Breast cancer stem cells (BCSCs) express high levels of the anti-apoptotic protein, survivin. This study aimed to discover a natural active compound with anti-cancer properties that targeted survivin in human breast cancer stem cells. From the seven examined compounds, andrographolide was selected as a lead compound through in silico molecular docking with survivin, caspase-9, and caspase-3. We found that the affinity between andrographolide and survivin is higher than that with caspase-9 and caspase-3. Human CD24-/CD44+ BCSCs were treated with andrographolide in vitro for 24 hours. The cytotoxic effect of andrographolide on BCSCs was compared to that on human mesenchymal stem cells (MSCs). The expression of survivin, caspase-9, and caspase-3 mRNA was analyzed using qRT-PCR, while Thr34-phosphorylated survivin and total survivin levels were determined using ELISA and Immunoblotting assay. Annexin-V/PI flow cytometry assays were performed to evaluate the apoptotic activity of andrographolide. Our results demonstrate that the CC50 of andrographolide in BCSCs was 0.32mM, whereas there was no cytotoxic effect in MSCs. Moreover, andrographolide decreased survivin and Thr34-phosphorylated survivin, thus inhibiting survivin activation and increasing survivin mRNA in BCSCs. The apoptotic activity of andrographolide was revealed by the increase of caspase-3 mRNA and protein, as well as the increase in both the early and late phases of apoptosis. In conclusion, andrographolide can be considered an anti-cancer compound that targets BCSCs due to its molecular interactions with survivin, caspase-9, and caspase-3, which induce apoptosis. We suggest that the binding of andrographolide to survivin is a critical aspect of the effect of andrographolide.
Andrographolide is the main bioactive compound derived from sambiloto, Andrographis paniculata. Andrographolide compounds can potentially be used as phytopharmaca substances. Andrographolide has very broad pharmacological aspects, including anti-inflammatory, anticancer and anti-diabetic. The pharmacological aspects possessed by andrographolide are probably closely related to the chemical profile and the mechanism of action of andrographolide as an antioxidant in counteracting free radicals. Therefore, it is important to know the chemical profile and mechanism of action of andrographolide compounds as antioxidants to understand the mechanism of action of these compounds in dealing with various diseases. This study is based on a review of related literature. Based on the literature review, it was found that the mechanism of action of andrographolide as anti-cancer, anti-inflammatory and anti-dyslipidemia is closely related to the mechanism of action of this compound as an antioxidant. The unsaturated γ- lactone structure at C13 and C14 of andrographolide can neutralize superoxide anions. The double bond in this carbonyl ester group will affect the deprotonization of the H atone located at C15 so that the H atoms on C15 will be easily extracted by the highly reactive superoxide anion. Thus, andrographolide can stop the chain reaction of a radical molecule. This mechanism can cause andrographolide compounds to play a role in reducing the effects of free radicals in various diseases.
and a high survival rate. Breast CSCs (BCSCs) are heterogeneous and identified based on the presence of several surface antigen markers, such as CD44+, CD24−, and ALDH+. Because BCSCs are considered to be responsible for recurrence, the development of breast cancer therapy should focus on its elimination (Li et al.,
This study aims to determine the immunomodulatory activity of lemongrass essential oil on the proliferation of mouse lymphocyte cells in vitro. The method used is steam distillation to obtain citronella essential oil. Isolation of lymphocyte cells was obtained from the spleen organ of Swiss-Webster strain mice which was carried out aseptically. The lymphocyte cell proliferation test was carried out using the MTT Assay method and the absorbance was measured using an ELISA reader at 550 nm. The results showed that the lemongrass essential oil contained positive alkaloids, flavonoids, saponins, and steroids/triterpenoids with an essential oil yield of 0.043%. The higher the volatile oil concentration, the higher the Optical Density (OD) value obtained, but the OD increase at a 50 to 100 g/mL concentration was not significantly different. In conclusion, lemongrass essential oil has immunomodulatory activity against lymphocyte cell proliferation in mice tested in vitro. Keywords: Immunomodulator, Essential Oil, Lemongrass (Cymbopogon citratus), Immune System
Abstract.Yunita E, Kurniati T, Rosa FL, Melati P, LestariN. 2022. Short Communication: Analysis of detected metabolites compounds from the crude extract of Rimau Gerga Lebong orangesfruit (Citrus reticulata ‘RGL’) using LC-QTOF-MS/MS. Biodiversitas 23: 3778-3783. Rimau Gerga Lebong (RGL) oranges are the leading commodity in Bengkulu Province. However, the content of bioactive compounds in RGL oranges has not been widely reported. This study aims to identify the flavonoid, alkaloids, and tannins from the ethanol extract of RGL oranges. The results of further identification will be used as a reference in further research on molecular docking in various biological activities. Chemical compounds were identified using qualitative tandem liquid chromatography quadrupole time of flight mass spectrometry (LC-QTOF-MS/MS). The measurement of vitamin C levels was carried out using High-Performance Liquid Chromatography (HPLC). The results showed 25 identified compounds, consisting of 6 compounds belonging to the alkaloid group, 17 from the flavonoid group, and 2 from the tannin group. The alkaloid group compounds were 2?, 3?, 6exo-trihydroxy nortopane, 2?, 3?-dihydroxy nortopane, isosalsolin,3?-dihydrocadambine, chelidimerine, and oleracein D. The compounds from identified flavonoid group were chebuloside, neokurarinol, rutinoside, flavonone, glucoside, licochalcone, viscumneoside, and pinnatifinoside. The identified tannins are corilagin and moracin. These compounds that have been identified have biological activity potential as antioxidants, anti-asthma, anti-dementia, and anticancer. The vitamin C content of the ethanol extract of RGL oranges was 0.02±0.0001%. This vitamin C supports the antioxidant activity of RGL orange.
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