31 results about "Pentacyclic Triterpenes" patented technology

The invention discloses an application of an A-ring trihydroxyl substituted pentacyclic triterpene compound to preparation of an antibacterial or anti-tobacco mosaic virus drug. The general formula of the compound is as shown in the specification, wherein hydroxyls of C1, C2 and C3 are respectively in alpha configuration or beta configuration; R1 and R2 are selected from hydrogen or methyl and are different from each other; R3 is selected from -COOH, -CH2OH, -CHO, -COOR1, -CONH2, -CONHR1 and -CONR1R2; R1 and R2 are selected from alkyl containing 1-15 carbon atoms, substituted or unsubstituted phenyl and substituted or unsubstituted phenyl alkyl; and the substituent group is selected from halogen, hydroxyl, cyan, amino, nitryl, sulfydryl or phenyl, acyl, aryl, alkoxy and alkyl containing 1-15 carbon atoms. The compounds have antibacterial or anti-tobacco mosaic virus activity, have extremely high bacteriostatic activity especially to gram positive bacteria, phytophthora nicotiana and tobacco mosaic virus, and have a good application prospect in fields of medicines and pesticides.

The invention discloses mitochondrion-targeted antitumor pentacyclic triterpene derivatives of which the structural formula are disclosed as Formula (I), Formula (II), Formula (III), Formula (IV) or Formula (V), wherein R1 is hydrogen, formacyl, acetyl or a group (n=1-19) disclosed in the specification; R2 is disclosed in the specification (n=1-19); R3 is hydroxy, methoxy or ethoxy; and R4 is disclosed in the specification (n=1-19). The compounds have favorable antitumor activity; and the natural compounds are targeted to the mitochondrion, so that the antitumor pentacyclic triterpene derivatives can be better applied to the development of antitumor drugs. The compounds are salts, thereby greatly enhancing the water solubility of drugs and improving the pharmacokinetic parameters.

The invention relates to the field of pharmacy, in particular to a synthesis method of 13 (18)-oleanane-type pentacyclic triterpene as shown in a formula II and derivatives or pharmaceutically acceptable salts or esters of the 13 (18)-oleanane-type pentacyclic triterpene by 12-oleanane-type pentacyclic triterpene as shown in a formula I and derivatives of the 12-oleanane-type pentacyclic triterpene. Definitions of R1-9 are as shown in specification.

The present invention belongs to the field of organic chemistry and relates to a multi-substituted hydrogenated naphthalene compound, the preparation methods and uses. Specifically, the present invention relates to a chiral multi-substituted ten-hydrogen and/or eight-hydrogen naphthalene compound, the synthetic method and uses. The present invention aims to provide a chiral multi-substituted ten-hydrogen and/or eight-hydrogen naphthalene compound; the oleanane-type or usu-type five-ring triterpenoid compound is used as a raw material for preparing the compound. The multi-substituted ten-hydrogen and/or eight-hydrogen naphthalene compound of the present invention can be used for synthesis of drugs or spices containing multi-hydrogen naphthalene fragments and the analogues. The method of the present invention is simple and easy, low in cost, high in production rate, and can realize industrialization.

The invention relates to the medical technical field, in particular to a pentacyclic triterpene compound which is separated to be obtained from a ranunculaceae plant of pulsatilla cernua (Thunb.) Bercht.et Opiz, and the chemical structural formula is shown in the accompanying drawing, wherein glc, rha and ara respectively represent beta-D-glucopyranose, alpha-L-pyrane rhamnose and alpha-L-pyrane arabinose, and the compounds A and B are respectively a new compound. Cell experiments in vitro show that the compound has a remarkable protection function to neuroblastoma cell strain SH-SY5Y induced by A beta (25-35). The compound disclosed by the invention has the advantages of simpleness in preparation and remarkable activity. The invention provides the new compound for preventing and curing AD (Alzheimer's Disease). In the invention, the glc, rha and ara respectively represent beta-D-glucopyranose, alpha-L-pyrane rhamnose and alpha-L-pyrane arabinose.

The invention relates to six new compounds for treating psoriasis, a preparation method and an application thereof. The six new compounds belong to a series of derivatives from a mother compound: acetyl-11-keto-[beta]-boswellic acid (AKBA) through modification of a hydrolysis reaction and an esterification reaction. Compared with the mother compound AKBA before chemical modification, the six compound, of which the structure are represented as the formulas (II-VII), can inhibit division and cell proliferation of keratinocyte in in-vitro experiments and can treat the psoriasis on mice more effectively in a live animal test. The new compounds can be used for preparing the medicine for treating the psoriasis.

The invention discloses pentacyclic triterpene saponin compounds with anti-breast cancer activity in spina gleditsiae and an extraction method thereof. The extraction method comprises the following steps: (1) grinding spina gleditsiae, and using an organic extracting agent to carry out heating reflux extraction and concentration to obtain a crude extract of spina gleditsiae; (2) dispersing the crude extract obtained in the step (1) into water, extracting the crude extract by petroleum ether and ethyl acetate in sequence to obtain a water phase, and concentrating the water phase to obtain a water phase part; (3) diluting obtained water phase part by water, making diluted water phase part go through an adsorbent resin chromatographic column to carry out adsorption, then eluting the adsorbent resin chromatographic column by an ethanol-water system in a gradient elution mode, and concentrating each elution part until no water is left; (4) making the 60% ethanol-water elution part go through a silica gel chromatographic column to carry out adsorption, and eluting the silica gel chromatographic column by a CH2Cl2-MeOH system in a gradient elution mode; and (5) making the elution part with a volume ratio of CH2Cl2 to MeOH of 1:1 go through a RP-C18 medium pressure chromatographic column, eluting the RP-C18 medium pressure chromatographic column by a methanol-water system in a gradient elution mode, and saving the 80% methanol-water elution part to prepare spina gleditsiae saponin A by using CH3CN/H2O (26:74 v/v).

The invention discloses a series of 3-(L-phenylalanine)-pentacyclic triterpene derivatives as well as a synthetic method and an application thereof. The pentacyclic triterpene derivatives comprise two3-(L-phenylalanine)-oleanolic acid derivatives and two 3-(L-phenylalanine)-glycyrrhetinic acid derivatives, specially, one 3-(L-phenylalanine)-oleanolic acid derivative or one 3-(L-phenylalanine)-glycyrrhetinic acid derivative is obtained from oleanolic acid/glycyrrhetinic acid, Boc-L-phenylalanine, dicyclohexylcarbodiimide and 4-dimethylaminopyridine by a reaction and subjected to a reaction with trifluoroacetic acid, and the other two derivatives are obtained. In-vitro test results prove that the 3-(L-phenylalanine)-pentacyclic triterpene derivatives have good proliferation inhibition activity on certain tumor cell lines, have better potential medicinal values and are expected to be applied to preparation of various antitumor drugs.

The invention discloses application of pentacyclic triterpene compounds to preparation of medicine for treating adiposis and weight losing functional food. The pentacyclic triterpene compounds comprise pedunculoside and rotundic acid. The compounds have higher inhibition effect on lipase. Compared with synthetic medicine of Orlistat, the pentacyclic triterpene compounds have the advantages that the effect is mild; no irritation effect exists on the gastrointestinal tracts; the medicine is suitable for being taken for a long time.

The invention discloses a polyglycosidated pentacyclic triterpene-28-acid, and a preparation method and an application thereof. The water solubility of polyhydroxypentacyclic triterpene-28-acid is further enhanced on the basis of maintaining or improving the activity of the polyhydroxypentacyclic triterpene-28-acid, and a plurality of glycosyl groups are introduced to the hydroxyl position of polyhydroxypentacyclic triterpene-28-acid and are glycosidated to synthesize a series of the polyglycosidated pentacyclic triterpene-28-acid with good water solubility. Researches show that like compounds have good in vitro alpha-glucosidase inhibition activity. The invention provides a method for screening an alpha-glucosidase inhibitor with the advantages of good water solubility, high inhibition activity, mild effects and small toxic and side effects. The screening method can be widely used in subsequent anti-diabetic clinic fields.

At least five classes of MNP-based compounds have been demonstrated to form supramolecular particles for effective delivery by injection or topically of different types of therapeutic, prophylactic, or diagnostic agents. These compounds are isolated from natural sources such as plants. Exemplary MNP-based compounds, from which synthetic analogs or derivatives are made and appreciated to function similarly, e.g., capable of forming supramolecular particles include diterpene resin acids (e.g., abietic acid and pimaric acid), phytosterols (e.g., stigmasterol and β-sitosterol), lupane-type pentacyclic triterpenes (e.g., lupeol and betulinic acid), oleanane-type pentacyclic tritepenes (e.g., glycyrrhetic acid and sumaresinolic acid), and lanostane-type triterpenes and derivatives (e.g., dehydrotrametenolic acid and poricoic acid A). In some cases the MNP-based compounds are therapeutically effective in the absence of added therapeutic, prophylactic or diagnostic agent. Betulinic acid (BA) NPs were capable of efficiently penetrating ischemic brains and effectively promoting functional recovery as antioxidant agents.

The invention specifically relates to a method for separating high-purity saponin monomers from tea seeds, belonging to the field of separation and purification of natural compounds. In particular, the method involves separation and purification of six high-purity pentacyclic triterpene oleanane saponins in tea seeds. Compared with the prior art, the method provided by the invention has the following beneficial effects: (a) the purity of the compounds are high, as high as 91 to 99%; (b) separation process is simple, and six main monomeric saponin substances in tea seeds can be obtained at thesame time; and (c) the method has good repeatability and is well targeted.

The present invention relates to a composition comprising at least one pentacyclic triterpene or one of the pharmaceutically acceptable salts thereof for use in the treatment and/or prevention of vitiligo.

The invention discloses a series of 28-(L-phenylalanine)-pentacyclic triterpene derivatives as well as synthesis methods and application thereof. The pentacyclic triterpene derivatives particularly comprises two 28-(L-phenylalanine)-oleanolic acid derivatives, two 28-(L-phenylalanine)-ursolic acid derivatives and two 28-(L-phenylalanine)-glycyrrhetinic acid derivatives. Shown by results of in vitro tests by the applicant, the derivatives have favorable proliferation inhibition activity to certain tumor cell strains, have better potential medicinal value, and are expected to be used for preparing various anti-tumor drugs.