Effects Of Xanthones Research Articles

Effect of 1-Carbaldehyde-3,4-dimethoxyxanthone on Prostate and HPV-18 Positive Cervical Cancer Cell Lines and on Human THP-1 Macrophages.

Xanthone derivatives have shown promising antitumor properties, and 1-carbaldehyde-3,4-dimethoxyxanthone (1) has recently emerged as a potent tumor cell growth inhibitor. In this study, its effect was evaluated (MTT viability assay) against a new panel of cancer cells, namely cervical cancer (HeLa), androgen-sensitive (LNCaP) and androgen-independent (PC-3) prostate cancer, and nonsolid tumor derived cancer (Jurkat) cell lines. The effect of xanthone 1 on macrophage functions was also evaluated. The effect of xanthone 1-conditioned THP-1 human macrophage supernatants on the metabolic viability of cervical and prostate cancer cell lines was determined along with its interference with cytokine expression characteristic of M1 profile (IL-1 ≤ β; TNF-α) or M2 profile (IL-10; TGF-β) (PCR and ELISA). Nitric oxide (NO) production by murine RAW264.7 macrophages was quantified by Griess reaction. Xanthone 1 (20 μM) strongly inhibited the metabolic activity of the cell lines and was significantly more active against prostate cell lines compared to HeLa (p < 0.05). Jurkat was the cell most sensitive to the effect of xanthone 1. Compound 1-conditioned IL-4-stimulated THP-1 macrophage supernatants significantly (p < 0.05) inhibited the metabolic activity of HeLa, LNCaP, and PC-3. Xanthone 1 did not significantly affect the expression of cytokines by THP-1 macrophages. The inhibiting effect of compound 1 observed on the production of NO by RAW 264.7 macrophages was moderate. In conclusion, 1-carbaldehyde-3,4-dimethoxyxanthone (1) decreases the metabolic activity of cancer cells and seems to be able to modulate macrophage functions.

Pengaruh Pemberian Ekstrak Kulit Buah Manggis (Garcinia mangostana L.) Menghambat Flexi Cranial Embrio Ayam Umur 48 Jam

Embryonic development forms three layers of germinativum that is endoderm, mesoderm and ectoderm. At the beginning of intrauterine fetus exchange of substances through diffusion, but in line with the development of the embryo, nutrition is not obtained through diffusion alone. Endoderm lining mesoderm cells will then be formed angioblasts as an early sign of vascularity. In the development of flexi cranial can be known from the development of the brain and heart which is characterized by bending the head of the embryo and decreased heart from the cranial down. The development of a normal vascular system will have an effect on organogenesis and morphogesis processes. If there are disturbances in the process of growth and development at that stage can cause congenital abnormalities. Xanthones mangosteen peel is rich in benefits, but in research on the effects of xanthones on embryos is still very limited and has not been able to explain their effects on the condition of the fetus. The study was conducted with the aim to determine the effect of mangosteen peel extract inhibiting the flexi cranial of 48 hours chicken embryos using doses of 100 µg/mL, 150 µg/mL and 200 µg/mL. Mangosteen peel extract is injected into chicken eggs less than 7 days after oviposition then incubated for 48 hours. The results showed that mangosteen peel extract inhibited flexi cranial of chicken embryos with Chi-Square test results (p = 0.002). The conclusion of the study was that exposure to mangosteen peel extract inhibited flexi cranial and gave significant results.

Therapeutic potential of xanthones from Swertia chirata in breast cancer cells.

Background & objectives:Medicinal plants like Swertia chirata are rich sources of different xanthones. This study was aimed to assess the cytotoxic potential of four most abundant xanthones present in S. chirata both in vivo and in vitro in Ehrlich ascites carcinoma (EAC), a mouse transplantable breast carcinoma cell line and two human breast carcinoma cell lines (MCF-7 and MDA-MB-231).Methods:Four xanthones derived from S. chirata namely 1-hydroxy-3,7,8-trimethoxyxanthone (XA), 1,8-dihydroxy-3,5-dimethoxyxanthone (XB), 1-hydroxy-3,5,8-trimethoxyxanthone (XC) and 1,5,8-trihydroxy-3-methoxyxanthone (XD) were used for determination of sub-lethal dose on the cell lines EAC, MCF-7, MDA-MB-231 and verified toxicity of sub-lethal dose on normal murine fibroblast cells. Cytotoxicity was measured in vivo and survivability of mice was plotted accordingly. Therapeutic efficacy of XD was evaluated both in vivo and in vitro by determination of lipid peroxidation (LPO), reactive oxygen species (ROS) generation and by quantitating the enzyme status (GSH, catalase, superoxide dismutase) in treated and untreated samples. DNA damage was evaluated using comet and DNA fragmentation assays. Furthermore, apoptotic effect was analyzed by flow cytometry and validated by TUNEL assay and Western blotting.Results:Among all the xanthones tested XD showed IC50 at the lowest dose, and normal cells were unaffected at this dose. Survivability of mice increased significantly when treated with XD compared to other xanthones and cisplatin. Significantly increased ROS and LPO were found in cancer cells as a result of XD treatment which was unaltered in normal cell line. XD induced DNA damage and apoptosis in cancer cell lines.Interpretation & conclusions:Our experimental data indicate that XD may potentially act as a chemotherapeutic agent by enhancing ROS in breast cancer cells thereby leading to apoptosis.

The potential of xanthones as a therapeutic option in macrophage-associated inflammatory diseases

Xanthones are well known for their significant biological activities and can be found in many herbal medicines. These compounds have the ability to regulate various inflammatory activities and signaling pathways in immune cells, especially macrophages. Macrophages are innate immune cells that can either fuel or dampen an inflammatory response depending on their activation states and play an active role in the development of inflammatory diseases such as atherosclerosis, arthritis, cancer, and diabetes. Many traditional medicines used as a remedy for these diseases contain xanthones, and their bioactivities may be partially attributed to their ability in regulating macrophage responses. In this review, we discuss the in vitro and in vivo findings on the effects of xanthones on different macrophage immune functions including nitric oxide and cytokine production, migration, polarization, and phagocytosis. Their specific modes of action are highlighted whenever known. We also discuss the potential and challenges in using xanthones as a therapeutic option in various inflammatory diseases. It is hoped that this review can pave the way for future research that focuses on developing xanthones as specific macrophage-targeted therapeutics.

Effect of Xanthone and 1-Hydroxy Xanthone on the Dipole Potential of Lipid Membranes

Xanthone (Xa) and 1-OH Xanthone (1-OHXa) in 1,2-dipalmitoyl-sn-glycero-3-phosphocholine (DPPC) membranes increase the dipole potential. Results with 1,2-di-O-tetradecyl-sn-glycero-3-phosphocholine (Ether PC), lacking carbonyl groups, indicate that the CO dipole of Xa molecule does not contribute to the increase of dipole potential. Molecular Dynamics calculations confirm that CO group of Xa locates parallel to the membrane interphase. Xa decreases the area per lipid in DPPC monolayers and the membrane polarity as measured by GP of Laurdan explaining the dipole potential increase. This rearrangement of water in the CO region is consistent with Fourier Transform Infrared Spectroscopy results indicating that CO of Xa are buried in the membrane phase. In contrast, CO groups of DPPC show an additional population of bound COs that seems to be more exposed to water, which contributes to the increase in dipole potential. These results are also corroborated by MD simulations.

The development of antiseptic gel from mangosteen shell extract

Mangosteen (Garcinia mangostana L.) is widely grown throughout the Southeast Asian countries and well known as the queen of fruits. The mangosteen shell extracts have more potential for antibacterial activity. This study was undertaken to develop an antiseptic hand cleansing gel which increased efficiency for killing potentially pathogenic organisms by effect of xanthones in mangosteen shell extracts and to investigate antibacterial activity of this antiseptic gel. The mangosteen shell was extracted by acetone and the xanthones concentrations were analyzed by using HPLC. The result showed that the extract contained the active xanthones: alpha‐mangostin and gamma‐mangostin 34.12 and 5.63 g%, respectively. The optimum formulation of antiseptic gel contained mangosteen shell extract 0.5% of gel. This antiseptic gel showed good effective to control bacteria; Escherichia coli, MRSA, Micrococcus leteus, Pseudomonas aeruginosa, Bacillus subtilis, Staphylococcus aureus, and Candida albicans. Consumer acceptance testing with 20 volunteers who were between 18–30 years old showed that 95% of consumers accepted antiseptic gel with mangosteen shell extract and the overall liking was like slightly. Therefore, this antiseptic hand cleansing gel would be possibly for an alternative product for the personal hand hygiene.

Potential effects of xanthone on inflammation status in atherosclerotic rats

Aim: To clarify an effect of xanthones on inflammation status in hypercholesterolemic rats. Method: A total of 32 Wistar rats were divided into four groups (n=8), including control, hypercholesterolemic diet groups, hypercholesterolemic diet + xanthone at dose 35; 70; and 140 mg/kg body weight (mg/kgBW). Control group received standard diet for 60 days. Hypercholesterolemic diet group received standard diet plus yellow egg, sheep oil, cholic acid, and pig oil for 60 days per oral. Analysis of nuclear factor-kappa beta p65/p50 distribution and tumor necrosis factor-alpha level, was done using enzyme linked immunosorbent assay technique. Analysis of nitric oxide level was done by colorimetric technique using spectrophotometer. Results: Hypercholesterolemic diet significantly increased nuclear factor-kappa beta p65/p50 distribution, tumor necrosis factor-alpha level, and nitric oxide level compared with the control group (p

Effect of xanthone from Kielmeyera coriacea stems on serotonergic neurons of the median raphe nucleus

Kielmeyera coriacea Mart. (Clusiaceae), known as "Pau Santo", is used to treat several tropical diseases. The hydroethanolic extract (HE) of Kielmeyera coriacea stems and its semi-pure dichloromethane constituent (DCM) produced an anti-immobility effect in rats submitted to the forced swimming test (FST), suggesting a antidepressant-like profile. This study evaluated the effect of intra-median raphe nucleus (MRN) microinjection of 1,3,7-trihydroxy-2-(3-methylbut-2-enyl)-xanthone, present in large quantity in the HE from Kielmeyera coriacea stems, on immobility behaviour in the FST in rats. The effects of xanthone were compared with intra-MRN microinjections of Way100635 (5-HT1A antagonist) or (+) 8-OH-DPAT (5-HT1A agonist). Locomotor activity in the open-field test (OFT) was evaluated as a complementary measure. Xanthone (0.3ng) or Way100635 (2.5microg) reduced, whereas (+) 8-OH-DPAT (5.0microg) increased immobility time in the FST. Way100635 (2.5 or 5.0microg) completely reversed the effects of (+) 8-OHDPAT (5.0microg), and potentiated the anti-immobility effect of the ineffective dose of xanthone (0.2ng) in the FST. The association of effective doses of (+) 8-OH-DPAT (5.0microg) and xanthone (0.3ng) annulled the effect of each compound on immobility time. These results suggest that xanthone acts as an antagonist at 5-HT1A autoreceptors in MRN and increases serotonin (5-HT) availability in projection regions, proving to be a prototype drug that may be useful in mood isorders such as depression, or indeed be a beneficial adjunctive treatment improving the efficacy and/or accelerating the effects of antidepressant drugs in patients with major depression.

Anti‐Inflammatory Effects of Xanthones from Mangosteen in Primary Cultures of Human Adipocytes

The xanthones, α‐ and γ‐ mangostin (MG), are major bioactive compounds found in mangosteen reported to have anti‐inflammatory activities in several murine models. Given the association between chronic, low grade inflammation and obesity, we examined the anti‐inflammatory effects of α‐ and γ‐ MG in primary cultures of human adipocytes in the presence or absence of lipopolysaccharide (LPS). α‐ and γ‐MG significantly decreased LPS induction of inflammatory adipocytokines (i.e., TNF‐α, IL‐1β, IL‐6, IL‐8, and MCP‐1). Moreover, α‐ and γ‐ MG attenuated LPS activation of the mitogen‐activated protein kinases (MAPK) c‐jun NH2‐terminal kinase (JNK), extracellular signal‐related kinase (ERK), and p38. γ‐ MG was more effective than α‐ MG on an equimolar basis. Furthermore, γ‐MG, but not α‐MG, attenuated LPS‐mediated IκB‐α degradation and nuclear factor‐κB (NF‐κB) transcriptional activity. In conclusion, these data demonstrate for the first time that α‐ and γ‐ MG attenuate LPS‐mediated inflammation in human (pre)adipocytes by inhibiting MAPK or NF‐κB signaling. These data suggest that MG has the potential to attenuate chronic inflammation associated with obesity. (Supported by National Research Council of Thailand)Grant Funding SourceNational Research Council of Thailand

Induction of calcium release from sarcoplasmic reticulum of skeletal muscle by xanthone and norathyriol.

1. Effects of xanthone and its derivative, 1,3,6,7-tetrahydroxyxanthone (norathyriol), on Ca2+ release and ryanodine binding were studied in isolated sarcoplasmic reticulum (SR) vesicles from rabbit skeletal muscle. 2. Both xanthone and norathyriol dose-dependently induced Ca2+ release from the actively loaded SR vesicles which was blocked by ruthenium red, a specific Ca2+ release inhibitor, and Mg2+. 3. Xanthone and norathyriol also dose-dependently increased apparent [3H]-ryanodine binding. Norathyriol, but not xanthone, produced a synergistic effect on binding activation when added concurrently with caffeine. 4. In the presence of Mg2+, which inhibits ryanodine binding, both caffeine and norathyriol, but not xanthone, could restore the binding to the level observed in the absence of Mg2+. 5. Xanthone activated the Ca(2+)-ATPase activity of isolated SR vesicles dose-dependently reaching 70% activation at 300 microM. 6. When tested in mouse diaphragm, norathyriol potentiated the muscle contraction followed by twitch depression and contracture in either a Ca(2+) -free bathing solution or one containing 2.5 mM Ca2+. These norathyriol-induced effects on muscle were inhibited by pretreatment with ruthenium red or ryanodine. 7. These data suggest that xanthone and norathyriol can induce Ca2+ release from the SR of skeletal muscle through a direct interaction with the Ca2+ release channel, also known as the ryanodine receptor.