A double-blinded, randomized, split-side, vehicle-controlled study of the efficacy of cleanser containing Acanthus ebracteatus Vahl., Suregada multiflora, and Acacia concinna in patients with atopic dermatitis: A pilot study.

BACKGROUND: Barrier repair therapy is the key management approach for both eczematous and non-lesional skin of atopic dermatitis. The use of appropriate cleansers to enhance skin hydration is an adjunctive treatment that increases topical drug penetration. Anti-inflammatory properties of various medicinal plants in tropical Asia have been reported. OBJECTIVE: Investigate the efficacy of herbal cleanser containing a combination of herbal extracts from Acanthus ebracteatus Vahl., Suregada multiflora, and Acacia concinna on seemingly intact skin in patients with atopic dermatitis by measuring improvements in the skin barrier function. METHODS: This 2-week pilot study was a split-side, randomized, double-blinded, vehicle-controlled trial. All patients (n = 30) were asked to use both a cleanser with an active formulation containing the herbal extracts and a vehicle- controlled cleanser on each side of mid-volar forearm. Biophysical assessments including transepidermal water loss (TEWL), skin hydration, skin pH, and skin roughness were performed at baseline and upon study completion. RESULTS: Compared to baseline, the median percentage change in TEWL at the end of the study was significantly greater for the active side 10.4 (-19, 20.7) g/m2h than the control side -13.2 (-28.7, 9.1) g/m2h; p = 0.01. The median percentage change of skin hydration, skin pH, and skin roughness of the active side compared to the control side had no a statistical significance. CONCLUSIONS: This cleanser is beneficial when used as adjunctive therapy. Further studies should evaluate its anti- sinflammatory properties in the remedy or active phase of atopic dermatitis or other inflammatory skin diseases.

Modified ent-Abietane Diterpenoids from the Leaves of Suregada zanzibariensis.

The leaf extract of Suregada zanzibariensis gave two new modified ent-abietane diterpenoids, zanzibariolides A (1) and B (2), and two known triterpenoids, simiarenol (3) and ß-amyrin (4). The structures of the isolated compounds were elucidated based on NMR and MS data analysis. Single-crystal X-ray diffraction was used to establish the absolute configurations of compounds 1 and 2. The crude leaf extract inhibited the infectivity of herpes simplex virus 2 (HSV-2, IC50 11.5 µg/mL) and showed toxicity on African green monkey kidney (GMK AH1) cells at CC50 52 µg/mL. The isolated compounds 1-3 showed no anti-HSV-2 activity and exhibited insignificant toxicity against GMK AH1 cells at ≥100 µM.

Ent-abietane diterpenoids from Suregada zanzibariensis Baill. (Euphorbiaceae), their cytotoxic and anticancer properties.

The stem bark extract of Suregada zanzibariensis afforded a previously undescribed ent-abietane diterpenoid trivially named mangiolide (1) and a known jolkinolide B (2) via anticancer bioassay-guided fractionation. The CH2Cl2:MeOH extract of S. zanzibariensis was initially analysed for its anticancer properties against three cancer cell lines, renal (TK10), melanoma (UACC62), and breast (MCF7) and was found to be potent at low µg/mL ranges. Compound 1, 6α-acetoxy-14-keto-ent-abieta-7(8),13(15)-diene-16,12-olide (mangiolide) inhibited the growth of renal (TK10) with a GI50 of 0.02 µg/mL; a GI50 of 0.03 µg/mL for melanoma (UACC62) and a GI50 of 0.05 µg/mL for breast (MCF7) cancer cell lines. Compound 2, 8,13-diepoxy-13,15-ent-abietene-16,12-olide (jolkinolide B) inhibited the growth (GI50) of the cell lines at 3.31 µg/mL for renal (TK10), 0.94 µg/mL for melanoma (UACC62) and 2.99 µg/mL for the breast (MCF7). The structures were established on the basis of their spectroscopic analysis and the absolute stereostructures assigned using electronic circular dichroism (ECD).

Bauerenol, a triterpenoid from Indian Suregada angustifolia: Induces reactive oxygen species-mediated P38MAPK activation and apoptosis in human hepatocellular carcinoma (HepG2) cells.

The triterpenoid, bauerenol, from Suregada angustifolia (Baill. ex Muell.-Arg.) Airy Shaw (Euphorbiaceae) was screened for anti-cancer property using hepatocellular carcinoma cell line, HepG2. Bauerenol exhibited growth inhibitory and apoptosis inducing potential against HepG2 cancer cells. 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide cytotoxic assay revealed that bauerenol treatment significantly reduced the growth of HepG2 cells in a time- and dose-dependent manner with 50% growth inhibitory concentration doses of 45 and 25 µg/mL at 24 and 48 h treatments, respectively. Bauerenol-induced cell death reflected apoptotic morphological features, that is, cell membrane blebbing, vacuolization, chromatin condensation, and nuclear fragmentation. In addition, bauerenol treatment diminished the mitochondrial membrane potential, by inducing the efflux of cytochrome c, downregulating the levels of anti-apoptotic Bcl-2 as well as upregulating the levels of pro-apoptotic Bax, and inducing caspase activation and poly (ADP-ribose) polymerase cleavage. Moreover, bauerenol treatment activates p38MAPK and inactivates the anti-apoptotic kinases Akt and ERK1/2 through the induction of reactive oxygen species. Furthermore, bauerenol-mediated S-phase arrest was associated with downregulation of cell cycle-rate-limiting factor (cyclin D1) and upregulation of cyclin-dependent kinase inhibitor p21 and tumor suppressor p53. Interestingly, pre-treatment of cells with reactive oxygen species inhibitor and p38 inhibitor significantly decreases bauerenol-induced cytotoxicity, Bax upregulation, and p38 activation. This study clearly states that bauerenol induces cell cycle arrest and apoptosis through the reactive oxygen species-dependent p38MAPK activation in HepG2 cancer cells.

Anti-inflammatory principles of Suregada multiflora against nitric oxide and prostaglandin E2 releases.

AIM OF THE STUDY: The stem bark of Suregada multiflora and the isolated compounds were carried out to investigate for anti-inflammatory activity. MATERIALS AND METHODS: The stem bark of Suregada multiflora and its isolated compounds were tested for their anti-inflammatory effects against lipopolysaccharide (LPS)-induced nitric oxide (NO) and prostraglandin E(2) (PGE(2)) releases in RAW264.7 cells as well as the anti-inflammatory mechanism on mRNA expression of the active compound (5, helioscopinolide A). RESULTS: The extract of Suregada multiflora possessed potent NO inhibitory effect with an IC(50) value of 8.6 µg/ml. Among the isolated compounds, helioscopinolide A (5) exhibited the highest activity against NO release with an IC(50) value of 9.1 µM, followed by helioscopinolide C (6) and suremulol D (2) with IC(50) values of 24.5 and 29.3 µM, respectively. The IC(50) value of 5 against PGE(2) production was found to be 46.3 µM. The mechanism in transcriptional level of compound 5 was found to inhibit iNOS and COX-2 mRNA expressions in dose-dependent manners. CONCLUSIONS: The present study may support the traditional use of Suregada multiflora stem bark for treatment of inflammatory-related diseases.

Three new water-soluble alkaloids from the leaves of Suregada glomerulata (Blume) Baill.

Three new water-soluble alkaloids (1-3) together with twelve known compounds (4-15) have been isolated from the water extract of leaves of Suregada glomerulata. Their structures were determined by spectroscopic analysis and chemical method. Compounds 1-3 were evaluated for their in vitro inhibitory activity against α-glucosidase and HIV-1 replication. However, no significant activities were found.

ent-Abietane and ent-kaurane diterpenoids from the roots of Suregada glomerulata.

Twelve ENT-abietane and ENT-kaurane type diterpenoids, 1- 12, including five new compounds 1- 5, were isolated from the roots of Suregada glomerulata. The structures of the new compounds were elucidated on the basis of 1D and 2D NMR and other spectroscopic studies, and the structures of 1 and 2 were confirmed by X-ray crystallography. Cytotoxic activities against five human tumor cell lines were evaluated.

Diterpenoids from the roots of Suregada glomerulata.

Six new diterpenoids, 7beta,8alpha-dihydroxy-12-oxo- ent-abietan-16,14-olide ( 1), 3,4,18beta-cyclopropa-7beta,17-dihydroxy- ent-abieta-8(14),13(15)-dien-16,12-olide ( 2), 3alpha,7beta-dihydroxy- ent-abieta-8(14),13(15)-dien-16,12-olide ( 3), 3-oxo-8beta,14beta-epoxy- ent-abieta-11,13(15)-dien-16,12-olide ( 4), 17-hydroxy- ent-pimara-8(14),15-dien-3-one ( 5), and 3alpha,6beta-dihydroxy- ent-kaur-16-ene ( 6), and two known compounds, 7beta-hydroxy- ent-abieta-8(14),13(15)-dien-16,12-olide ( 7) and jolkinolide B, were isolated from roots of Suregada glomerulata. The structures of the new compounds were elucidated on the basis of 1D and 2D NMR and other spectroscopic studies. The structure of compound 1 was confirmed by X-ray crystallography. Cytotoxic activities were evaluated against five human tumor cell lines.

[Studies on chemical constituents of Suregada glomerulata II].

OBJECTIVE: To study the chemical constituents of Suregada glomeruldata. METHOD: Isolation and purification were carried out on silica gel, sephardex LH -20, ODS column chromatography etc. Constituents were identified by physicochemical properties and spectral analysis. RESULT: Nine compounds, Jolkinolide B (1), 8alpha, 14-dihydro-7-oxo-jolkinolide E (2), helioscopinolide B (3), ent-kauran-16beta, 17-diol (4), 7-oxo-beta-sitosterol (5), scopoletin (6), adenosine (7), 1'-sinapoylglucose (8), sucrose (9), were obtained and identified. CONCLUSION: Compounds 2-9 were isolated from S. glomerulata for the first time.

Studies on chemical constituents of Suregada glomerulata II / 中国中药杂志

<p><b>OBJECTIVE</b>To study the chemical constituents of Suregada glomeruldata.</p><p><b>METHOD</b>Isolation and purification were carried out on silica gel, sephardex LH -20, ODS column chromatography etc. Constituents were identified by physicochemical properties and spectral analysis.</p><p><b>RESULT</b>Nine compounds, Jolkinolide B (1), 8alpha, 14-dihydro-7-oxo-jolkinolide E (2), helioscopinolide B (3), ent-kauran-16beta, 17-diol (4), 7-oxo-beta-sitosterol (5), scopoletin (6), adenosine (7), 1'-sinapoylglucose (8), sucrose (9), were obtained and identified.</p><p><b>CONCLUSION</b>Compounds 2-9 were isolated from S. glomerulata for the first time.</p>

Potential anti-allergic ent-kaurene diterpenes from the bark of Suregada multiflora.

Two ent-kaurene diterpenes, ent-16-kaurene-3beta,15beta,18-triol (1) and ent-3-oxo-16-kaurene-15beta,18-diol (2), were isolated from a dichloromethane extract of the bark of Suregada multiflora along with five known diterpenes:ent-16-kaurene-3beta,15beta-diol (3), abbeokutone (4), helioscopinolide A (5), helioscopinolide C (6) and helioscopinolide I (7). Their structures were elucidated on the basis of spectroscopic analysis. Compounds 1-7 possessed appreciable anti-allergic activities in RBL-2H3 cells model with IC50 values ranging from 22.5 to 42.2 microM.

Antibacterial potential from Indian Suregada angustifolia.

Phytochemical analysis of the leaves from Indian Suregada angustifolia (Baill. ex Muell. Arg.) Airy Shaw (Euphorbiaceae) resulted in the isolation and identification of six known compounds, viz. friedelin, epi-friedelinol, n-octacosanol, alpha-amyrin, beta-sitosterol and beta-sitosterol-3-beta-D-glucopyranoside. Aqueous (room temperature, boiled and autoclaved) and various solvent (methanol, chloroform and hexane) extracts of leaves were tested against 12 human pathogenic bacteria by the agar well-diffusion method. Aqueous extracts did not express any activity. Antibacterial activity was recorded in the order of methanol, hexane and chloroform extracts. Maximum activity recorded against Staphylococcus aureus (skin infections) in methanol and hexane extracts and moderate activity recorded against diarrhoea causing bacteria, Vibrio vulnificus (hexane extract) and Vibrio cholerae (chloroform extract).

Six new diterpenoids from Suregada multiflora.

Six new diterpenoids were isolated from a CH(2)Cl(2)-MeOH extract of the bark of Suregada multiflora. The structures were established on the basis of one- and two-dimensional NMR and other spectroscopic studies and chemical derivatizations. Two compounds, suregadolides C (1) and D (2), were identified as new diterpene lactones of two antipodal series, containing a cyclopropane ring bridging C-3 and C-4 of the basic abietane skeleton. Suremulide A (3) was found to be a new abietene diterpene lactone. Bannaringaolide A (4), a diterpene lactone, based on a novel carbon skeleton with a seven-membered ring, possibly formed by the rearrangement of the exocyclic C-17 in ring C of an ent-pimarane framework, has also been isolated. A kaurane triol, suremulol A (5), and a kaurane diol, suremulol B (6), were also identified as new metabolites.