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Five new steroids, colebrin A-E (1-5) were isolated from the aerial parts of Clerodendrum colebrookianum. The structures of the new compounds were elucidated on the basis of spectral evidence.
The ethanolic extract of Clerodendrum petasites was tested to evaluate the spasmolytic activity on isolated guinea-pig tracheal smooth muscle. The crude extract (2.25-9.0 mg/ml) dose-dependently caused relaxation of tracheal smooth muscle which was contracted by exposure to histamine. A bioassay-guided fractionation of the crude extract was performed by means of partitioning and centrifugal partition chromatography. Finally the active principle was isolated and identified as the flavonoid hispidulin (EC(50): (3.0+/-0.8)x10(-5) M). These results suggest that hispidulin may be beneficial in the treatment of asthma.
A study was undertaken to evaluate the effect of methanolic extract of leaves of Clerodendrum phlomidis Linn. (MECP) (Family: Verbenaceae) for its anti-diarrhoeal potential against several experimental models of diarrhoea in Wistar albino rats. MECP showed significant inhibitory activity against castor oil induced diarrhoea and PGE2 induced enteropooling in rats. The extract also showed a significant reduction in gastrointestinal motility in charcoal meal test in rats. The results obtained establish the efficacy and substantiated the folklore claim as an anti-diarrhoeal agent.
The leaves of Clerodendrum inerme have yielded two new iridoid biglycosides which have been characterized as 2'-O-[5"-O-(8-hydroxy-2,6-dimethyl-2(E)-octenoyl)-beta-D-apiofuranosy l]- mussaenosidic acid (inerminoside A) [1], and 2'-O-[5"-O-(8-hydroxy-2,6-dimethyl-2(E),6(E)-octadienoyl)-beta-D- apiofuranosyl]-8-epi-loganic acid (inerminoside B [2]), respectively. Structure elucidation was carried out both chemically and spectroscopically.
The Clerodendrum aculeatum-systemic resistance inducing (CA-SRI) protein, a 34 kDa basic protein, plays a key role in inducing strong systemic resistance in susceptible plants against various plant viruses [22]. We have cloned the cDNA encoding the CA-SRI from C. aculeatum leaves using antibodies raised against the purified protein and degenerate oligonucleotide probes derived from microsequencing of the CA-SRI protein. The full-length cDNA consisted of 1218 nucleotides with an open reading frame of 906 bp. The deduced amino acid sequence of CA-SRI protein showed varying homology (ranging from 11 to 54%) to the ribosome inactivating proteins (RIPs) from other plant species. CA-SRI inhibited in vitro protein synthesis both in rabbit reticulocyte lysate and wheat germ lysate but not in Escherichia coli in vitro translation system. The CA-SRI open reading frame was expressed in an E. coli expression vector and the purified recombinant protein inhibited protein synthesis in rabbit reticulocyte lysate. Southern blot analysis indicated that the CA-SRI gene may be present in low copy number.
A 70% EtOH extract of Clerodendrum mandarinorum root bark was assessed for CNS activity against 18 radioligand receptor binding assays. The results showed that the extract was able to bind to opiate, adenosine-1, alpha 2-adrenergic, 5HT-1, 5HT-2, dopamine-2, histamine-1, GABA(A), and GABA(B) receptors. Fourteen compounds were isolated and identified by El-MS, 1H-NMR and 13C-NMR spectra as known triterpenoids (friedelanone, lupeol, betulinic acid), steroids (24S-stigmata-5,25-dien-3 beta-ol,22E,24S-stigmata-5,22,25-trien-3 beta-ol), flavonoids (cirsimaritin, cirsimaritin-4'-glucoside, quercetin-3-methyl ether), tetra-hydro-alpha-pyrone and saccharides (sucrose, alpha-D- and beta-D-glucopyranose, ethyl-alpha-D-glucopyranoside, 2-ethyl-beta-D-fructofuranoside). The isolated compounds were assessed for activity by the radioligand receptor binding assays. Betulinic acid and ethyl-alpha-D-glucopyranoside showed weak activities against sulphonylureas (IC50 = 7.5 microM) and muscarinic receptors (IC50 = 5.5 microM), respectively. Cirsimaritin-4'-glucoside was weakly active in the adenosine-1 binding assay (IC50 = 3.0 microM), whereas seven structurally related flavonoids, not isolated from C.mandarinorum, were inactive.
The methanolic extract of Clerodendrum phlomidis Linn. (MECP) leaves was evaluated for its psychopharmacological activities in several experimental models using Swiss albino mice and Wistar albino rats. The MECP was found to cause significant reduction in spontaneous activity, and decreases in exploratory behavioral profiles by the Y-maze and head dip test. It also showed reduction in muscle relaxant activity by rotarod, 30 degrees inclined screen and traction tests, as well as significantly potentiated the phenobarbitone sodium-induced sleeping time in the doses examined (200, 400 and 600 mg/kg body wt.). All the results were compared with respective controls for the evaluation of significance.
Colebroside A (1), a new diglucoside of fatty acid ester of glycerin, was isolated from the aerial parts of Clerodendrum colebrookianum Walp., along with nine known compounds (2-10). Their structures were elucidated by spectroscopic and chemical methods. Compounds 2, 3, 4, 5, 7, 8, 9 and 10 have been obtained from this plant for the first time.
Five new abietane derivatives which have a commonly rearranged abietane skeleton contained a 17(15-->16),18(4-->3)-diabeo-abietane framework, mandarones D-H, were isolated from the stem of Clerodendrum nmantarinorum Diels (Verbenaceae). The structures were characterized as (16S)-12,16-epoxy-11-hydroxy-17(15-->16), 18(4-->3)-diabeo-abieta-3,5,8,11,13-pentaene-7-one (mandarone D, 1), 12,16-epoxy-11,14-dihydroxy-17(15-->16),18(4-->3)-diabeo-abieta-3,5,8,11, 13,15-hexaene-7-one (mandarone E, 2), 12,16-epoxy-6,11,14-trihydroxy-17(15-->16),18(4-->3)-diabeo-abieta-3,5,8,11,13,15-hexaene-7-one (mandarone F, 3),12,16-epoxy-11,14-dihydroxy-6-methoxy-17(15-->16),18(4-->3)-diabeo-abieta-3,5,8,11,13,15-hexaene-2,7-dione (mandarone G, 4) and 12,16-epoxy-11,14-dihydroxy-17(15-->16),18(4-->3)-diabeo-abieta-3,5,8,11,13,15-hexaene-1,7-dione (mandarone H, 5) respectively, mainly based on the spectral analysis and by comparison with those of closely related compounds.
In vitro adventitious shoots (about 28) of Clerodendrum inerme were regenerated from leaf segments on MS medium containing BA (4 mg/L). These shoots developed directly from the leaf explants without callusing after 5 weeks. Leaf explant when cultured in MS medium containing BA (2 mg/L) and NAA (0.5 mg/L) developed compact callus that became nodular and regenerated shoots (about 50) after 5 weeks. The in vitro developed shoots were rooted in MS medium supplemented with IAA (2 mg/L). The hardened plantlets were successfully established in the field with 90% survival.
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Multidimensional reversed-phase HPLC was employed to isolate the active constituents from a crude extract of Clerodendrum floribundum R. Br. These active constituents were known to have bioactivity against the enzyme xanthine oxidase and potentially could be employed in the treatment of gout. Using a multidimensional separation approach, rapid isolation of the active constituents was achieved from a complex sample matrix. As each separation dimension was isocratic, no equilibration time was required and consequently the technique shows promise in the scale up to preparative levels where high throughput is important.
Sixty organic and aqueous extracts of eleven plants used for the control of malaria by local communities in Kisii District, Kenya were screened for in vitro anti-plasmodial activity. The plants selection was based on existing ethnobotanical information and interviews with local communities. The extracts were tested against chloroquine sensitive and resistant laboratory adapted strains of Plasmodium falciparum. The study revealed that 63.6% of the plants were active (IC50 < or = 100 microg/mL). Extracts of four plants, Ekebergia capensis, Stephania abyssinica, Ajuga remota and Clerodendrum myricoides gave IC50 values below 30 microg/mL against both chloroquine sensitive and resistant P. falciparum strains. Combination of extracts of E. capensis and C. myricoides with chloroquine against the multi-drug resistant P. falciparum isolate (V1/S) revealed synergistic effect. The plants which showed activity may be useful as sources for novel anti-plasmodial compounds.
We investigated spatio-temporal genetic variation in allele frequency and estimated gene flow among sympatric populations of Tetranychus kanzawai on different host plants by the use of microsatellite markers. In the analysis of spatial genetic variation, no isolation by distance was detected among the populations. Gene flow between populations on Hydrangea macrophylla and those on other host plants was relatively restricted, whereas the populations on Akebia quinata and Clerodendrum trichotomum were almost panmictic. Our study on temporal genetic variation showed (1) that population differentiation was slightly reduced during the period from April to May owing to frequent gene flow among populations; and (2) that population differentiation was greatly enhanced from May to October because of bottleneck effects. Genetic differentiation among T. kanzawai populations was caused by the effect of host plants rather than by the effect of geographic distance among populations, suggesting possibility of sympatric host race formation in this species.
A multidimensional heart-cutting reversed-phase HPLC separation approach, where two columns were operated independently via two six-port two-position switching valves, was employed in the isolation of a major bioactive found in the ethanol-water (80:20) crude extract of Clerodendrum floribundum. In this mode of operation, the specific productivity of the multidimensional approach under overload conditions was twice that of conventional gradient methods with the same loading factor. Isolated sample purities were greater than 99% with recoveries of 95%. The independent operation of each of the two columns employed in the multidimensional approach allowed the cycle time to be less than 7 min, compared to 23 min in the gradient elution single-dimension mode of operation.
Dichloromethane and 90% methanol extracts of 42 South African plants were screened for mutagenicity and antimutagenicity using the Salmonella/microsome mutagenicity assay (Ames) against Salmonella typhimurium TA98 and TA100 bacterial strains in the presence and absence of metabolic activator S9. The methanol extracts from whole plants of Helichrysum simillimum, Helichrysum herbaceum and Helichrysum rugulosum indicated mutagenicity. These are the first reported tests on the mutagenicity of Helichrysum species. Six species indicated antimutagenic properties, all in the presence of S9: methanol leaf extract of Bauhinia galpinii, and dichloromethane leaf extracts of Bauhinia galpinii, Clerodendrum myricoides, Datura stramonium, Buddleja saligna, Millettia sutherlandii and Sutherlandia frutescens.