Brucea
Quassins
Glaucarubin
Amebicides
Brusatol-mediated induction of leukemic cell differentiation and G(1) arrest is associated with down-regulation of c-myc. (1/11)
Employing the natural product quassinoid brusatol, we currently report cellular and molecular events leading to cell death or terminal differentiation in a panel of leukemic cells. Brusatol and bruceantin exerted significant cytotoxic effects with several leukemic cell lines, but not with K562 or normal lymphocytic cells. Cell lines that were less sensitive to the cytotoxic effects of brusatol responded primarily through induction of terminal differentiation. The differentiated phenotype in cell lines derived from acute or chronic myeloid leukemias (HL-60, K562, Kasumi-1, NB4, U937, BV173) was characterized for producing superoxide and non-specific esterase, and some with up-regulation of CD13 (cluster of differentiation) and down-regulation of CD15. Chronic myeloid leukemic cell lines, K562 and BV173, and acute lymphoblastic cell lines, SUPB13 and RS4;11, were induced to differentiate along the erythrocytic pathway. Withdrawal studies showed that brusatol treatment for 48 h was sufficient to induce commitment towards terminal differentiation in HL-60, K562 and SUPB13. Reh cells did not undergo maturation. Analysis of c-MYC protein expression revealed that brusatol or bruceantin down-regulated expression to undetectable levels in cell lines that were most sensitive, based on cell death or terminal differentiation. Generally, c-myc RNA was reduced, but to a lower extent than c-MYC protein levels, indicating c-myc expression was regulated by quassinoids at the post-transcriptional level. Thus, regulation of c-myc expression may represent a critical event that leads to terminal differentiation. Since these responses are facilitated at clinically achievable concentrations, quassinoids may be of value for the management of hematological malignancies. (+info)Formulation, preparation and evaluation of an intravenous emulsion containing Brucea javanica oil and Coix Seed oil for anti-tumor application. (2/11)
The purpose of this study was to prepare and evaluate the intravenous emulsion (BCOE) containing Brucea javanica oil (BJO) and Coix seed oil (CSO), which is used in anti-tumor treatment. The formulation and preparation of BCOE were systematically investigated. High-pressure homogenization, particle size distribution, zeta-potential and HPLC were carried out. The pharmacokinetics of the main component, oleic acid, and anti-tumor activity studies about the tumor growth inhibitory ratios (TGIR) and the mortality experiments were also employed to evaluate BCOE in vivo compared with BJO emulsion (BJOE) and CSO emulsion (CSOE) using S180 sarcoma-bearing mice. The final BCOE formulation was 10% (w/v) oils with BJO and CSO 3 : 1, 0.6% (w/v) Lipid E 80, 0.3% (w/v) Pluronic F-68 (F-68), 0.1% (w/v) sodium oleate and 2.5% (w/v) glycerin in water. The preparation conditions involved 70 degrees C for preparing the crude emulsion, 6 cycles for high-pressure homogenization at 500 bar, pH value was adjusted to 8.5 after high-pressure homogenization and 115 degrees C for 30 min in a rotating water bath for sterilization. The pharmacokinetics parameters showed the combination of BJO and CSO may not influence the elimination of BCOE and have no significant difference between BCOE and BJOE or CSOE. The data of TGIR and mortality indicated that BCOE could increase the anti-tumor activity of CSOE and reduced the toxicity of BJOE. The mortality study (BCOE 0, BJOE 63.3%, CSOE 13.3%) showed that BCOE greatly reduced the toxicity of BJOE and CSOE. Therefore, the development and application of BCOE will make an important contribution to anti-tumor therapy. (+info)Bioactivity-guided isolation of cytotoxic constituents of Brucea javanica collected in Vietnam. (3/11)
(+info)Evaluation of efficacy of bruceine A, a natural quassinoid compound extracted from a medicinal plant, Brucea javanica, for canine babesiosis. (4/11)
Bruceine A, a natural quassinoid compound extracted from the dried fruits of Brucea javanica (L.) Merr., was evaluated for its antibabesial activity in vitro and in vivo. Bruceine A inhibited the in vitro growth of Babesia gibsoni in canine erythrocytes at lower concentration compared with the standard antibabesial drug diminazene aceturate and killed the parasites within 24 hr at a concentration of 25 nM. Oral administration of bruceine A at a dosage of 6.4 mg/kg/day for 5 days resulted in no clinical findings in a dog with normal ranges of hematological and biochemical values in the blood. Three dogs were infected with B. gibsoni and two of them were treated with bruceine A at a dosage of 6.4 mg/kg/day for 6 days from day 5 post-infection. An untreated dog developed typical acute babesiosis symptoms including severe anemia, high fever, and complete loss of appetite and movement. However, the two bruceine A-treated dogs maintained their healthy conditions throughout the experimental period of 4 weeks although complete elimination of parasites from the peripheral blood was not achieved and decreases in the packed cell volume and the erythrocyte and platelet counts were observed. Since natural quassinoid compounds have been used as traditional medicines for the treatment of various ailments including cancer and malaria, the present results suggest that bruceine A or other related compounds are potential candidates for the treatment of canine babesiosis. (+info)Isolation of antibabesial compounds from Brucea javanica, Curcuma xanthorrhiza, and Excoecaria cochinchinensis. (5/11)
One new curcuminoid, 3'-demethoxycyclocurcumin (1), was isolated from Curcuma xanthorrhiza as an antibabesial compound, together with p-hydroxybenzaldehyde (2) and cleomiscosin A (3) from Brucea javanica and (+)-epiloliolide (4) from Excoecaria cochinchinensis. The antibabesial activities were examined in vitro, and compounds 1-4, and diminazene aceturate were studied with IC(50) values of 16.6, 7.6, 15.6, 10.0, and 0.6 microg/ml, respectively. (+info)Preparation, safety, pharmacokinetics, and pharmacodynamics of liposomes containing Brucea javanica oil. (6/11)
(+info)NF-kappaB inhibitors from Brucea javanica exhibiting intracellular effects on reactive oxygen species. (7/11)
AIM: Brucea javanica was studied to identify nuclear factor kappaB (NF-kappaB) inhibitors exhibiting reactive oxygen species (ROS) intracellular amplification. MATERIAL AND METHODS: Eight compounds were evaluated for selective cytotoxicity using HT-29, HeLa, and HL-60 cells, and in a NF-kappaB assay. Active compounds were then tested using ROS and mitochondria transmembrane potential (MTP) assays. NF-kappaB and nuclear factor activated T-cell (NFAT) translocation were also assessed using their respective whole cell assays. RESULTS: Bruceajavanone B, bruceantin, bruceine A, (-)-hydnocarpin, and chrysoeriol exhibited cytotoxic potential and NF-kappaB p65 inhibition. Chrysoeriol exhibited selective cytotoxicity against leukemia cells with greater potency and also showed an ability to up-regulate NFAT transcriptional pathways through the amplification of intracellular ROS, in the presence of H2O2, to a greater degree than bruceantin and bruceine. CONCLUSION: Chrysoeriol selectively kills leukemic cells and potentiates the amplification of ROS levels. Therefore, chrysoeriol could serve as a potential chemotherapeutic modifier for leukemia chemotherapy since leukemia cells have a higher susceptibility to elevated ROS levels. (+info)Chemical components, pharmacological properties, and nanoparticulate delivery systems of Brucea javanica. (8/11)
(+info)"Brucea" is a genus of flowering plants in the family Simaroubaceae. It includes several species of small trees and shrubs that are native to tropical regions of Africa and Asia. Some species of Brucea have been used in traditional medicine for their antimalarial, anti-inflammatory, and antipyretic properties. The active compounds in these plants include quassinoids, which have been shown to have various biological activities. However, it is important to note that the use of Brucea species in medical treatments should be based on scientific evidence and under the guidance of a healthcare professional.
Quassinoids are a group of naturally occurring compounds that are found in various plants, including the bark of Quassia amara, a tree native to South America. Quassins, one type of quassinoid, have been studied for their potential medicinal properties, particularly as antimalarial and anticancer agents. They are known to interact with cell membranes and can affect the growth and multiplication of certain types of cells. However, more research is needed to fully understand their mechanisms of action and potential therapeutic uses. It's important to note that quassins can also be toxic in high concentrations, so further studies are necessary to determine safe and effective dosages for medical use.
Glaucarubin is not typically defined in a medical context, but it is a chemical compound found in certain plants. It is a quassinoid, a type of triterpene, and has been isolated from the bark of the tree *Glaucothea glauca*, also known as *Picrasma excelsa*.
In some traditional medicine systems, such as Amazonian and West African, extracts containing Glaucarubin have been used for various purposes, including as a purgative or to treat intestinal parasites. However, it is not widely used in modern medical practice due to its potential toxicity and lack of rigorous clinical research supporting its efficacy.
Therefore, while Glaucarubin may be mentioned in some medical contexts related to traditional medicine or phytochemistry, it does not have a specific medical definition.
Amebicides are medications that are used to treat infections caused by amebae, which are single-celled microorganisms. One common ameba that can cause infection in humans is Entamoeba histolytica, which can lead to a condition called amebiasis. Amebicides work by killing or inhibiting the growth of the amebae. Some examples of amebicides include metronidazole, tinidazole, and chloroquine. It's important to note that these medications should only be used under the guidance of a healthcare professional, as they can have side effects and may interact with other medications.
Flavanolignans are a type of biologically active compounds that are found in certain plants. They are formed from the combination of flavonoids and lignans, two classes of plant phenolic compounds. One of the most well-known groups of flavanolignans is the one found in milk thistle (Silybum marianum), which includes silibinin, silidianin, and silicristin. These compounds have been studied for their potential antioxidant, anti-inflammatory, and liver-protective effects.
Coix is the medical term for a genus of plants commonly known as Job's tears. The seeds of this plant have been used in traditional medicine in various cultures, including Chinese and Ayurvedic medicine. They are believed to have anti-inflammatory, analgesic, and diuretic properties, among others. However, it is important to note that the use of Coix as a medical treatment should be done under the guidance of a healthcare professional, as its effectiveness and safety have not been fully studied in clinical trials.