Isolation of Bioactive Compound of Michelia Champaca L. Bark and Its Activity Test Using Mechanism-Based Yeast Bioassay

Zuhrotun, Ade; Suganda, Asep Gana; Wirasutisna, Komar Ruslan; Wibowo, Marlia Singgih

doi:10.22159/ajpcr.2016.v9i5.12856

Cited by 7 publications

(14 citation statements)

References 14 publications

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“…Yellow champaka bark, n-hexane (Merck), chloroform (Merck), ethyl acetate (Merck), methanol, aqua distillate (chemical laboratory), dimethyl sulfoxide (DMSO, Merck), precoated plate silica gel GF254 (Merck), agar bacteriological (Oxoid), peptone (Oxoid), dextrose (Oxoid), yeast extract (Oxoid), and sodium chloride (Merck), camptothecin (Sigma) and Liriodenine (isolated by previous research with 95.25% of purity) [11].…”

Section: Methodsmentioning

confidence: 99%

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Topoisomerase Inhibitors Activity of Yellow Champaka (Michelia Champaca L.) Bark Extracts and Fractions and Its Liriodenine Contents

et al. 2022

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Objective: This research is aimed to investigate the activity of various extracts and fractions of yellow champaka (Michelia champaca L.) by mechanism-based yeast bioassay (MBYB) against the mutant yeasts. Liriodenin content, an active compound in M. champaca, will analyze to know the correlation with this assay. Methods: The bark of M. champaca was extracted by maceration and graded maceration using n-hexane, ethyl acetate, and methanol. The methanol extract was fractionated using water, n-hexane and ethyl acetate in the liquid-liquid extraction process. Each extract and fractions were tested in vitro by mechanism-based yeast bioassay for their topoisomerase inhibitor activity. Liriodenine content of all samples was analyzed by thin layer chromatography (TLC) densitometry method. Results: The yeast bioassay results showed that all extracts were active as topoisomerase inhibitors (IC12 values under 8000 µg/ml) except MGM. Liriodenine can be used as a marker of active compound in ethyl acetate samples that were EAM, EAGM and EAF with Pearson analysis value-0.887 (P=0.153) and these samples were relatively more active than others. Conclusion: This research showed that various extracts and fractions of yellow champaka bark have topoisomerase inhibitor's activity. Liriodenine can be used as a marker of the active compound so yellow champak bark is a potent natural agents for breast cancer.

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Section: Methodsmentioning

confidence: 99%

“…Liriodenine, an aporphine alkaloid isolated from ethyl acetate fraction of yellow champaka bark was proven active both as topoisomerase I and II inhibitors. This activity is one of the anticancer drug mechanisms [11]. This research is aimed to find out the prospect of yellow champaka bark as a natural agent for breast cancer.…”

Section: Introductionmentioning

confidence: 99%

Topoisomerase Inhibitors Activity of Yellow Champaka (Michelia Champaca L.) Bark Extracts and Fractions and Its Liriodenine Contents

et al. 2022

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“…The Mechanism-based Yeast Bioassay screening method was adapted from Gunatilaka et al (1992) and Gunatilaka and Kingston (1998) in Zuhrotun [22]. In this study, wild-type and mutant Saccharomyces cerevisiae were used, consisting of Saccharomyces cerevisiae strain 1140 (permeable to topoisomerase inhibitor I and has topoisomerase I and II enzymes), 1353 (Rad52 deletion enzyme topoisomerase I (rad52.topI type); only has topoisomerase II enzyme), and 1138 (Rad52 deficient) which is a collection of the Faculty of Pharmacy, Padjadjaran University.…”

Section: Mechanism-based Yeast Bioassaymentioning

confidence: 99%

“…The Ramie leaf ethanol extract, n-hexane fraction, and EtOAc fraction showed the cell inhibition mechanism through topoisomerase I, whereas the CH2Cl2 fraction showed inhibition through the activity of topoisomerase I and II. [22], also stated that most topoisomerase I and II inhibitors cause mutagenic events related to the replication process and part in cell apoptosis.…”

Section: Topoisomerase Inhibitor Activity Of the Ramie Leaf Extract And Its Fractions Using A Mechanism-based Yeast Bioassaymentioning

confidence: 99%

Anti-Cancer Assessment of a Ramie (Boehmeria nivea L. Gaud.) Leaf Extract Using Mcf-7 Cell Line and a Yeast-Based Bioassay

Wulandari

Qaromah

Lolowang

et al. 2021

IJMP

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Introduction: One strategy for molecular cancer therapy is to know the key mechanism of cytotoxic compounds that can kill cancer cells. Ramie (Boehmeria nivea L. Gaud.) leaves contain active compounds that have important effects on cancer chemoprevention. Objective: To obtain the active fraction of a Ramie leaf extract in inhibiting the proliferation of MCF-7 breast cancer cell lines and to determine the mechanism of apoptosis induction using MCF-7 and Saccharomyces cerevisiae strains 1140, 1353, and 1138. Method: Fractions were prepared using n-hexane, dichloromethane (CH2Cl2), ethyl acetate, and n-butanol as solvents. All fractions were tested qualitatively through phytochemical. The MTT-based cytotoxicity assay used MCF-7 (in vitro) to obtain the IC50 value, whereas the model system that targets the enzymatic (topoisomerase) used a yeast-based bioassay to obtain the IC12 value. Apoptotic induction of the active fraction in MCF-7 was performed using flow cytometry and qPCR (2-ΔΔCt method). Results: The phytochemical analysis indicated that the extract fraction consisted of alkaloids and steroids. The smallest IC50 value was obtained from the CH2Cl2 fraction as 3.79 g/mL, potentially act as an anticancer. A higher percentage of apoptosis than that of necrotizing cells and live cells was observed through flow cytometry. The CH2Cl2 fraction with an IC12 value < 8000 in strains 1140, 1353, and 1138 consistently showed the mechanism of apoptosis induction as topoisomerase I and II inhibitors. Also, another mechanism could be through the intrinsic pathway, indicated by the highest expression level in p53. Conclusions: The CH2Cl2 fraction of Ramie leaves can inhibits the proliferation of MCF-7 cells in the active and strong categories. The CH2Cl2 fraction induces apoptosis by increasing p53 gene expression and inhibiting topoisomerase I and II. Thus, it showed potential as an anticancer drug candidate.

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“…This plant has been shown to have analgesic and anti-inflammatory effects, has shown antiproliferative activity, has been found to be useful for wound healing, and has antioxidant and antimicrobial properties. Besides, liriodenine is used both as topoisomerase I inhibitor and topoisomerase II inhibitor [11]. N. nucifera, known in Indonesia as lotus, has been shown to reduce the production of HBsAg.…”

Section: Virtual Screening Using Autodock Vinamentioning

confidence: 99%

Virtual Screening of Indonesian Herbal Database for Cp Allosteric Modulator of Hepatitis B Virus

Ivonie

Yanuar

Firdayani³

2018

Int J App Pharm

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Objective: This study performed a virtual screening of the Indonesian Herbal Database for the core protein allosteric modulator of the hepatitis B virus (HBV) using AutoDock and AutoDock Vina software, to discover novel safe drugs for patients. Methods:The method was validated using the parameters enrichment factor (EF), receiver operating characteristics, and area under the curve (AUC). The grid box size used in virtual screening with AutoDock was 55 × 55 × 55 with EF10% of 0.7652 and AUC of 0.6709, whereas that used in virtual screening with AutoDock Vina was 20.625 × 20.625 × 20.625 with EF5% of 0.5075 and AUC of 0.7832. Results:The top 10 compounds from virtual screening with AutoDock at G levels −11.74-−10.31 kcal/mol were yuehchukene, lansionic acid, stigmast-4-en-3-one, myrtillin, sanggenol O, lanosterol, erycrista-gallin, alpha-spinasterol, cyanidin 3-arabinoside, and cathasterone and with AutoDock Vina at G levels −12.1 to −10.7 kcal/mol were sanggenol O, cucumerin A, yuehchukene, palmarumycin CP1, dehydrocycloguanandin, myrtillin, liriodenine, myricetin 3-alpha-L-arabinopyranoside, myricetin 3-galactoside, and cassameridine.Conclusion: Three compounds were in top list of both virtual screening methods against Cp allosteric modulator of HBV are myrtillin, sanggenol O, and yuehchukene have a prospect to be investigated futher for anti HBV.

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Isolation of Bioactive Compound of Michelia Champaca L. Bark and Its Activity Test Using Mechanism-Based Yeast Bioassay

Cited by 7 publications

References 14 publications

Topoisomerase Inhibitors Activity of Yellow Champaka (Michelia Champaca L.) Bark Extracts and Fractions and Its Liriodenine Contents

Topoisomerase Inhibitors Activity of Yellow Champaka (Michelia Champaca L.) Bark Extracts and Fractions and Its Liriodenine Contents

Anti-Cancer Assessment of a Ramie (Boehmeria nivea L. Gaud.) Leaf Extract Using Mcf-7 Cell Line and a Yeast-Based Bioassay

Virtual Screening of Indonesian Herbal Database for Cp Allosteric Modulator of Hepatitis B Virus

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