for its anti-inflammatory and anti-proliferative properties. However, the antioxidant and antidiabetic potential of the plant has not been explored. In this work, hydrophilic extracts of the plant's aerial parts were prepared in order to investigate its antioxidant and anti-diabetic properties. Also, the cytotoxicity of the root was evaluated and compared to that of the aerial parts. All of the extracts inhibited lipid peroxidation with IC₅₀ values ranging from 2.05 to 3.56 ㎍/mL, indicating substantial antioxidant activity. At an IC₅₀ value of 4.80 ㎍/mL, the 50% ethanol extract exhibited the most potent inhibition of α-glucosidase. The cytotoxic activity of root extracts is 2 to 5-fold less than that of the aerial parts. Nevertheless, dichloromethane and ethyl acetate extracts of the root demonstrated a selective effect on leukemia cells, with no harm towards the normal HEK-293 cell line. This work provides a scientific support for the antioxidant and antidiabetic activity of the plant. Hence, it may find a promising material for the development of novel antioxidant and antidiabetic agents. More research can be conducted on the phytochemistry and anticancer activities of the plant's root.

• Toxicological Research
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• v.32 no.3
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• pp.225-230
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• 2016

Zingiber officinale Roscoe has been widely used as a folk medicine to treat various diseases, including cancer. This study aims to re-examine the therapeutic potential of co-administration of natural products and cancer chemotherapeutics. Candidate material for this project, ${\alpha}$-zingiberene, was extracted from Zingiber officinale Roscoe, and ${\alpha}$-zingiberene makes up $35.02{\pm}0.30%$ of its total essential oil. ${\alpha}$-Zingiberene showed low $IC_{50}$ values, $60.6{\pm}3.6$, $46.2{\pm}0.6$, $172.0{\pm}6.6$, $80.3{\pm}6.6$ (${\mu}g/mL$) in HeLa, SiHa, MCF-7 and HL-60 cells each. These values are a little bit higher than $IC_{50}$ values of general essential oil in those cells. The treatment of ${\alpha}$-zingiberene produced nucleosomal DNA fragmentation in SiHa cells, and the percentage of sub-diploid cells increased in a concentration-dependent manner in SiHa cells, hallmark features of apoptosis. Mitochondrial cytochrome c activation and an in vitro caspase-3 activity assay demonstrated that the activation of caspases accompanies the apoptotic effect of ${\alpha}$-zingiberene, which mediates cell death. These results suggest that the apoptotic effect of ${\alpha}$-zingiberene on SiHa cells may converge caspase-3 activation through the release of mitochondrial cytochrome c into cytoplasm. It is considered that anti-proliferative effect of ${\alpha}$-zingiberene is a result of apoptotic effects, and ${\alpha}$-zingiberene is worth furthermore study to develop it as cancer chemotherapeutics.

• Korean Journal of Materials Research
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• v.20 no.6
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• pp.331-337
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• 2010

A highly porous Biphasic Calcium Phosphate (BCP) scaffold was fabricated by the sponge replica method with a microwave sintering technique. The BCP scaffold had interconnected pores ranging from $80\;{\mu}m$ to $1000\;{\mu}m$, which were similar to natural cancellous bone. To enhance the mechanical properties of the porous scaffold, infiltration of polycaprolactone (PCL) was employed. The microstructure of the BCP scaffold was optimized using various volume percentages of polymethylmethacrylate (PMMA) for the infiltration process. PCL successfully infiltrated into the hollow space of the strut formed after the removal of the polymer sponge throughout the degassing and high pressure steps. The microstructure and material properties of the BCP scaffold (i.e., pore size, morphology of infiltrated and coated PCL, compressive strength, and porosity) were evaluated. When a 30 vol% of PMMA was used, the PCL-BCP scaffold showed the highest compressive strength. The compressive strength values of the BCP and PCL-BCP scaffolds were approximately 1.3 and 2MPa, respectively. After the PCL infiltration process, the porosity of the PCL-BCP scaffold decreased slightly to 86%, whereas that of the BCP scaffold was 86%. The number of pores in the $10\;{\mu}m$ to $20\;{\mu}m$ rage, which represent the pore channel inside of the strut, significantly decreased. The in-vitro study confirmed that the PCL-infiltrated BCP scaffold showed comparable cell viability without any cytotoxic behavior.

• Food Science and Biotechnology
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• v.17 no.5
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• pp.983-989
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• 2008

Two flavonoids, isorhamnetin 3-O-$\beta$-D-glucopyranoside (1) and quercetin 3-O-$\beta$-D-glucopyranoside (2), from slander glasswort (Salicornia herbacea, Korean name hamcho) were isolated. Antioxidative and matrix metalloproteinase-9(MMP-9) inhibitory effects of these compounds were investigated in HT 1080 cell lines. These compounds suppressed the electron spin resonance (ESR) signal intensity on generation of 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical in a free-cellular system. Their scavenging effects on generation of intercellular reactive oxygen species (ROS) also exhibited similar trends with DPPH radical in the free cellular system. Also, a control group combined only with Fe(II)-$H_{2}O_2$ resulted in DNA apoptosis by oxidative stress, whereas treatments with these compounds suppressed radical-mediated DNA damage. Intracellular glutathione (GSH) levels were slightly increased in the presence of compound 1 and 2. Moreover, these compounds led to the reduction of the expression levels of MMP-9 without cytotoxic influence. These results suggest that these compounds have a potential as a valuable natural antioxidant and MMP inhibitor related to oxidative stress. Therefore, these compounds not only can be developed as a candidate for a therapeutic potential but also a source for use as ingredients of health foods or functional foods to prevent metastasis involving MMP-9, closely related to ROS.

• Journal of Physiology & Pathology in Korean Medicine
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• v.19 no.1
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• pp.124-129
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• 2005

Resveratrol, a phytoalexin found at high levels in grapes and in grape products such as red wine, has been reported to possess a wide range of biological and pharmacological activities including anti-oxident, anti-inflammatory, anti-mutagenic, and anti-carcinogenic effects, but its molecular mechanism is poorly understood. In this study, we examined the effects of resveratrol on lipopolysaccharide (LPS)-induced growth inhibitory activity and cell growth-regulatory gene products in astroglioma C6 cells to elucidate its possible mechanism for anti-cytotoxicity. It is shown that LPS induced time-dependent growth inhibition and morphological changes of C6 cells, which were recovered by pre-treatment with resveratrol. The anti-proliferative effect of LPS was associated with the induction of tumor suppressor p53 and cyclin-dependent kinase (Cdk) inhibitor p21 (WAF1/CIP1) expression assessed by RT-PCR and Western blot analysis in time-dependent manner in C6 cells. In addition, the pro-apoptotic Bax expression was also up-regulated in LPS-treated C6 cells without alteration of anti-apoptotic Bcl-2 and Bcl-XL expression. However, resveratrol significantly inhibited LPS-induced p53, p21 and Bax levels, suggesting that the modulation of p53, p21 and Bax levels could be one of the possible pathways by which resveratrol functions as anti-cytotoxic agent.

• Biomolecules & Therapeutics
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• v.16 no.3
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• pp.270-276
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• 2008

In this study we investigated the effects of Magnolia Bark (MB) extract and its constituents, such as honokiol and magnolol, on gastritis in rats and the growth of human gastric cancer cells. The MB extract, honokiol, and magnolol showed the acid-neutralizing capacities, the antioxidant activities, and the inhibitory effect on the growth of Helicobacter pylori (H. pylori.) at the dose of $50\;{\mu}g/ml$ and over, which is equivalent to that of ampicillin ($100\;{\mu}g/ml$). Honokiol and magnolol had no significant cytotoxicity to human gastric caner cells (AGS and SNU638). However, the MB extract had cytotoxic activity against AGS gastric cancer cell. The MB extract, honokiol, and magnolol significantly inhibited HCI-ethanol-induced gastric lesions without clear change of mucus content. In pylorus ligated rats, honokiol significantly decreased the volume of gastric secretion and gastric acid output, and increased the pH. Magnolol increased the mucus content to almost the same as the control group at oral doses of 50 mg/kg. Therefore, we could guess that antigastritic action of honokiol and magnolol may be associated with the antioxidant activities, acid-neutralizing capacities, inhibition of secretion in gastric acid, and anti-H. pylori action. From these results, we could suggest that MB extract and its constituents, such as honokiol and magnolol, may be useful for the treatment and/or protection of gastritis.

• Natural Product Sciences
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• v.10 no.6
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• pp.268-271
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• 2004

In order to examine their effects on the P-glycoprotein (P-gp) activity in human breast cancer cells, MCF-7/ADR, one hundred Indonesian plant extracts were screened. Among them, the five chloroform extracts of Calotropis gigantea, Curcuma aeruginosa, Merremia mammosa, Sindora sumatrana, and Zingiber cassumunar, showed the most potent P-gp inhibitory activity. When each of these extracts was treated together with the anticancer agent, daunomycin, they increased the cytotoxic activity of daunomycin up to $IC_{50}$ values of less than $6.62\;{\mu}M$, which is a value with a positive control, verapamil. Also, other 15 plant extracts exhibited significant P-gp inhibitory activity with $IC_{50}$ values between 6.62 and $13.20\;{\mu}M$. These prospective samples will be subjected to further laboratory phytochemical investigation to find active principles.

• Journal of Microbiology and Biotechnology
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• v.16 no.8
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• pp.1262-1268
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• 2006

In the search for a novel cytotoxic substance from medicinal plants, HY53 ($C_{17}H_{32}O_2N_2$; molecular weight 296) was isolated from the leaves of Pata de Vaca (Bauhinia forficata). The growth of the HepG2 cells was inhibited in a dose-dependent manner when treated with 0.07 to 0.40 mM HY53 for 24 h (IC$_{50}$: 0.13 mM). Furthermore, nuclear DAPI staining revealed the typical nuclear features of apoptosis in the HepG2 cells exposed to 0.27 mM HY53, whereas a flow cytometric analysis of the HepG2 cells using propidium iodide showed that the apoptotic cell population increased gradually from 8% at 0 mM to 23% at 0.14 mM and 45% at 0.40 mM after being exposed to each concentration of HY53 for 24 h. Moreover, a TUNEL assay also exhibited the apoptotic induction of the HepG2 cells treated with HY53. To obtain further information on the HY53-induced apoptosis, the expression level of certain apoptosis-associated proteins was examined using a Western blot analysis. Treatment of the HepG2 cells with HY53 resulted in the activation of caspase-3, and subsequent proteolytic cleavage of poly(ADP-ribose) polymerase (PARP). Consequently, the results confirmed that the apoptosis in the HepG2 cells was induced by HY53 and the involvement of caspase-3-mediated PARP cleavage in the apoptotic process.

• Journal of Microbiology and Biotechnology
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• v.30 no.8
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• pp.1184-1194
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• 2020

Melanin is a major factor that darkens skin color as one of the defense systems to prevent the harmful effects of UV light. However, darkened skin from the localized or systemic accumulation of melanin is viewed in many cultures as an esthetic problem. Consequentially, searching for anti-melanogenic agents from natural sources is very popular worldwide. Previous screening of fermented rice products, obtained from various rice cultivars fermented with different sources of loog-pang (Thai traditional fermentation starter), revealed that the highest ability to reduce the melanin content in B16F10 melanoma cells was from unpolished black rice fermented with a defined starter mixture of microbes isolated from loog-pang E11. The aim of this study was to investigate the mechanism of the fermented unpolished black rice (FUBR) on the inhibition of melanogenesis in B16F10 melanoma cells. The strongest reduction of cellular melanin content was found in the FUBR sap (FUBRS). The melanin reduction activity was consistent with the significant decrease in the intracellular tyrosinase activity. The FUBRS showed no cytotoxic effect to B16F10 melanoma or Hs68 human fibroblast cell lines. It also significantly reduced the transcript and protein expression levels of tyrosinase, tyrosinase-related protein 1 (TYRP-1), TYRP-2, and microphthalmia-associated transcription factor. Furthermore, it induced a significantly increased level of phosphorylated ERK, p38 and Akt signaling pathways, which likely contributed to the negative regulation of melanogenesis. From these results, a model for the mechanism of FUBRS on melanogenesis inhibition was proposed. Moreover, these results strongly suggested that FUBRS possesses anti-melanogenesis activity with high potential for cosmeceutical application as a skin depigmenting agent.

• THE JOURNAL OF KOREAN ORIENTAL ONCOLOGY
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• v.1 no.1
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• pp.167-190
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• 1995

Bikiwhan is one of the oriental medicines that have been used for the treatment of tumors since ancient times. However, the mechanism of the drug action is not closely surved. This study was made to investigate the effects of Bikiwhan on the innate immunity were analysed by measuring the functions of phagocytes, and those of specific immunity were analysed by measuring T and B cells activities. The followings are the results obtained from this study : 1. Bikiwhan has direct cytotoxic effects against human lymphoma cell lines (K562) in a dose dependent manner. 2. An administration of Bikiwhan increased allogenic immune response in the mouse. 3. An administration of Bikiwhan increased the antibodies formation against SRBC. 4. An administration of Bikiwhan enhanced the apperance of rosette forming cells in the spleen. 5. An administration of Bikiwhan decreased the delayed-type hypersensitivity against dinitrofluorobenzene. 6. An administration of Bikiwhan has no effect on natural killer cells. 7. Bikiwhan increased the phagocyte activity of peritoneal macrophages in vitro and in in vivo as well. 8. Bikiwhan depressed the formation of reactive oxygen intermediated in vitro and in vivo as well. 9. Bikiwhan has the capacity to make peritoneal macrophages secrete nitric oxide. The above results demonstrate that Bikiwhan has enhancing effects of immune responses against tumors by decreasing tissue demages caused by immune responses.