This work was launched to study on the chemical constituents from Euphorbia thymifolia. Thirteen compounds were isolated from the 95% ethanol extract of the aerial parts of E. thymifolia by column chromatographies on silica gel, Sephadex LH-20, MCI, and ODS, and preparative HPLC, including two thymol derivatives(1-2), four alkaloids(3-6), five isocoumarins(7-11), together with two ellagic acids(12-13). All the compounds are listed as follows:(Z)-8,9-dehydro-9,10-diisobutyryloxythymol(1), 8-hydro-xy-9,10-diisobutyryloxythymol(2), N-(N-benzoyl-L-phenylalanyl)-L-phenylalanol(3), aurantiamide acetate(4), 1-carboethoxy-β-carboline(5), isoechinulin A(6), ethyl brevifolincarboxylate(7), euphorhirtin B(8), 4,5-didehydro chebulic acid triethyl ester(9), euphorhirtin G(10), pomegranatate(11), 3,3',4'-tri-O-methylellagic acid(12), 3,3'-di-O-methylellagic acid(13). Compound 1 is a new compound. Except for compound 4, the others were isolated from this plant for the first time. All the compounds were screened for anti-neuroinflammatory activity in vitro, and compounds 1-3 and 7 showed significant activity with IC_(50) values of 0.19,12.93,7.29,25.4 μmol·L~(-1).
Chromatography, High Pressure Liquid ; Euphorbia

BACKGROUND: There is a growing interest in the use of Euphorbia hirta Linn. as herbal remedy for dengue, supposedly based on folkloric practice. However, there has been no ethnobotanical documentation of such use in the Philippines. Because of this, the medical community cautions the public against the sole use of E. hirta in treating dengue.

OBJECTIVE: To describe the ethnomedicinal uses of Euphorbia hirta Linn. In selected communities in the Philippines. Specific Objectives. (1) To identify the vernacular names of the plant; (2) to identify the earliest known use of the plant against dengue infection and for other indications; (3) to document the methods of preparation and administration, side effects, and contraindications of use.

METHODS: Cross-sectional descriptive design using the snowball sampling of interviewer-guided key informants for the ethnobotanical interview.

LIMITATIONS: The results of this study may be limited by its convenient sampling design and the use of plant pictures with different magnifications.

RESULTS AND CONCLUSION: Majority of the respondents were female (93%), 41-60 years old (39%), had high school education (43%), and resided in Quezon City (31%). The plant is locally known as tawatawa, butobutonesan, malagatas, and mangagaw. It has been used to treat fever in the Philippines as early as 1948. Its use as a treatment for dengue started only in the 1980s. The plant is either squeezed, crushed, or boiled, and is administered topically or orally. The only reported side-effect is increased urinary frequency.

RECOMMENDATIONS: It is recommended that more comprehensive and large scale studies be conducted, including (1) identification of folkloric uses of E. hirta for the treatment of other diseases; (2) determination of different concentrations of extract (crude or semicrude) using the various reported preparations for optimal outcomes for the different reported medicinal uses.

In our search for natural soluble epoxide hydrolase (sEH) inhibitors from plants, an extract of the dried whole plants of Euphorbia supina Rafin was found to significantly inhibit sEH activity in vitro. Phytochemical investigation of E. supina resulted in isolation of 17 compounds (1 - 17), including triterpenes (1 - 4), phenolic compounds (5 - 8), and flavonoid derivatives (9 - 17). The structures of the isolated compounds were established mainly by extensive analysis of the 1D and 2D NMR, and MS data. All of the isolated compounds were evaluated for their sEH inhibitory activity. Among the isolated phenolic compounds, 8 was identified as a significant inhibitor of sEH, with an IC50 value of 15.4 +/- 1.3 microM. Additionally, a kinetic analysis of isolated compounds (2, 5, 8 - 11, 13, and 17) indicated that the inhibitory effects of flavonoid derivatives 10 and 11 were of mixed-type, with inhibitory constants (Ki) ranging from 3.6 +/- 0.8 to 21.8 +/- 1.0 microM, whereas compounds 2, 5, 8, 9, 13, and 17 were non-competitive inhibitors with inhibition Ki values ranging from 3.3 +/- 0.2 to 39.5 +/- 0.0 microM.
Euphorbia* ; Euphorbiaceae ; Inhibitory Concentration 50 ; Phenol ; Triterpenes

The investigation on the herbal of Euphorbia humifusa Wild. was carried out to find its anti-HBV constituents. The isolation and purification were performed by chromatography such as macroporous resin, polyamide, Sephadex LH-20, MCI GEL CHP 20P and so on. Based on the spectral analysis, seven phenols were identified as brevifolin (1), brevifolin carboxylic acid (2), methyl brevifolincarboxylate (3), phyllanthussin E methyl ester (4), sanguisorbic acid dilactone (5), 3,3'-2-di-O-methyl ellagic acid (6), ellagic acid (7). Among them, Compounds 2-6 were isolated from this plant for the first time.
Euphorbia ; chemistry ; Phenols ; chemistry ; isolation & purification

The combination of normal-phase silica gel column chromatography, octadecyl silica(ODS) column chromatography, semi-preparative high performance liquid chromatography(HPLC), etc. was employed to isolate and purify the chemical components from Euphorbia resinifera, and 7 triterpenoids were separated from the ethanol extract of the medicinal materials. Their structures were identified by various spectroscopy methods as cycloartan-1,24-diene-3-one(1), cycloartan-1,24-diene-3-ol(2), 3β-hydroxy-lanosta-8,24-diene-11-one(3), lnonotusane C(4), eupha-8,24-diene-3β-ol-7,11-dione(5), eupha-24-methylene-8-ene-3β-ol-7,11-dione(6), and eupha-8,24-diene-3β,11β-diol-7-one(7). Compounds 1 and 2 are new compounds, and compound 3 is obtained from nature for the first time.
Drugs, Chinese Herbal ; Euphorbia ; Molecular Structure ; Triterpenes

Four new lanostane triterpenoids, 3β-hydroxy-12α-methoxylanosta-7,9(11),24-triene(1), 3β-hydroxy-12α-methoxy-24-methylene-lanost-7,9(11)-dien(2), 3,7-dioxo-lanosta-8,24-diene(3), and 3,7-dioxo-24-methylene-lanost-8-en(4), were isolated from the latex of Euphorbia resinifera with a variety of chromatography methods. Their structures were elucidated based on spectroscopic data and/or comparison with the data reported in previous research. Compounds 1, 2, and 4 showed moderate inhibition of LPS-induced NO production by RAW264.7, with IC_(50) of 30.4, 37.5, and 28.3 μmol·L~(-1), respectively.
Euphorbia ; Latex ; Molecular Structure ; Steroids ; Triterpenes

This study aims to optimize the parameters for stir-frying of Kansui Radix with vinegar based on the conversion of representative toxic diterpenes, which is expected to serve as a reference for the standardized production of Kansui Radix stir-fried with vinegar. To be specific, the toxic components [3-O-(2'E,4'Z-decadienoyl)-20-O-acetylingenol(3-O-EZ), kansuiphorin C(KPC)] in Kansui Radix and the products(ingenol, 20-deoxyingenol) after the stir-frying with vinegar were selected. The toxicity to intestine and water-draining activity were evaluated with NCM460(normal human colon mucosal epithelial cell line) and HT-29(a human colorectal adenocarcinoma cell line). An HPLC method was then developed to assess the conversion of toxic components. On this basis, temperature, time, and amount of vinegar for the processing of Kansui Radix were optimized with the Box-Behnken design and the content of ingenol and 20-deoxyingenol as evaluation index. The results showed that after the stir-frying of Kansui Radix with vinegar, 3-O-EZ and KPC were first converted to monoester 3-O-(2'E,4'Z-decadienoyl)ingenol(3-EZ) and 5-O-benzoyl-20-deoxyingenol(5-O-Ben) and finally to almost non-toxic ingenol and 20-deoxyingenol, respectively. Meanwhile, the water-draining activity was retained. Six compounds had a good linear relationship with the peak area in the corresponding concentration ranges(R~2≥0.999 8), and the average recovery fell in the range of 98.20%-102.3%(RSD≤2.4%). The content of representative diterpenes and intermediate products was 14.78%-24.67% lower in the Kansui Radix stir-fried with vinegar than in the Kansui Radix, while the content of the conversed products was 14.37%-71.37% higher. Among the process parameters, temperature had significant influence on the total content of products, followed by time. The optimal parameters were 210 ℃, 15 min, and 30% vinegar. The relative error between the experimental results and the predicted values was 1.68%, indicating that the process was stable and reproducible. The strategy of screening optimal parameters for stir-frying of Kansui Radix with vinegar based on the transformation of toxic components can help improve the production stability, reduce the toxicity, and ensure the efficacy of Kansui Radix stir-fried with vinegar, which can serve as a reference for the process optimization of similar toxic Chinese medicinals.
Humans ; Acetic Acid ; Euphorbia ; HT29 Cells

BACKGROUND: Phytoclear-EL1, an extract from Euphorbia lathyris seeds, has a whitening effect due to inhibition of tyrosinase activity. OBJECTIVE: The purpose of this study was to investigate the inhibitory effect of phytoclear-EL1 on melanogenesis. METHODS: Cultured B-16 melanoma cells and 30 human volunteers were used for in vitro and in vivo studies, respectively. Phytoclear-EL1 was added to the cultured B-16 melanoma cells, and applied to UVB-induced hyperpigmented lesions of human volunteers twice daily for 7 weeks. Changes in the number of B-16 melanoma cells, as well as changes in morphology, melanin content, and tyrosinase activity, were measured and then compared with the normal control and the 10(-3)M arbutin groups. Also, the effect of phytoclear-EL1 on UVB-induced hyperpigmented lesions was examined through subjective and objective measurements. RESULTS: In the in vitro study (p<0.05), the number, melanin content, and tyrosinase activity of cultured B-16 melanoma cells were decreased in the 5microgram/ml phytoclear-EL1 group compared to the control group. On objective assessment with a chromameter, the 0.2% phytoclear-EL1 group had a larger difference in the mean L values before and 7 weeks after applying phytoclear-EL1 as compared to the other groups. On subjective assessment by both the researchers and subjects 7 weeks after applying experimental materials, the 0.2% phytoclear-EL1 group and positive control (3% arbutin) had higher scores than the placebo groups. These results demonstrated that phytoclear-EL1 in vivo and in vitro had an inhibitory effect on melanogenesis. CONCLUSION: Phytoclear-EL1 may be a candidate extract in the control of hyperpigmentary disorders.
Arbutin ; Euphorbia ; Human Experimentation ; Melanins ; Melanoma ; Monophenol Monooxygenase ; Seeds

Sixteen compounds were isolated from the aerial parts of Euphorbia sikkimensis by means of various chromatographic techniques such as silica gel, Sephades LH-20 and RP-18, and their structures were elucidated as naringenin (1), kaempferol (2), quercetin (3), kaempferol-3-O-alpha-L-arabinopyranoside (4), quercetin-3-O-alpha-L-arabinopyranoside (5), quercetin-3-O-(2"-galloyl)-alpha-L-arabinopyranoside (6), 5alpha, 8alpha-epidioxy-(22E, 24R)-ergosta-6,22-dien-3beta-ol (7), stigmast-5-ene-7-one-3beta-ol (8), 3beta-hydroxy4a, 14alpha-dimethyl-5alpha-ergosta-8, 24(28)-dien-7-one(9), beta-sitosterol (10) , 10-cucurbitadienol( 1) , scopoletin(12) , ethyl gallate(13), p-hydroxybenzaldehyde (14), 3 betahydroxybenzeneethanol( 15) ,and 2,4-dihydroxy-6-methoxy-acetophenone (16) on the basis of spectroscopic data analysis. All the compounds are isolated from this plant for the first time, and compounds 1, 4-8, 15 are obtained from Euphorbia species for the first time.
Chromatography ; Euphorbia ; chemistry ; Organic Chemicals ; analysis ; isolation & purification

The effect of water extracts of Euphorbia hirta on the histological features and expressions of matrix metalloproteinases (MMPs) and tissue inhibitors of matrix metalloproteinases (TIMPs) in the rat articular cartilage was investigated. Arthritis was induced in rats using Freund's Complete Adjuvant containing heat-killed M. tuberculosis, and treated with water extracts of E. hirta. Paraffin tissue sections of the arthritic joints were evaluated. The extent of cartilage degeneration was found to be greatest in rats treated with the highest dosage of E. hirta, followed by rats in the untreated group. Rats treated with the intermediary and low dosages of Euphorbia hirta showed improved histology. MMP-13 levels were found to be decreased with decreasing dosages of E. hirta. TIMP-1 levels were found to increase with decreasing dosages of E. hirta. MMP-3 levels fluctuated without any appreciable pattern. Low dosages of E. hirta seem to be beneficial in reducing cartilage degeneration in cases of arthritis.
Upper case ee ; Rattus norvegicus ; Euphorbia ; Water ; Degeneration, NOS