• Genomics & Informatics
• /
• v.19 no.4
• /
• pp.46.1-46.11
• /
• 2021

Moringa oleifera is nowadays raising as the most preferred medicinal plant, as every part of the moringa plant has potential bioactive compounds which can be used as herbal medicines. Some bioactive compounds of M. oleifera possess potential anti-cancer properties which interact with the apoptosis protein p53 in cancer cell lines of oral squamous cell carcinoma. This research work focuses on the interaction among the selected bioactive compounds derived from M. oleifera with targeted apoptosis protein p53 from the apoptosis pathway to check whether the bioactive compound will induce apoptosis after the mutation in p53. To check the toxicity and drug-likeness of the selected bioactive compound derived from M. oleifera based on Lipinski's Rule of Five. Detailed analysis of the 3D structure of apoptosis protein p53. To analyze protein's active site by CASTp 3.0 server. Molecular docking and binding affinity were analyzed between protein p53 with selected bioactive compounds in order to find the most potential inhibitor against the target. This study shows the docking between the potential bioactive compounds with targeted apoptosis protein p53. Quercetin was the most potential bioactive compound whereas kaempferol shows poor affinity towards the targeted p53 protein in the apoptosis pathway. Thus, the objective of this research can provide an insight prediction towards M. oleifera derived bioactive compounds and target apoptosis protein p53 in the structural analysis for compound isolation and in-vivo experiments on the cancer cell line.

• BMB Reports
• /
• v.42 no.12
• /
• pp.806-811
• /
• 2009

Recently, various phenolic acid phenethyl ureas (PAPUs) have been synthesized from phenolic acids by Curtius rearrangement for the development of more effective anti-oxidants. In this study, we examined the anti-tumor activity and cellular mechanism of the synthetic compound (E)-1-(3,4-dihydroxyphenethyl)-3-styrylurea (PAPU1) using melanoma B16/F10 and M-3 cells. Results showed that PAPU1 inhibited the cell proliferation and viability, but did not induce cytotoxic effects on primary cultured fibroblasts. PAPU1 induced apoptotic cell death rather than necrosis in melanoma cells, a result clearly proven by the shift of cells into sub-$G_1$ phase of the cell cycle and by the substantial increase in cells positively stained with TUNEL or Annexin V. Collectively, this study revealed that PAPU1 induced apoptosis in a caspase-dependent manner, suggesting a potential role as a cancer chemopreventive agent for melanoma cells.

• Food Quality and Culture
• /
• v.1 no.1
• /
• pp.18-21
• /
• 2007

The objective of this study was to prepare bioactive ginseng yogurts containing compound K, which is transformed from ginsenosides, and to investigate the compound's cytotoxicity against tumor cells. Milk containing ginseng was fermented by Bifidobacteria KK-I and KK-2, and their activities for transforming ginsenosides to compound K were measured. Among the tested concentrations of ginseng in the milk, compound K was effectively produced in the 3% and 6% ginseng yogurts fermented for 48 hrs. These fermented ginseng yogurts were extracted with BuOH, and their cytotoxicities against tumor cells were examined. The BuOH extract of the yogurt made from the 3% ginseng milk showed cytotoxic activity against P388 and HeLa tumor cells. However, the nonfermented ginseng milk did not exhibit cytotoxicity against these cells. Therefore, we deem that the ginseng yogurt, which contained compound K, could be developed as a potential fermented drink product.

• Analytical Science and Technology
• /
• v.10 no.2
• /
• pp.153-159
• /
• 1997

This study was conducted to test antifungal activity and to separate bioactive compound using C. japonica extract which was shown the most effective control on the B. berengeriana, G. cingulata and P. expansum. $EC_{50}$ on the test pathogene of C. japonica extract was $400{\sim}500{\mu}g/mL$. Bioactive compound analyzed by TLC and HPLC method was identified as a kind of alkaloids, berberine, and the content was 81.14%.

• Journal of Ginseng Research
• /
• v.42 no.3
• /
• pp.255-263
• /
• 2018

Orally administered ginsengs come in contact with the gut microbiota, and their hydrophilic constituents, such as ginsenosides, are metabolized to hydrophobic compounds by gastric juice and gut microbiota: protopanxadiol-type ginsenosides are mainly transformed into compound K and ginsenoside Rh2; protopanaxatriol-type ginsenosides to ginsenoside Rh1 and protopanaxatriol, and ocotillol-type ginsenosides to ocotillol. Although this metabolizing activity varies between individuals, the metabolism of ginsenosides to compound K by gut microbiota in individuals treated with ginseng is proportional to the area under the blood concentration curve for compound K in their blood samples. These metabolites such as compound K exhibit potent pharmacological effects, such as antitumor, anti-inflammatory, antidiabetic, antiallergic, and neuroprotective effects compared with the parent ginsenosides, such as Rb1, Rb2, and Re. Therefore, to monitor the potent pharmacological effects of ginseng, a novel probiotic fermentation technology has been developed to produce absorbable and bioactive metabolites. Based on these findings, it is concluded that gut microbiota play an important role in the pharmacological action of orally administered ginseng, and probiotics that can replace gut microbiota can be used in the development of beneficial and bioactive ginsengs.

• Journal of Photoscience
• /
• v.9 no.2
• /
• pp.138-141
• /
• 2002

A photo-labile compound which is bioinactive but, upon irradiation with light, yields bioactive species is called as "caged compound". Photolysis of caged compounds generating bioactive species, has become a general method to produce a desired amounts of bioactive species in the specific time interval at the desired place or area of the target biological systems. For this purpose, we designed and synthesized caged hydroxyl radical., "Photo-Fenton Reagent" NP-IIl. NP-IIl has a strong absorption maximum at 377 nm and yields hydroxyl radicals upon UV light irradiation. The antioxidant activity of the ${\alpha}$ -lipoic acid and other naturally occurring compounds has been examined by using NP-IIl as a molecular probe. For example, upon photoirradiation of NP-lII with BSA or apolipoprotein of human low density (LDL), the significant oxidative modifications were observed in both cases. The oxidation was completely suppressed in the presence of ${\alpha}$-lipoic acid, which clearly demonstrates the strong hydroxyl radical scavenging activity of ${\alpha}$-lipoic acid. Other applications of NP-lII will also be described

• Proceedings of the Korean Society of Crop Science Conference
• /
• 2018.10a
• /
• pp.42-42
• /
• 2018

Anthocyanins has a strong antioxidant capacity but exhibit poor stability in water. Therefore, stability of anthocyanin from purple potato (Solanum tuberosum L.) was encapsulated by the application of food polymers. Solid formulation of purple potato was prepared using whey protein, tapioca and lecithin by capillary rheometer at $80^{\circ}C$. The ratio of the polymer and potato powder was 2:8. Total phenolic compound, total flavonoid, total anthocyanin and antioxidant activity was investigated by the spectrophotometer. Result revealed that total phenolic compound (TP) ($5321{\mu}g/100g$), total flavonoid (TF) ($1352{\mu}g/100g$) total anthocyanin (TA) ($764{\mu}g/100g$) and free radical antioxidant activity (DPPH) (86%) was higher in 0.01 M acetic acid mediated lecithin based formulation compared to control (Potato powder) (TP: $1357{\mu}g/100g$; TF) ($634{\mu}g/100g$, TA) ($264{\mu}g/100g\;DPPH$) (64%). Lecithin is a strong emulsifier having capacity to extract bioactive compound and encapsulate extracted compound by nonpolar tail and negatively charged head. Therefore, it would be concluded that lecithin might be used as an encapsulating agent for the bioactive compound from purple potato.

• Proceedings of the Korean Society of Crop Science Conference
• /
• 2018.10a
• /
• pp.274-274
• /
• 2018

Anthocyanins has a strong antioxidant capacity but exhibit poor stability in water. Therefore, stability of anthocyanin from purple potato (Solanum tuberosum L.) was encapsulated by the application of food polymers. Solid formulation of purple potato was prepared using whey protein, tapioca and lecithin by capillary rheometer at $80^{\circ}C$. The ratio of the polymer and potato powder was 2:8. Total phenolic compound, total flavonoid, total anthocyanin and antioxidant activity was investigated by the spectrophotometer. Result revealed that total phenolic compound (TP) ($5321{\mu}g/100g$), total flavonoid (TF) ($1352{\mu}g/100g$) total anthocyanin (TA) ($764{\mu}g/100g$) and free radical antioxidant activity (DPPH) (86%) was higher in 0.01 M acetic acid mediated lecithin based formulation compared to control (Potato powder) (TP: $1357{\mu}g/100g$; TF) ($634{\mu}g/100g$, TA) ($264{\mu}g/100g\;DPPH$) (64%). Lecithin is a strong emulsifier having capacity to extract bioactive compound and encapsulate extracted compound by nonpolar tail and negatively charged head. Therefore, it would be concluded that lecithin might be used as an encapsulating agent for the bioactive compound from purple potato.

• Archives of Pharmacal Research
• /
• v.24 no.4
• /
• pp.270-275
• /
• 2001

Bioisostere approach has been shown to be useful to augment potency or to modify certain physiological properties of a lead compound. Based upon well documented bioisosterism, an isosteric replacement of benzene ring of 4-hydroxy-2-quinolone compound (L-695902) with a thiophene moiety was carried out to prepare the title compounds, 4-hydroxy-6-oxo-6,7-dihydro-thieno[2,3-b] pyrimidines 15. The resulting bioisosteric compounds 15 were evaluated for their antagonistic activity (birding assay) for NMDA receptor glycine site.

• Archives of Pharmacal Research
• /
• v.24 no.4
• /
• pp.300-306
• /
• 2001

A novel and two known bioactive mono-tetrahydrofuran (THF) annonaceous acetogenins, annomocherin (1), annonacin (2) and annomontacin (3), have been isolated from the fractionated ethanolic extracts of the seeds of Annona cherimolia, guided by the brine shrimp lethality test (BST). Their structures were elucidated on the basis of spectroscopic and chemical methods. All compounds have a relative stereochemistry of threo/trans/threo for the mono-THF ring with two flanking hydroxyls. Compound 1 has a double bond at C-23/ 24 of aliphatic chain. Compound 1 was isolated from natural sources for the first time, and was named annomocherin. Two known Compounds 2 and 3 which have never been isolated from this species before, were obtained. Compound 1 exhibited potent and selective cytotoxicities against the breast carcinoma (MCF-7) and kidney carcinoma (A-498) cell lines with 100 to 1,000 times the potency of adriamycin. In brine shrimp lethality test (BST), 1-3 exhibited cytotoxicity.