Nicholas Farnsworth

The Ohio State University | OSU · Department of Anthropology

Several new and known sesquiterpene lactones (SQLs) were isolated from Piptocoma rufescens Cass. (Asteraceae) using column chromatography guided by cytotoxicity to HT-29 cells. The structures of the SQLs were established from translation of their IR, UV, NMR, and mass spectra, and the absolute configurations were determined by analysis of a combina...

ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.

Three new biflavonoids to which we have accorded the trivial names calycopterone (1), isocalycopterone (2), and 4-demethylcalycopterone (3) and the known flavone 4',5-dihydroxy-3,3',6,7-tetramethoxyflavone (4) were isolated as cytotoxic constituents from the flowers of Calycopteris floribunda Lamk. (Combretaceae). Compounds 1-3 showed a wide range...

ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.

ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.

ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.

ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.

ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.

ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.

Abstract From samples of Muntingia calabura leaves and stems of Thai origin were obtained the cytotoxic flavonoids chrysin, 2′, 4′-dihydroxychalcone, and galangin 3, 7-dimethyl ether. These compounds were active against one or more of a panel of human and murine cell lines. Also isolated were the inactive compounds, 5, 7-dihydroxy-8-methoxyflavonol...

The dried ripe fruit of Vitex agnus-castus L. (VAC) is widely used for the treatment of premenstrual syndrome (PMS). A previous study reported that extracts of VAC showed affinity to opiate receptors; however, functional activity was not determined. We tested two different VAC extracts in receptor binding and functional assays. Our objectives were:...

As the population ages, there is an ever-increasing need for therapeutic agents that can be used safely and efficaciously to manage symptoms related to postmenopausal estrogen deficiency. Endogenous estrogens, e.g., 17beta-estradiol, of exogenous mammalian origin, e.g., horses, have long been used to manage such symptoms. There are more than 20 dif...

Botanical dietary supplements, as compared with nutritional supplements or single-component pharmaceutical drugs, are typically less-refined preparations derived from bulk plant material and, as such, require a modified approach to their development, production, and evaluation. An integrated, multidisciplinary team of scientific and clinical invest...

A methanol extract of chaste-tree berry (Vitex agnus-castus L.) was tested for its ability to displace radiolabeled estradiol from the binding site of estrogen receptors alpha (ERalpha) and beta (ERbeta). The extract at 46 +/- 3 microg/ml displaced 50% of estradiol from ERalpha and 64 +/- 4 microg/ml from ERbeta. Treatment of the ER+ hormone-depend...

We present the results of an antimycobacterial screening of 270 Peruvian plant samples representing 216 species from 171 genera in 63 families. Dichloromethane extracts were tested at a concentration of 50 microg/ml for inhibition of Mycobacterium tuberculosis in radiometric culture. Slightly more than half of the samples tested showed inhibition o...

Traditional taxonomic methods of botanical identification that rely primarily on morphological observations cannot be used efficiently when only powdered plant materials are available. Thus, our objectives were to determine if we could apply a molecular approach to: a) produce unique DNA profiles that are characteristic of the species, and b) deter...

A high-performance liquid chromatographic method with photodiode array detection was developed for the detection of the presence of colchicine in commercial ginkgo products. The method is based on the baseline separation of constituents in ginkgo samples plus reference colchicine. The minimal detectable concentration of colchicine is 1.0 ng on colu...

Study plots totaling 0.2 Ha were established in primary forest in the highlands of central Palawan Island, Philippines. Samples of various anatomical parts [typically leaf + twig (If/tw), stem bark (sb), and root (rt)] were collected from all tree species represented within the plots by individuals having a diameter at breast height > or = 10 cm. I...

Bioassay-guided fractionation of an ethyl acetate-soluble extract from the whole plants of Broussonetia papyrifera, using an in vitro aromatase inhibition assay, led to the isolation of five new active compounds, 5,7,2',4'-tetrahydroxy-3-geranylflavone (1), isogemichalcone C (8), 3'-[gamma-hydroxymethyl-(E)-gamma-methylallyl]-2,4,2',4'-tetrahydroxy...

Fractionation of a methanol extract of the roots of Licania intrapetiolaris, as directed by activity against the KB assay, has led to the isolation of two novel clerodane diterpenoids, intrapetacins A (1) and B (2), and the known triterpenoid cucurbitacin B (3). The structures of 1 and 2 were deduced from one- and two-dimensional NMR experiments, i...

Bioassay-guided investigation of the twigs of Ochanostachys amentacea using LNCaP (hormone-dependent human prostate cancer) cells as a monitor led to the isolation of three alkynes, the known (S)-17-hydroxy-9,11,13,15-octadecatetraynoic acid (minquartynoic acid, 1) and two novel analogues, (S)-17,18-dihydroxy-9,11,13,15-octadecatetraynoic acid (2)...

A survey of plants used ethnomedically against cancer was undertaken, using the NAPRALERT database currently maintained by the Program for Collaborative Research in the Pharmaceutical Sciences, College of Pharmacy, University of Illinois-Chicago. We report over 350 species which are reported to be used against cancer and not cited in the work of Jo...

Atropine, camptothecin, cocaine, digitoxin, digoxin, morphine, pilocarpine, quinine, taxol, vinblastine and vincristine, among others, are important drugs obtained from higher plants and are used clinically. They have also served as lead compounds for the synthesis and modification of more effective and safer drugs, in many cases. In this chapter,...

An ethyl acetate-soluble extract of the combined leaves and twigs of Thuja occidentalis was found to inhibit 12-O-tetradecanoylphorbol 13-acetate (TPA)-induced ornithine decarboxylase (ODC) in cultured mouse epidermal ME 308 cells. Bioassay-guided fractionation of this extract led to the isolation of six active constituents (1-6), namely, (+)-7-oxo...

Bioactivity-directed fractionation of the CHCl(3) extract of the roots of Ekmanianthe longiflora resulted in the isolation of three new natural products, (2R,3R,4R)-3,4-dihydro-3, 4-dihydroxy-2-(3-methyl-2-butenyl)-1(2H)-naphthalenone (1), (2S,3R, 4R)-3,4-dihydro-3, 4-dihydroxy-2-(3-methyl-2-butenyl)-1(2H)-naphthalenone (2), and (2R, 3aR,9R,9aR)-9-...

A new coumarin, 5-(4-hydroxyphenethenyl)-4,7-dimethoxycoumarin (1) was isolated from the combined ethyl acetate extracts of the root bark, root wood and stem bark of Monotes engleri, and found to be cytotoxic against two cell lines in a human tumor panel. Its structure was determined on the basis of spectroscopic methods.

From the leaves of Isodon megathyrsus, a novel ent-kaurene diterpene, megathyrin B, was isolated and its structure determined as 1 alpha,7 beta,11 beta,15 beta-tetrahydroxy-ent-7 alpha,20-epoxy-kaur-16-ene by 1D- and 2D-NMR spectral analysis. Additionally, its stereochemistry was unambiguously assigned by X-ray crystallography. This compound was cy...

We currently describe a programmatic effort to discover novel natural product cancer chemopreventive agents, i.e., agents capable of preventing, inhibiting or reversing the process of carcinogenesis. Employing a panel of bioassays reflective of modulating carcinogenesis at the stages of initiation, promotion or progression, and a mouse mammary orga...

EEG data were recorded under field conditions from 11 members of the Santo Daime Doctrine, a Brazilian shamanistic religion, before and after ingesting the psychoactive alkaloid preparation, ayahuasca, or daime, as they term it. Post-ingestion, we observed increases in power in the 36-44 Hz frequency band ("40 Hz") from the left occipital-temporal-...

Recent studies on biologically active natural products

An extract of a leaf and twig sample from Swintonia foxworthyi demonstrated weak in vitro activity against two clones of Plasmodium falciparum. At the same time, the extract was inactive in cancer cell cytotoxicity assays. Bioassay-directed fractionation led to the isolation of methyl gallate as the principal antiplasmodial constituent; the compoun...

From the leaves of Monotes engleri, five prenylated flavanones were isolated as constituents that displayed cytotoxic activity against several human cancer cell lines. There of these substances are novel, namely, 6-(1,1-dimethylallyl)naringenin, 6-(1,1-dimethylallyl)eriodictyol and 3'-O-methyl-6-(1,1-dimethylallyl)-eriodictyol, with the other two a...

Resveratrol, a phytoalexin found in grapes and other food products, was purified and shown to have cancer chemopreventive activity in assays representing three major stages of carcinogenesis. Resveratrol was found to act as an antioxidant and antimutagen and to induce phase II drug-metabolizing enzymes (anti-initiation activity); it mediated anti-i...

Utilizing the hepatitis B virus (HBV)-producing hepatoblastoma cell line, HepG2.2.15, which is stably transfected with the cloned HBV genome, methods were devised to examine the effects of test substances on intracellular extrachromosomal HBV DNA levels and secretion of hepatitis B surface antigen (HBsAg). The known inhibitor of HBV replication, di...

Ethyl acetate and aqueous extracts of tannin-containing topoisomerase inhibitory plant samples were subjected to one or more of seven tannin removal procedures, and the resulting products were subsequently evaluated for topoisomerase inhibitory activity. In most of the samples investigated, the initial activity was lost after tannin removal. It was...

Diabetes mellitus is a debilitating and often life-threatening disease with increasing incidence in rural populations throughout the world. A scientific investigation of traditional herbal remedies for diabetes may provide valuable leads for the development of alternative drugs and therapeutic strategies. Alternatives are clearly needed because of...

Four cytotoxic lignans were isolated from the stem bark of Bursera permollis (Burseraceae), namely, deoxypodophyllotoxin (1), beta-peltatin methyl ether (2), picro-beta-peltatin methyl ether (3), and dehydro-beta-peltatin methyl ether (4). Also isolated was the inactive lignan, nemerosin (5). Compounds 1 and 2 were potently cytotoxic when evaluated...

Three cytotoxic clerodane diterpenes were purified from an ethyl acetate-soluble extract of the stem bark of Polyalthia barnesii, namely, 16 alpha-hydroxycleroda-3,13(14)Z-dien-15,16-olide, a known compound, and two novel compounds, 3 beta, 16 alpha-dihydroxycleroda-4(18),13(14)Z-dien-15,16-olide and 4 beta, 16 alpha-dihydroxyclerod-13(14)Z-en-15,1...

Three cytotoxic clerodane diterpenes were purified from an ethyl acetate-soluble extract of the stem bark ofPolyalthia barnesii, namely, 16α-hyd

By means of activity-directed chromatographic fractionation using cultured astrocytoma (ASK) cells, six dibenzocyclo-octadiene lignans were isolated from Steganotaenia araliacea stem bark. In addition to the most abundant analogue, steganangin [1], two other known compounds, steganacin [3] and steganolide A [6], and three new compounds, episteganan...

NAPRALERT (Natural Products ALERT) is a specialized database which contains information derived from the literature on medicinal folklore, biological activity, and the chemistry of organisms of potential or actual pharmaceutical interest: plants make up about 75 per cent of the organisms included. The database is relational in design and is managed...

Five known cardenolides, digitoxigenin (1), oleandrigenin (2), digitoxigenin alpha-L-cymaroside (3), digitoxigenin beta-gentiobiosyl-alpha-L-cymaroside (4), and delta 16-digitoxigenin beta-D-glucosyl-alpha-L-cymaroside (5), were isolated from the stems of Beaumontia brevituba Oliver by cytotoxicity-directed fractionation monitored by a cultured hum...

By random screening test, Marsdenia koi was found to have antifertility activity on SD rat. From MeOH extracts of this plant two steroidal glycosides, marsdekoiside A and B, were isolated, and their structures were elucidated on the basis of spectral evidence and by comparison of the hydrolysis products with the authentic samples. Both are newly id...

By random screening test, Marsdenia koi was found to have antifertility activity on SD rat. From MeOH extracts of this plant two steroidal glycosides, marsdekoiside A and B, were isolated, and their structures were elucidated on the basis of spectral evidence and by comparison of the hydrolysis products with the authentic samples. Both are newly id...

A new diarylheptanoid, casuarinondiol, and two known compounds, alnusdiol (a further diarylheptanoid) and (±)-lyoniresinol 2α-O-rhamnoside (a lignan), have been isolated from the roots ofCasuarina junghuhniana and characterized spectroscopically. These are the first representatives of these compound classes to have been obtained from a plant in the...

Following bioassay-directed fractionation procedures, two 7-oxygenated-8-prenylflavones, (-)-pseudosemiglabrin [1] and (-)-semiglabrin [2], were isolated from an MeOH extract of Tephrosia semiglabra. (-)-Pseudosemiglabrin [1] displayed in vitro inhibitory effects on human platelet aggregation.

Further bioactivity-guided fractionation of a chloroform extract of the twigs of Agrostistachys hookeri against cultured P-388 lymphocytic leukemia cells, has led to the isolation of a cytotoxic ellagic acid derivative, 3,3′,4-O-trimethylellagic acid (1), and three inactive compounds, consisting of a new compound, 3,4,5,5′-O-tetramethyl-3′,4′-O,O-m...

Bull. Chem. Soc. Ethiop., 3(2), 91-96 (1989).

Plant-derived drugs are of major importance to the health and well-being of mankind. Although many of these useful drugs have been synthesized, very few are produced commercially by synthesis. Thus, the plant source remains extremely important, not only in producing drugs, but in providing novel biologically active model compounds from which potent...

A new sesquiterpene acid, cyperenoic acid, has been isolated, together with acetylaleuritolic acid, chettaphanin-I, and β-amyrin, from the root part of Croton crassifolius. On the basis of chemical and spectral evidence, the structure of cyperenoic acid was established as 2.

In addition to the previously characterized agrostistachin, three additional cytotoxic macrocyclic casbane-type diterpenes were isolated from a CHCl3 extract of Agrostistachys hookeri, by bioactivity-guided fractionation using the P-388 lymphocytic leukemia cell culture system. These novel compounds, 14-dehydroagrostistachin, 17-hydroxyagrostistach...

Agrostistachin, a cytotoxic constituent of , was characterized as a new member of the rare casbane class of diterpenoids. The structure and stereochemistry of this compound were established by analysis of its spectral and X-ray crystallographic parameters.

4′-Demethyldeoxypodophyllotoxin was isolated as the sole cytotoxic constituent of a chloroform-soluble extract of the stem bark of Amanoa oblongifolia. Also identified from this extract were a number of noncytotoxic isolates that comprised the lignans, (+)-sesamin and paulownin, the triterpenes, friedelin, canophyllol, betulin, betulinic acid, and...

An antileukemic quassinoid simalikalactone D (17) and two anticancer phenolic compounds, emodin and tricin, were isolated from the wood of Simaba multiflora (Simaroubaceae) as well as 8-hydroxycanthin-6-one (18) and coumarin. The constituents of the genus Simaba are reviewed. 1 For paper XXXIV in this series see ref. 1 2 These data were first pre...

Research in natural products, not unlike many other fields of investigation, requires access to large amounts of prior experimental data relevant to specific projects. The most efficient method of identifying and analyzing these data currently employs computer handling of the information. The NAPRALERT database has been designed to meet this need r...

1H-nmr spectra of the natural products cucurbitacins A, B, C, D, E, F, I, L, 23, 24-dihydrocucurbitacin F, and hexanorcucurbitacin F, as well as three acetylated derivatives, were measured at 360 MHz in pyridine-d5. Chemical shifts and coupling constants were tabulated. In addition to all of the ring and side-chain protons, it was possible to assig...

Several quassinoids, obtained by isolation and derivatization from Simaba multiflora and Soulamea soulameoides, were evaluated for growth inhibitory and insecticidal effects against the tobacco budworm (Heliothis virescens) and for antifeedant effects against H. virescens and the fall armyworm (Spodoptera frugiperda). The relative activity of the q...

Two lignans of known structure, (+)-syringaresinol, a cytotoxic agent, and (+)-nortrachelogenin, a compound with demonstrated antileukemic activity, were isolated from a biologically active extract of the stems of Passerina vulgaris. 1 For the previous paper in this series, see reference (1)

Caraipa densifolia Mart. (Clusiaceae) has afforded the new lupene derivative 3 beta-hydroxy-28-p-coumarolyoxy-lup-20(29)-en-27-oic acid (8), whose structure was deduced by chemical correlation with betulin (6). Simiarenol (1), taraxerone (2), friedelin (3), lupeol (4), betulinic acid (5), betulin (6), and beta-sitosterol-beta-D-glucoside (7) were a...

Two novel cytotoxic compounds, 12-O-undecadienoylphorbol-13-acetate (1) and ostodin (2), the Δ5,6-7β-hydroperoxide derivative of 1, were isolated from a chloroform extract of the stems and fruits of Ostodes paniculata (Euphorbiaceae). Ostodin (2) was shown to be an autooxidation product of 1 and, hence, probably was obtained in this investigation a...

This report reviews research on plant-derived agents that prevent sperm production if taken orally by the male or that incapacitate or kill sperm on contact if used vaginally by the female. It would be of great value to develop fertility inhibitors that are totally selective for reproductive systems and enzymes, and there is a possibility that a pl...

The known withanolide nicandrenone (1) is primarily responsible for the in vitro cytotoxicity of extracts prepared from Nicandra physalodes (Solanaceae).

Roylean Podophyllum specimens mounted on sheet no. 13/1 in deposit at the Merseyside County Museums (LIV), Liverpool (Great Britain), has been identified and designated as the lectotype of Podophyllum hexandrum Royle.

An aqueous extract of the flowering tops of Strumpfia maritima exhibited antifertility activity in female rats. The extract also contained the flavonol glycoside narcissin. This article represents the first reported isolation of this flavonoid from the Rubiaceae, as well as the first reported phytochemical and pharmacological investigation of the g...

A method is described for the analysis of stevioside and rebaudioside A from Stevia rebaudiana Bert. These compounds were hydrolyzed to steviolbioside and rebaudioside B, respectively, and reacted with p-bromophenacyl bromide and crown reagent to yield the corresponding chromophoric esters, which were separated and quantitated by high-performance l...

The cytotoxic activity of extracts of Asclepias albicans (Asclepiadaceae) was traced to uzarigenin (2), desglucouzarin (3) and a new cardenolide glycoside, uzarigenin 3-O-β-D-glucopyranosyl (1→4)-β-D-glucopyranoside (4). The latter compound also displayed significant antitumor activity against P-388 lymphocytic leukemia.