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Antimalarial activity of some Colombian medicinal plants.

Antimalarial activity of 10 vegetal extracts (9 ethanolic extracts and 1 crude alkaloid extract), obtained from eight species traditionally used in Colombia to treat malaria symptoms, was evaluated in culture using Plasmodium falciparum chloroquine resistant (FcB2) strain and in vivo on rodent malaria Plasmodium berghei. The activity on ferriprotoporphyrin biomineralization inhibition test (FBIT) was also assessed. Against Plasmodium falciparum, eight extracts displayed good activity Abuta grandifolia (Mart.) Sandwith (Menispermaceae) leaves, Acacia farnesiana (L.) Willd. (Mimosaceae) leaves, Acnistus arborescens (L.) Schltdl. (Solanaceae) aerial part, Croton leptostachyus Kunth (Euphorbiaceae) aerial part, Piper cumanense Kunth (Piperaceae) fruits and leaves, Piper holtonii C. DC. (Piperaceae) aerial part and Xylopia aromatica (Lam.) Mart. (Annonaceae) bark with IC(50) values ranging from <1 to 2.1 microg/ml, while in the in vivo model only Abuta grandifolia alkaloid crude extract exhibits activity, inhibiting 66% of the parasite growth at 250 mg/kg/day. In the FBIT model, five extracts were active (Abuta grandifolia, Croton leptostachyus, Piper cumanense fruit and leaves and Xylopia aromatica).

Animals↗

Medicinal plants of the Shinasha, Agew-awi and Amhara peoples in northwest Ethiopia.

Study was conducted in two sub-districts in northwestern Ethiopia to compile and analyse knowledge on the use of medicinal plants for treatment or prevention of human ailments by three socio-cultural groups, namely the Amharas, Shinashas and Agew-Awis. Data were mainly collected through individual interviews conducted with selected knowledgeable farmers and professional healers of the three socio-cultural groups. A total of 76 medicinal plants belonging to 48 families were documented, of which 50 species were reported by the Amharas, 25 by the Shinashas and 20 by the Agew-Awis. Large proportions of medicinal plants were found to have been used for the treatments of gastro-intestinal complaints (26%), skin diseases (24%) and malaria (22%). Relatively, higher numbers of informants agreed on the use of Croton macrostachyus against malaria (21%), Cynoglossum coeruleum against 'mich', illness mainly characterized by fever, headache and sweating (18%) and Zehneria scabra against malaria (13%). The species Croton Macrostachyus, Calpurnia aurea, Clematis hirsuta and Plumbago zeylanica were found to have the highest diversity of medicinal applications. We recommend that priority for further investigation should be given to medicinal plants with higher informant consensuses, as this could indicate their better efficacy. Measures are needed to conserve plants that are reported as scarce in the study area but still are only harvested from the wild.

Data Collection↗

Ethnotherapeautic management of skin diseases among the Kikuyus of Central Kenya.

Skin health is increasingly becoming an important aspect of primary health care among many communities particularly because of the increased challenge of HIV-AIDS, skin conditions being among the common opportunistic diseases in immuno-compromised individuals. This study investigated the use of traditional remedies in managing various skin conditions in the Central Province of Kenya. Fifty-seven plant species in 31 families were identified as regularly utilized. Of these plants 27 species had a frequency of three and above. Some of the highly utilized plant species include: Croton megalocarpus Hutch., Senna didymobotrya (Fresen.) Irwin & Barneby, Vernonia lasiopus O. Hoffm., Croton macrostachyus Del. and Aloe secundifolia Engl. In the majority of the cases the sap or occasionally the latex was applied directly on the affected areas. In other cases the plant parts were heated and used as poultice. Only in few conditions were the plant parts boiled and the extract used for washing affected areas, probably acting as antiseptic. This study found that 14 skin conditions were commonly managed using herbal preparations. Of these conditions nine (9) had informant consensus of 0.5 and above, with the highest consensus found in management of swellings and skin sores. Soils were also cited as an important non-plant resource for management of skin conditions especially those associated with measles. Since most skin conditions are caused by microorganisms such as bacteria, viruses and fungi, the medicinal plants and other resources reported in this study form a justifiable basis for antimicrobial trials, pharmacological and phytochemical analysis, with promising results.

Geography↗

Anti-inflammatory effects of jojoba liquid wax in experimental models.

Jojoba [Simmondsia chinensis (Link 1822) Schneider 1907] is an arid perennial shrub grown in several American and African countries. Jojoba seeds, which are rich in liquid wax, were used in folk medicine for diverse ailments. In the current study, the potential anti-inflammatory activity of jojoba liquid wax (JLW) was evaluated in a number of experimental models. Results showed that JLW caused reduction of carrageenin-induced rat paw oedema in addition to diminishing prostaglandin E2 (PGE2) level in the inflammatory exudates. In a test for anti-inflammatory potential utilizing the chick's embryo chroioallantoic membrane (CAM), JLW also caused significant lowering of granulation tissue formation. Topical application of JLW reduced ear oedema induced by croton oil in rats. In the same animal model, JLW also reduced neutrophil infiltration, as indicated by decreased myeloperoxidase (MPO) activity. In addition, JLW ameliorated histopathological changes affected by croton oil application. In the lipopolysaccharide (LPS)-induced inflammation in air pouch in rats, JLW reduced nitric oxide (NO) level and tumor necrosis factor-alpha (TNF-alpha) release. In conclusion, this study demonstrates the effectiveness of JLW in combating inflammation in several experimental models. Further investigations are needed to identify the active constituents responsible for the anti-inflammatory property of JLW.

Animals↗

Simultaneous determination of four active ingredients of dinocap in crops by high-performance liquid chromatography.

A procedure for high-performance liquid chromatographic (HPLC) determination of four active ingredients of dinocap, 2,4-dinitro-6-octylphenyl crotonate, 2,6-dinitro-4-octylphenyl crotonate, 2,4-dinitro-6-octylphenol and 2,6-dinitro-4-octylphenol, in crops was examined. The four compounds were extracted with acetone and re-extracted into hexane. After clean-up successively by hexane-acetonitrile partition and silica gel column chromatography, the compounds were determined by HPLC with an UV detector (245 nm). The column was Cosmosil 5C18 (ODS, 5 micron) and the eluent was methanol-water-acetic acid (330:70:1). The limit of detection was 0.02 ppm and the recoveries from crops (spiked with 0.5 ppm) were 85-100%. The four compounds were determined simultaneously and the method was shown to be applicable to residue analysis of these compounds in crops sprayed with dinocap.

Chromatography, High Pressure Liquid↗

On-line derivatization for resonance-enhanced multiphoton ionization time-of-flight mass spectrometry: detection of aliphatic aldehydes and amines via reactive coupling of aromatic photo ionization labels.

Resonance-enhanced multiphoton ionization time-of-flight mass spectrometry (REMPI-TOFMS) is a powerful technique for the on-line analysis of aromatic compounds with unique features regarding selectivity and sensitivity. Aliphatic compounds, however, are difficult to address by REMPI due to their unfavorable photo ionization properties. This paper describes the proof of concept for an on-line derivatization approach for converting nonaromatic target analytes into specific, photoionizable aromatic derivatives that are readily detectable by REMPI-TOFMS. A multichannel silicone trap or poly(dimethylsiloxane) (PDMS) open tubular capillary was used as a reaction medium for the derivatization of volatile alkyl aldehydes and alkylamines with aromatic "photoionization labels"and to concentrate the resulting aromatic derivatives. The aldehydes formaldehyde, acetaldehyde, acrolein, and crotonal, which when underivatized are poorly detectable by REMPI, were converted into their easily photoionizable phenylhydrazone derivatives by the on-line reaction with phenylhydrazine as reagent. Similarly, the methyl-, ethyl-, propyl-, and butylamines were converted into their REMPI-ionizable benzaldehyde alkylimine derivatives by the on-line reaction with benzaldehyde as reagent. The derivatives were thermally desorbed from the PDMS matrix and transferred into the REMPI-TOFMS for detection. The REMPI-TOFMS detection limits obtained for acetaldehyde; acrolein; crotonal; and methyl-, ethyl-, propyl-, and butylamine using this photo ionization labeling method were in the sub-parts-per-million range and, thus, readily below the permissible exposure limits set by OSHA.

Aldehydes↗

Asymmetric conjugate 1,4-addition of arylboronic acids to alpha, beta-unsaturated esters catalyzed by Rhodium(I)/(S)-binap

Arylboronic acids underwent the conjugate 1,4-addition to alpha, beta-unsaturated esters to give beta-aryl esters in high yields in the presence of a rhodium(I) catalyst. The addition of arylboronic acids to isopropyl crotonate resulted in high yields and high enantioselectivity exceeding 90% ee in the presence of 3 mol % of Rh(acac)(C(2)H(4))(2) and (S)-binap at 100 degrees C. The rhodium/(S)-binap complex provided (R)-3-phenylbutanoate in the addition of phenylboronic acid to benzyl crotonate. The effects on the enantioselectivity of chiral phosphine ligands, rhodium precursors, and substituents on alpha,beta-unsaturated esters are discussed, as well as the mechanistic aspect of the catalytic cycle.

Journal Article↗

Theoretical study of the photochemical [2 + 2]-cycloadditions of cyclic and acyclic alpha,beta-unsaturated carbonyl compounds to ethylene.

The ground and first triplet excited-state potential energy surfaces of the [2 + 2]-cycloadditions of 2-cyclohexenone, methyl acrylate, and methyl crotonate to ethylene have been studied by means of CASSCF and DFT-B3LYP calculations. The attack of ethylene to the (3)(pi-pi) alpha,beta-unsaturated carbonyl compound leads to the formation of a triplet 1,4-biradical intermediate that evolves to the ground-state potential energy surface. The outcome of the reaction is governed by the competition between the deactivation of the (3)(pi-pi) alpha,beta-unsaturated carbonyl compound itself and its reaction with ethylene to form the triplet 1,4-biradical. For 2-cyclohexenone, the potential energy barrier corresponding to the formation of the biradical intermediate is lower than for the acyclic systems. On the other hand, the energy necessary to reach the crossing point between the (3)(pi-pi) and the ground-state potential energy surfaces is lower for the acyclic systems than for 2-cyclohexenone. For methyl acrylate and methyl crotonate, the decay of the (3)(pi-pi) state of the isolated molecule is therefore expected to be faster than the formation of the 1,4-biradical, so that the [2 + 2]-cycloaddition will not take place. However, for 2-cyclohexenone the formation of the triplet 1,4-biradical is favorable, and the process will lead to the formation of the corresponding cyclobutane derivative.

Journal Article↗

Anti-inflammatory and antishock water-soluble polyesters of glucocorticoids with low level systemic toxicity.

PURPOSE: The objective of this study was to evaluate the pharmacological activity of glucocorticoid hormones incorporated into the structure of water-soluble carbochain polymers via the esterified 21-CH2OH group. METHODS: Polymer analogs of glucocorticoids were prepared by radical copolymerization of 1-vinyl-2-pyrrolidone with cortisol or dexamethasone 21-crotonates and crotonic acid or 2-(diethylamino) ethylcrontonate which served as ionogenic comonomers. Anti-inflammatory, immunosuppressive and catabolic activities for ionogenic tertiary copolymers and previously prepared non-ionogenic binary copolymers were evaluated in standard animal models. The antishock activity of some of the copolymers was evaluated using the "declamping shock" model. RESULTS: Water-soluble tertiary copolymers with a steroid content up to 14 mol% and an intrinsic viscosity up to 0.30 dl/g in ethanol were synthesized. It was shown that the copolymers were stable in aqueous solutions at pH 5.2-7.3. All of the polymers studied suppressed inflammatory reactions at the level of free hormones when administered interperitoneally. The antishock activity was considerably higher compared to free steroids. The copolymers, unlike unmodified glucocorticoids, did not influence the physical development of young animals. They also caused much lower thymus hypotrophy than free hormones. No clear effect of the presence and nature of ionogenic units in copolymers on the pharmacological performance of the copolymers was detected. CONCLUSIONS: The water-soluble polymers bearing glucocorticoid 21-residues in the side chains retain the anti-inflammatory activity of free steroids and exhibit a higher antishock, a lower immunosuppressive and no catabolic effect.

Animals↗

Antiinflammatory screening of the medicinal plant Gynura procumbens.

Gynura procumbens is used in Thai folk medicine to treat topical inflammation, rheumatism, and viral ailments. In the present work, attempts were made to verify the folk medicinal claim that the crude ethanolic extract of G. procumbens has antiinflammatory action and to relate the activity to particular fractions using a croton oil-induced mouse ear inflammation model. The original ethanolic extract of G. procumbens was partitioned between water and ethyl acetate. The residues were subjected to antiinflammatory evaluation. While the water extract did not show any antiinflammatory activity, the administration of the original organic extract significantly inhibited the increase in ear thickness in response to croton oil (n = 5). The activity of 0.75 mg/ear original organic extract showed similar antiinflammatory activity (inhibition 65.2%) to that of 6 mg/ear hydrocortisone 21-hemisuccinate sodium salt (inhibition 64.8%). The organic extract was then fractionated with a series of solvents in order of increasing polarity. Each fraction was dried, dissolved in acetone and monitored using the same bioassay. These experiments showed that the hexane and toluene fractions showed significant inhibitions of 44.6% and 34.8%, respectively. These two fractions had similar activities to 4 mg/ear of hydrocortisone (inhibition 35.0%). The possible chemical constituents in the extracts and fractions were investigated using thin layer chromatography and specific color reagents. These tests showed that steroids might be one class of antiinflammatory compounds in this plant.

Animals↗

Effect of Salmonella enteritidis 11RX infection on two-stage skin carcinogenesis in mice.

S. enteritidis 11RX infection inhibits the growth of a number of transplantable tumours in mice. In addition, oral infection of mice with S. enteritidis 11RX inhibits colon carcinogenesis by 1,2 dimethylhydrazine. This study has examined the effect of S. enteritidis 11RX infection on two-stage skin carcinogenesis in mice using 7,12 dimethylbenz(a)anthracene (DMBA) as initiator and croton oil as promoter. No protection was observed in either LACA or (BALB/c x C57Bl/6J)F1 mice when live 11RX was repeatedly administered i.v. during promotion. When a protein antigen extract from S. enteritidis 11RX was administered i.v. to previously immunised mice during skin carcinogenesis, significant protection was observed both in terms of the number of mice with papillomas and the number of papillomas per mouse. However, the protection was weak and transient. LACA mice were much more susceptible to skin carcinogenesis by DMBA and croton oil than were (BALB/c x C57B1/6J)F1 mice. A preliminary study indicated that BALB/c, C57B1 and CBA mice were also relatively resistant to skin carcinogensis.

9,10-Dimethyl-1,2-benzanthracene↗

In-line monitoring of esterification using a miniaturised mid-infrared spectrometer.

A miniaturised mid-infrared (MIR) spectrometer attached directly to an in-line immersion probe with an attenuated total reflectance crystal has been used to monitor the progression of the batch reaction of crotonic acid and 2-butanol in toluene. Univariate calibration, using the signal at 1188 cm(-1) in the 2nd derivative spectrum, gave accurate (average error, 1.6%) and precise (average relative standard deviation, 5.2%) estimation of 2-butyl crotonate concentrations in the range 0.08-0.49 mol dm(-3). Calibration by partial least squares was of no additional benefit in this application. The performance of in-line MIR spectrometry was comparable to that of an off-line reference gas chromatography method and superior to that of other in-line process analysis techniques (near-infrared, Raman or UV-visible spectrometries).

Journal Article↗

Sulphide impairment of substrate oxidation in rat colonocytes: a biochemical basis for ulcerative colitis?

1. Isolated colonic epithelial cells of the rat were incubated for 40 min with [6-14C]glucose and n-[1-14C]butyrate in the presence of 0.1-2.0 mmol/l NaHS, a concentration range found in the human colon. Metabolic products, 14CO2, acetoacetate, beta-hydroxybutyrate and lactate, were measured and injury to cells was judged by diminished production of metabolites. 2. Oxidation of n-butyrate to CO2 and acetoacetate was reduced at 0.1 and 0.5 mmol/l NaHS, whereas glucose oxidation remained unimpaired. At 1.0-2.0 mmol/l NaHS, n-butyrate and glucose oxidation were dose-dependently reduced at the same rate. 3. To bypass short-chain acyl-CoA dehydrogenase activity necessary for butyrate oxidation, ketogenesis from crotonate was measured in the presence of 1.0 mmol/l NaHS. Suppression by sulphide of ketogenesis from crotonate (-10.5 +/- 6.1%) compared with control conditions was not significant, whereas suppression of ketogenesis from n-butyrate (-36.00 +/- 5.14%) was significant (P = < 0.01). Inhibition of FAD-linked oxidation was more affected by NaHS than was NAD-linked oxidation. 4. L-Methionine (5.0 mmol/l) significantly redressed the impaired beta-oxidation induced by NaHS. Methionine equally improved CO2 and ketone body production, suggesting a global reversal of the action of sulphide. 5. Sulphide-induced oxidative changes closely mirror the impairment of beta-oxidation observed in colonocytes of patients with ulcerative colitis. A hypothesis for the disease process of ulcerative colitis is that sulphides may form persulphides with butyryl-CoA, which would inhibit cellular short-chain acyl-CoA deHydrogenase and beta-oxidation to induce an energy-deficiency state in colonocytes and mucosal inflammation.

Animals↗

Dendritic epidermal gamma/delta T cells (DETC) activated in vivo proliferate in vitro in response to Mycobacterium leprae antigens.

BACKGROUND: gamma/delta T-cell receptor (TCR)+ dendritic epidermal T cells (DETC) are part of a primitive defense system in the skin; they are capable of responding only to a limited number of antigens. The aim of the present study was to test whether DETC can proliferate in vitro in response to antigens of Mycobacterium leprae. METHODS: DETC were obtained from CBA mouse ear skin by trypsinization and Histopaque gradient centrifugation. The resulting epidermal cell suspension contained up to 20% DETC, as analyzed by the fluorescence activated cell sorter (FACS) after staining with anti-Thy-1 or anti-gamma/delta TCR monoclonal antibodies (mAbs). The freshly isolated cells, or DETC cultured up to 4 weeks with interleukin-2 (IL-2), were exposed in vitro for up to 6 days to varying doses of the following M. leprae antigens: (1) integral (live) M. leprae bacilli; (2) Dharmendra antigen; and (3) PGL-1 (phenolic glycolipid of M. leprae). The DETC response was assessed by tritiated thymidine (3H-TdR) incorporation. RESULTS: The freshly isolated DETC, or DETC cultured up to 4 weeks with IL-2, did not respond significantly to any of the M. leprae antigens, although at the same time they were able to respond vigorously to concanavalin A (Con A), as positive control. If, however, DETC were isolated from skin, painted 7 days before with croton oil (10 microL/cm2 to cause irritant dermatitis, they were able to respond to all M. leprae antigens by a 3-4-fold incrase in the 3H-TdR uptake. The most effective stimulator was a 1 : 1 mixture of Dharmendra and PGL-1 (0. 01 microg/mL), which was as effective as 10-fold higher doses of either antigen alone. Cell counts confirmed that increased DNA synthesis was associated with cell proliferation. Experiments employing alpha/beta-TCR CBA murine spleen cells and epidermal cell suspension treated with anti-gamma/delta or antialpha/beta mAbs + C' proved that only the gamma/delta DETC were the responder cells to M. leprae antigens. CONCLUSIONS: The results suggest that activation of DETC in vivo may make them responsive to M. leprae antigens. A significant increase in the number of class II major histocompatibility complex (MHC) positive, nondendritic cells was observed in the croton oil-treated epidermis. We hypothesize that croson oil-induced upregulation of class II MHC expression, which endows epidermal cells with antigen-presenting capabilities, might be an important factor in vivo in delivering an immunogenic signal to resident DETC in the skin.

Animals↗

Anti-inflammatory activity of dichloromethane extract of Heterotheca inuloides in vivo and in vitro.

The dichloromethane extract from the dried flowers of Heterotheca inuloides Cass. was investigated on several pharmacological models of inflammation in vivo and in vitro. It showed anti-inflammatory activity on the croton oil-induced oedema test in mouse ear, at 1 mg/ear. The compound isolated from this extract, 7-hydroxy-3,4-dihydrocadalin, showed anti-inflammatory effect on the same experimental model (ED50 of 0.9 mumol/ear), as well as on COX-1 and COX-2 catalysed prostaglandin biosynthesis assays, with IC50 values of 22 microM and 526 microM, respectively. No effect was observed on carrageenan-induced oedema and on fMLP/PAF-induced exocytosis of human neutrophils. The COX-1 inhibitory effect showed by 7-hydroxy-3,4-dihydrocadalin might be related to the anti-inflammatory activity on the topical oedema induced by croton oil.

Animals↗

Mitogenic activities in African traditional herbal medicines.

Mitogenic activities in African traditional herbal medicines were examined using protein fractions obtained from their extracts by precipitation with ammonium sulfate. Potent mitogenic activities for human and mouse lymphocytes were found in the three plants: Croton macrostachyus, Croton megalocarpus (Euphorbiaceae), and Phytolacca dodecandra (Phytolaccaceae). All the gel chromatographic patterns of these protein fractions progressed toward the smaller molecule site with pronase treatment, while their mitogenic activities decreased significantly. Protein fractions from these three plants induced mitogenesis both in human and mouse isolated T cells, but not in lymphocytes from athymic nude mice. By testing further fractionated protein fractions with gel filtration chromatography, it was found that all three plants contained several mitogens having different molecule sizes.

Africa↗

Clostridium peptidivorans sp. nov., a peptide-fermenting bacterium from an olive mill wastewater treatment digester.

A new peptide-degrading, strictly anaerobic bacterium, designated strain TMC4T, was isolated from an olive mill wastewater treatment digester. Cells of strain TMC4T were motile, rod-shaped (5-10 x 0.6-1.2 microm), stained Gram-positive and formed terminal to subterminal spores that distended the cells. Optimal growth occurred at 37 degrees C and pH 7 in an anaerobic basal medium containing 0.5% Casamino acids. Arginine, lysine, cysteine, methionine, histidine, serine, isoleucine, yeast extract, peptone, Biotrypcase, gelatin and crotonate also supported growth, but not carbohydrates, organic acids or alcohols. The end-products of degradation were: acetate and butyrate from lysine and crotonate; acetate, butyrate, H2 and CO2 from Biotrypcase, gelatin and peptone; acetate, alanine, H2 and CO2 from cysteine; acetate, H2 and CO2 from serine, cysteine and yeast extract; acetate and formate from histidine; propionate from methionine; methyl 2-butyrate, H2 and CO2 from isoleucine; acetate and ethanol from arginine; and acetate, propionate, butyrate, methyl 2-butyrate, H2 and CO2 from Casamino acids. The DNA G+C content of strain TMC4T was 31 mol%. Phylogeny based on 16S rRNA sequence analysis showed that strain TMC4T was a member of the low-G+C-content Gram-positive genus Clostridium, with the closest relative being Clostridium pascui (sequence similarity of 96 %). Due to considerable differences in genomic and phenotypic properties between strain TMC4T and those of its nearest relative, strain TMC4T is proposed as a new species of the genus Clostridium, Clostridium peptidivorans sp. nov. Strain TMC4T has been deposited in the DSMZ as strain DSM 12505T.

Amino Acids↗

Alicycliphilus denitrificans gen. nov., sp. nov., a cyclohexanol-degrading, nitrate-reducing beta-proteobacterium.

A facultatively denitrifying bacterium, strain K601T, was isolated at 30 degrees C from a municipal sewage plant on cyclohexanol as sole carbon source and nitrate as electron acceptor. Under aerobic conditions this strain used acetate, fumarate, lactate, pyruvate, crotonate, indole, glucose, vanillate, 4-hydroxybenzoate, m-cresol, o-cresol and p-cresol. Under denitrifying conditions the strain used cyclohexanol, cyclohexanone, 1,3-cyclohexanedione, 2-cyclohexenone, 1,3-cyclohexanediol (cis and trans), monocarboxylic acids (C2-C7), adipate, pimelate, 5-oxocaproate, citrate, 2-oxoglutarate, succinate, malate, crotonate, lactate, pyruvate and fumarate. Cells were short rods, 0.6 microm wide and 1-2 microm long, motile, non-spore-forming, Gram-negative, and catalase- and oxidase-positive. Strain K601T used nitrate, nitrite and oxygen as electron acceptors, but not sulfate, sulfite or fumarate. The DNA G+C content of strain K601T was 66 mol%. Phylogenetic analysis, based on 16S rDNA sequencing, showed that strain K601T represents a separate lineage of the family Comamonadaceae in the beta-subclass of Proteobacteria. Based on the high 16S rDNA sequence divergence and phenotypic characteristics, the name Alicycliphilus denitrificans gen. nov., sp. nov. is proposed for this strain. The type strain is K60IT (=DSM 14773T =CIP 107495T).

Base Composition↗