Abstract: This disclosure is related to halonium compounds useful for cyclization of polyenes, alkenoic acids, and alkenyl alkyl ethers, and halogenation of aromatic compounds. The synthesis of such halonium compounds, compounds made using such halonium compounds, and synthesis of natural compounds, including decalins, using the halonium compounds is also disclosed.

Abstract: Improved processes for the extraction of quassinoids such as quassin and neoquassin from natural substances containing these compounds are described. The process uses compounds that are Generally Recognized As Safe by the U.S. Food and Drug Administration. In a first embodiment, the process includes a sonication method using water and no organic solvent. The process is highly efficient and comprises fewer steps than other processes known in the art. In a second embodiment, a method of extracting quassinoids from natural substance comprising bark of a plant of the plant family Simaroubaceae is also disclosed. In a third embodiment, indirect sonication of quassinoids is described using a mixture of polar and non-polar organic solvents.

Abstract: A means for the extraction and crystallization of quassinoids such as quassin and neoquassin from natural sources containing these compounds, using compounds that are Generally Recognized As Safe by the U.S. Food and Drug Administration is provided. In particular, a means for extraction that does not require use of lead acetate, chloroform, methanol, or diethyl ether is provided. The process includes a means of removing non-polar and very polar substances from an extracted residue to enhance crystallization of quassinoids from the residue.

Abstract: The present invention discloses the utility of factions and compounds from Polygonum chinense Linn in anti-diarrhea. The invention also includes their preparation and application method for anti-diarrhea treatment.

Abstract: Pharmaceutical or dermo-cosmetic compositions for topical and intravaginal application for treatment of human and veterinary affections caused by anaerobic organisms or parasites are provided comprising quassinoids or plant extracts containing these phytochemicals, in effective amounts. Such compositions can be administered topically or intravaginally to patients in need thereof in various pharmaceutical dosage forms.

Abstract: A novel chemical moiety triterpenoid AECHL-1 isolated from root bark of Ailanthus excelsa having the structure:

Abstract: The invention relates to the use of one or more compounds selected from ellagic acid, ethers thereof, ellagic acid salts and ellagic acid ether salts, as an anti-dandruff agent; and to a cosmetic treatment method associated with such a use.

Abstract: This invention relates to compounds which selectively bind to the survival protein MCL-1 with high affinity and selectivity, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for modulating MCL-1 activity and for treating hyperproliferative disorders, angiogenesis disorders, cell cycle regulation disorders, autophagy regulation disorders, inflammatory disorders, and/or infectious disorders and/or for enhancing cellular engraftment and/or wound repair, as a sole agent or in combination with other active ingredients.

Abstract: A means for the extraction and crystallization of quassinoids such as quassin and neoquassin from natural sources containing these compounds, using compounds that are Generally Recognized As Safe by the U.S. Food and Drug Administration is provided. In particular, a means for extraction that does not require use of lead acetate, chloroform, methanol, or diethyl ether is provided. The process includes a means of removing non-polar and very polar substances from an extracted residue to enhance crystallization of quassinoids from the residue.

Abstract: Catalytic processes for the production of carnosol from carnosic acid using hydrogen peroxide or a peracid are presented. The carnosic acid may be in pure form, in an impure form, part of a plant extract, or may be present in rosemary needles. The catalyst may be iron, iron salts, a minor amount of water, rosemary needles, or a mixture thereof.

Abstract: Novel catalytic processes for the production of carnosol from carnosic acid using hydrogen peroxide or a peracid are presented. The carnosic acid may be in pure form, in an impure form, part of a plant extract, or may be present in rosemary needles. The catalyst may be iron, iron salts, a minor amount of water, rosemary needles, or a mixture thereof.

Abstract: The present invention refers to carnosol and rosmanol for use (as medicament) in the treatment of a disorder connected to reduced neurotransmission, cognitive dysfunction and/or symptoms caused by headache and/or migraine, as well as to dietary and pharmaceutical compositions and their uses.

Abstract: A means for the extraction and crystallization of quassinoids such as quassin and neoquassin from natural sources containing these compounds, using compounds that are Generally Recognized As Safe by the U.S. Food and Drug Administration is provided. In particular, a means for extraction that does not require use of lead acetate, chloroform, methanol, or diethyl ether is provided. The process includes a means of removing non-polar and very polar substances from an extracted residue to enhance crystallization of quassinoids from the residue.

Abstract: Provided are compositions comprising compounds or precursors to compounds which may be used for a variety of therapeutic applications including, for example, treating and/or preventing a disease or disorder related to reduced or inadequate mitochondrial activity, including aging or stress, diabetes, obesity, and neurodegenerative diseases. The compounds relate generally to urolithins and precursors thereof, including but not limited to ellagitannins and urolithin A. In certain embodiments the compositions are presented in or as food products or nutritional supplements. These same compounds and compositions can also be used advantageously in generally healthy individuals to increase or maintain metabolic rate, decrease percent body fat, increase or maintain muscle mass, manage body weight, improve or maintain mental performance (including memory), improve or maintain muscle performance, improve or maintain mood, and manage stress.

Abstract: Carnosol can be crystallized from a plant extract by contacting the extract with acetic acid, and collecting the crystals so formed.

Abstract: Catalytic processes for the production of carnosol from carnosic acid using hydrogen peroxide or a peracid are presented. The carnosic acid may be in pure form, in an impure form, part of a plant extract, or may be present in rosemary needles. The catalyst may be iron, iron salts, a minor amount of water, rosemary needles, or a mixture thereof.

Abstract: Novel compounds and methods for activating the TrkB receptor are provided. The methods include administering in vivo or in vitro a therapeutically effective amount of a compound containing four six-membered rings and a substituted or unsubstituted C5 or C6 heteroaryl or hetero-cycloalkyl ring and pharmaceutically acceptable salts, prodrugs, and derivatives thereof. Specifically, methods and compounds for the treatment of disorders including neurologic, neuropsychiatric, and metabolic disorders are provided. For example, a method is provided of treating or reducing the risk of depression, anxiety, or obesity in a subject, which includes selecting a subject with or at risk of developing depression, anxiety, or obesity, and administering to the subject a therapeutically effective amount of the described compounds.

Abstract: Disclosed is a composition for modulating the release of a neurotransmitter, which includes naturally extracted polyphenols as an active ingredient. The disclosed composition suppresses the formation of a SNARE complex, thereby modulating the release of a neurotransmitter, and thus can be used as a modulator for a reaction within a cell related to the SNARE complex. Such an inhibitor of the SNARE complex formation can be used as a composition for reducing wrinkles and relieving pain.

Abstract: Compositions of purified and biologically active ellagitannins are provided by separation from pomegranate husk using a method of extraction and purification using a solid polymeric adsorbent and the uses of the said compounds.

Abstract: Aspects of the invention relate to compounds, extracts and compositions thereof, and methods of using of the same, to treat neurodegenerative disorders and/or improve brain health. In certain embodiments, said compounds are pomegranate flavonoids.

Abstract: Compositions of purified and biologically active ellagitannins are provided by separation from pomegranate husk using a method of extraction and purification using a solid polymeric adsorbent and the uses of the said compounds.

Abstract: Compositions and methods for maintenance of bone health or prevention, alleviation and/or treatment of bone disorders are presented. The present invention also provides the manufacture of a nutritional product, a supplement or a medicament for promoting bone growth or for the maintenance of bone health and methods regarding same. In an embodiment, the present invention provides a composition comprising an active ingredient having an effective amount of a plant or plant extract containing at least one phytochemical having the ability to induce bone morphogenic protein expression.

Abstract: A novel chemical moiety triterpenoid AECHL-1 isolated from root bark of Ailanthus excelsa having anti-cancer properties exhibiting remarkable activity in treatment of various forms of tumors with specificity wherein it blocks the growth of four tumor cell lines with distinct origins and of different p53 status (B16F10 mouse melanoma, PC3 human prostate cancer, MCF-7 and MDA-MB-231 human breast cancer), having following characteristic IR, NMR and mass spectra IR (KBr): 3425, 3419 (hydroxyl group), 2972, 2966, 2923, 2873 (alkyl C—H stretch), 1733 (? lactone), 1718 (Bi acetyl), 1680 (C?O conjugation with alkene), 1652 (—C?C stretching), 1600 (aromatic), 1492, 1454, 1394 (methyl stretching), 1222 (? lactone), 1184, 1110, 1051, 1031 (acetals), 1018 nm (alkanes). 1H-NMR (DMSO, 400 Hz) ?: 0.95 (3H, t, 4?-CH3), ?:1.15 (3H, d, H-24), ?:1.235 (3H, d, 5?-CH3), ?: 1.5 (2H, ddd, 5?-CH2), ?: 1.73 (3H, ddd, H-21), ?: 1.83 (1H, s, H-9), ?: 1.87 (1H, s, H-14), ?: 1.9 (2H, s, H-18), ?: 2.16 (3H, s, H-18), ?: 2.

Abstract: Novel catalytic processes for the production of carnosol from carnosic acid using hydrogen peroxide or a peracid are presented. The carnosic acid may be in pure form, in an impure form, part of a plant extract, or may be present in rosemary needles. The catalyst may be iron, iron salts, a minor amount of water, rosemary needles, or a mixture thereof.

Abstract: The present invention refers to carnosol and rosmanol for use (as medicament) in the treatment of a disorder connected to reduced neurotransmission, cognitive dysfunction and/or symptoms caused by headache and/or migraine, as well as to dietary and pharmaceutical compositions and their uses.

Abstract: Compositions of purified and biologically active ellagitannins are provided by separation from pomegranate husk using a method of extraction and purification using a solid polymeric adsorbent and the uses of the said compounds.

Abstract: A means for the extraction and crystallization of quassinoids such as quassin and neoquassin from natural sources containing these compounds, using compounds that are Generally Recognized As Safe by the U.S. Food and Drug Administration is provided. In particular, a means for extraction that does not require use of lead acetate, chloroform, methanol, or diethyl ether is provided. The process includes a means of removing non-polar and very polar substances from an extracted residue to enhance crystallization of quassinoids from the residue.

Abstract: A molecular conjugate is provided having the formula: wherein R1 is a de-hydroxyl or de-amino moiety respectively of a hydroxyl-bearing or amino-bearing biologically active molecule or an analog or derivative thereof, and Z is —O— or —NH—, respectively, Y is a straight or branched alkyl having 1 to 20 carbons that may be optionally substituted with one or more phenyl, a cycloalkyl optionally substituted with one or more alkyl or phenyl, or an aromatic group optionally substituted with one or more alkyl groups, electron-withdrawing groups, or electron-donating groups; and R2 is —CH?CH(W), —CH(OH)CH(OH)W, or —C(O)H, where W can be H, a straight or branched alkyl having 1 to 20 carbons that may be optionally substituted with one or more phenyl, a cycloalkyl optionally substituted with one or more alkyl or phenyl, or an aromatic group optionally substituted with one or more alkyl groups, electron-withdrawing groups, or electron-donating groups.

Abstract: Dibenzonaphthyrone of formula (I) 1

Abstract: The present invention provides novel antiviral compounds, refered to as calanolides, related compounds, and their derivatives, which may be isolated from plants, or derived from compounds from plants, of the genus Calophyllum in accordance with the present inventive method. The compounds and their derivatives may be used alone or in combination with other antiviral agents in compositions, such as pharmaceutical compositions, to inhibit the growth or replication of a virus, such as a retrovirus, in particular a human immunodeficiency virus, specifically HIV-1 or HIV-2.

Abstract: Calanolide analogues that demonstrate potent antiviral activity against many viruses are provided. Also provided is a method of using calanolide analogues for treating or preventing viral infections. The calanolide analogues provided are obtained via syntheses employing chromene 4 and chromanone 7 as key intermediates.

Abstract: A sulphamate compound suitable for use as an inhibitor of both oestrone sulphatase activity and aromatase activity. The compound can have the general formula (II) wherein F represents a phenolic ring structure (the first ring structure), J represents the third ring structure; I represents a phenolic ring structure (the second ring structure), G is an optional double bond, H is a link joining the second ring structure to the third ring structure, and Y represents a suitable second group; wherein any one of ring structures F, J and I has bound thereto a sulphamate group.

Abstract: A method of preparing (.+-.)-calanolide A, 1, a potent HIV reverse transcriptase inhibitor, from chromene 4 is provided. Useful intermediates for preparing (.+-.)-calanolide A and its derivatives are also provided. According to the disclosed method, chromene 4 intermediate was reacted with acetaldehyde diethyl acetal or paraldehyde in the presence of an acid catalyst with heating, or a two-step reaction including an aldol reaction with acetaldehyde and cyclization either under acidic conditions or neutral Mitsunobu conditions, to produce chromanone 7. Reduction of chromanone 7 with sodium borohydride, in the presence of cerium trichloride, produced (.+-.)-calanolide A. A method for resolving (.+-.)-calanolide A into its optically active forms by a chiral HPLC system or by enzymatic acylation and hydrolysis is also disclosed. Finally, a method for treating or preventing a viral infections using (.+-.)-calanolide or (-)-calanolide is provided.

Abstract: Described are novel photochromic six-membered heterocyclic-fused naphthopyran compounds, examples of which are naphthopyran compounds having a substituted or unsubstituted six-membered heterocyclic group fused to one side of the naphtho portion of the naphthopyran and having certain substituents at the position ortho to the oxygen atom of the naphthopyran ring. These compounds may be represented by the following graphic formula: ##STR1## Also described are polymeric organic host materials that contain or that are coated with such compounds or combinations thereof with complementary photochromic compounds, e.g., certain other naphthopyrans, benzopyrans, and spiro(indoline) type compounds.

Abstract: A method of preparing (+)-calanolide A, 1, a potent HIV reverse transcriptase inhibitor, from chromene 4 is provided. According to the disclosed method, chromene 4 intermediate was subjected to a chlorotitanium-mediated aldol reaction with acetaldehyde to selectively produce (.+-.)-8a. Separation and enzyme-mediated resolution of (.+-.)-8a produced (+)-8a. Cyclization of (+)-8a under neutral Mitsunobu conditions followed by Luche reduction of (+)-7 produced (+)-calanolide A in high yield and enantiomeric purity. The method of the invention has been extended to produce potent antiviral calanolide A analogues.

Abstract: A method of preparing (+)-calanolide A, 1, a potent HIV reverse transcriptase inhibitor, from chromene 4 is provided. According to the disclosed method, chromene 4 intermediate was subjected to a chlorotitanium-mediated aldol reaction with acetaldehyde to selectively produce (.+-.)-8a. Separation and enzyme-mediated resolution of (.+-.)-8a produced (+)-8a. Cyclization of (+)-8a under neutral Mitsunobu conditions followed by Luche reduction of (.+-.)-7 produced (+)-calanolide A in high yield and enantiomeric purity. The method of the invention has been extended to produce potent antiviral calanolide A analogues.

Abstract: A method of synthesis of the four optically active stereoisomers of calanolide A and B which produces the compounds in high yields and in a high degree of purity.

Abstract: A method for preparing (.+-.)-calanolide A, 1, a potent HIV reverse transcriptase inhibitor, from chromene 4 is provided. Useful intermediates for preparing (.+-.)-calanolide A and its derivatives are also provided.According to the disclosed method, chromene 4 intermediate was reacted with acetaldehyde diethyl acetal in the presence of an acid catalyst with heating to produce chromanone 7. Reduction of chromene 7 with sodium borohydride, in the presence of cerium trichloride, produced (.+-.)-calanolide A, which was purified chromatographically.

Abstract: A process for producing ellagic acid comprising reacting a tannin having gallic acid residues attached as constituents with an oxidizing agent at pH 7 or higher.

Abstract: An antitumor substance BE-12406 or a pharmaceutically acceptable salt thereof, which is represented by the general formula ##STR1## and a method of producing the novel substance.

Abstract: Novel antineoplastic ailanthone derivatives (IIb) represented by the following formula wherein R.sub.2 is C.sub.5 -C.sub.18 .alpha.,.beta.-unsaturated acyl group and its related compounds are disclosed. ##STR1## Particularly, some of the above compounds are far more effective than mitomycin C against mouse lymphocytic leucemia p388.These compounds can be synthesized from known ailanthone via important intermediates, triacyloxy ailanthone, represented by the formula: ##STR2## wherein R.sub.1 is acyl group.

Abstract: The present invention relates to new bisamidine derivatives of polycyclic compounds such as 5,10-dioxo-4,5,9,10-tetrahydro-4,9-dioxapyrene-6(5H)-phenanthridone and 5,10-dioxo-4,5,9,10-tetrahydro-4,9-dioxapyrenephenanthridine and to a process for their preparation. The polycyclic bisamidines according to the invention are distinguished by valuable chemotherapeutic properties, such as, for example, an action against amoebas and trichomonads.

Abstract: Tricyclic benzo fused compounds of the formula ##STR1## and pharmaceutically acceptable cationic and acid addition salts thereof, wherein n is zero, 1 or 2, and t is 1 or 2; M is CH or N, R.sub.1 is H or certain acyl groups; Q is CO.sub.2 R.sub.4, COR.sub.5, C(OR.sub.7)R.sub.5 R.sub.6, CN, CONR.sub.9 R.sub.10, CH.sub.2 NR.sub.9 R.sub.10, CH.sub.2 NHCOR.sub.11, CH.sub.2 NHSO.sub.2 R.sub.12, 5-tetrazolyl or when n is 1, Q and OR.sub.1 together form a lactone or certain reduced derivatives thereof; and Z is certain alkyl, alkoxy, alkoxyalkyl, aralkyl, aralkoxy, aryloxyalkyl or aralkoxyalkyl groups, are valuable central nervous system active agents, methods for their use, pharmaceutical compositions containing them and certain intermediates therefor.

Abstract: 1,4-naphthoquinone derivatives represented by the following general formula: ##STR1## (wherein R.sup.1 represents a hydrogen atom, a hydroxy group, a lower alkoxy group or an arylthio group, R.sup.2 represents a carboxy group, an esterified carboxy group or an amidated carboxy group or, when taken together, R.sup.1 and R.sup.2 form a group of ##STR2## R.sup.3 represents a hydrogen atom or a lower alkyl group, R.sup.4 represents a lower alkyl group, R.sup.5 represents a hydrogen atom or a halogen atom, and R.sup.6 represents a hydrogen atom, a lower alkyl group or a lower alkanoyl group), and the salts of the carboxy group thereof, which are novel compounds having an anticoccidium activity, and which can be obtained by synthesis or, partly, by cultivation of Streptomyces auranticolor.

Abstract: A polycyclic antitumor antibiotic designated herein as anandimycin is produced by fermentation of Streptomyces anandii subsp. araffinosus strain C-22,437 (ATCC 31431). Anandimycin possesses antibacterial activity and inhibits the growth of tumors in experimental animals.