Corn starch and methylcellulose edible films incorporated with fireweed (Chamaenerion angustifolium L.) extract: Comparison of physicochemical and antioxidant properties.

The properties of edible films derived from corn starch (CS) and methylcellulose (MC) supplemented with fireweed extract (FE; 0.0125-0.05% w/w) were analyzed. Due to their more crystalline structure, the MC films were significantly stronger (~26 MPa) than the CS films (~4 MPa). In turn, CS produced films with lower water vapor permeability (WVP, 50.12-51.74 vs. 56.52-59.10 g mm m-2 d-1 kPa-1). The hydrothermally-disrupted starch granules contributed to high roughness and opacity of the CS films. The FE-supplemented films exhibited an intensive yellow color and improved the UV-absorbing effect. FE delayed starch retrogradation, as indicated by the reduced crystallinity and slightly improved transparency of the CS films. Incorporation of FE significantly enhanced the released radical scavenging activity (RSA) of the films, while did not affect the WVP and mechanical properties. Due to better FE-trapping capacity, the CS-based films exhibited lower antioxidant activity (RSA60min = 2.21-19.75%) as compared to the MC counterparts (RSA60min = 4.87-38.31%).

Momordin Ic induces G0/1 phase arrest and apoptosis in colon cancer cells by suppressing SENP1/c-MYC signaling pathway.

Momordin Ic (MI) is a natural pentacyclic triterpenoid enriched in various Chinese natural medicines such as the fruit of Kochia scoparia (L.) Schrad. Studies have shown that MI presents antitumor properties in liver and prostate cancers. However, the activity and potential mechanisms of MI against colorectal cancer remain elusive. Here, we showed that MI inhibited cell proliferation with G0/1 phase cell cycle arrest in colon cancer cells. Moreover, it was observed that MI increased apoptosis compared to untreated cells. Further investigation showed that the SUMOylation of c-Myc was enhanced by MI and led to the down-regulated protein level of c-Myc, which is involved in regulating cell proliferation and apoptosis. SENP1 has been demonstrated to be critical for the SUMOylation of c-Myc. Meanwhile, knockdown of SENP1 by siRNA abolished the effects of MI on c-Myc level and cell viability in colon cancer cells. Together, these results revealed that MI exerted an anti-tumor activity in colon cancer cells via SENP1/c-Myc signaling pathway. These finding provide an insight into the potential of MI for colon cancer therapy.

In Vitro Human Skin Penetration, Antioxidant and Antimicrobial Activity of Ethanol-Water Extract of Fireweed (Epilobium angustifolium L.).

Epilobium angustifolium L. is applied as an antiseptic agent in the treatment of skin diseases. However, there is a lack of information on human skin penetration of active ingredients with antioxidative potential. It seems crucial because bacterial infections of skin and subcutaneous tissue are common and partly depend on oxidative stress. Therefore, we evaluated in vitro human skin penetration of fireweed ethanol-water extracts (FEEs) by determining antioxidant activity of these extracts before and after penetration study using 2,2-diphenyl-1-picrylhydrazyl (DPPH), 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS), and Folin-Ciocalteu methods. Microbiological tests of extracts were done. The qualitative and quantitative evaluation was performed using gas chromatography-mass spectrometry (GC-MS) and high-performance liquid chromatography (HPLC-UV) methods. The in vitro human skin penetration using the Franz diffusion chamber was assessed. The high antioxidant activity of FEEs was found. Gallic acid (GA), chlorogenic acid (ChA), 3,4-dihydroxybenzoic acid (3,4-DHB), 4-hydroxybenzoic acid (4-HB), and caffeic acid (CA) were identified in the extracts. The antibacterial activities were found against Serratia lutea, S. marcescens, Bacillus subtilis, B. pseudomycoides, and B. thuringiensis and next Enterococcus faecalis, E. faecium, Streptococcus pneumoniae, Pseudomonas aeruginosa, and P. fluorescens strains. In vitro penetration studies showed the penetration of some phenolic acids and their accumulation in the skin. Our results confirm the importance of skin penetration studies to guarantee the efficacy of formulations containing E. angustifolium extracts.

Kochia scoparia seed extract suppresses VEGF-induced angiogenesis via modulating VEGF receptor 2 and PI3K/AKT/mTOR pathways.

Context: Kochia scoparia (L.) Schrad (Amaranthaceae), known as a traditional medicine in China, Japan and Korea, is reported to have various biological activities. However, K. scoparia seed extract (KSE) functional roles on angiogenesis and prostate cancer inhibition have not been elucidated. Objective: This study elucidates the effects of KSE on vascular endothelial growth factor (VEGF)-induced angiogenesis in human umbilical vein endothelial cells (HUVECs) and inhibition of proliferation in prostate cancer cells. Materials and methods: HUVECs were treated with 10-20 µg/mL of KSE and 20-50 ng/mL of VEGF for 12-72 h. Anti-angiogenesis properties of KSE were determined by wound healing, trans-well, tube formation, rat aortic ring assay and western blotting. Prostate cancer and normal cells were incubated with 10-250 µg/mL of KSE for 24 h, and cell viability was measured by SRB assay. Phenolic compounds in KSE were analyzed using a HPLC-PDA system. Results: IC50 for cell viability of HUVECs, LNCaP, PC-3, RC-58T and RWPE-1 by KSE were 30.64, 89.25, 123.41, 141.62 and >250 µg/mL, respectively. Treatment with KSE (20 µg/mL) significantly suppressed VEGF-induced migration, invasion and capillary-like structure formation of HUVECs and microvessel sprouting from rat aortic rings. In addition, KSE down-regulated PI3K/AKT/mTOR levels and phosphorylation of VEGF receptor 2 in HUVECs. 3-OH-tyrosol (1.63 mg/g) and morin hydrate (0.17 mg/g) were identified in KSE. Conclusions: KSE inhibits angiogenesis in HUVECs as well as proliferation in human prostate cancer cells, suggesting KSE may be useful herbal medicine for preventing progression of prostate cancer and angiogenesis.

Water-soluble exudates from seeds of Kochia scoparia exhibit antifungal activity against Colletotrichum graminicola.

Plant seed exudates are composed of complex mixtures of chemicals with potential for bioactive compounds with antimicrobial properties. This study focused on kochia (Kochia scoparia), one of many weedy plant species considered invasive in many agricultural systems. Extraction of compounds in water yielded an exudate mass equivalent to 7% of the original seed mass used. Water-soluble exudates were tested against 16 known plant pathogens in disk diffusion assays and kochia exudates were found to inhibit Colletotrichum graminicola, the fungal causative agent of anthracnose and stalk rot in maize. The narrow range of fungi found as targets suggested the mechanism of inhibition may be specific rather than broadly antifungal. A decline in viability of cells over four orders of magnitude occurred within six hours of exposure to exudate. The minimum inhibitory concentration was 3.125 mg L-1. Hyphae formation in C. graminicola appeared inhibited following exposure to the exudate. Small molecular weight compounds as determined by GC/MS analysis showed high relative amounts of the sugars fructose, galactopyranose, glucose, and sorbitol, along with moderate proportions of organic acids and amino acids. Protein content averaged 0.7% in the standard concentration (100 mg mL-1) used for inhibition assays. Size fractionation of the exudate and subsequent disk diffusion assays revealed bioactive fractions with compounds in the MW range <5 kDa. To the best of our knowledge, this study is the first to show promising bioactivity against C. graminicola that was associated with water-extractable compounds from a common weed species. The results suggest that seeds of persistent plant species with long-lived seed banks like kochia may have potential for use in the discovery of compounds active in inhibiting fungal pathogens.

A Mixture of Extracts of Kochia scoparia and Rosa multiflora with PPAR α/γ Dual Agonistic Effects Prevents Photoaging in Hairless Mice.

Activation of peroxisome proliferator-activated receptors (PPAR) α/γ is known to inhibit the increases in matrix metalloproteinase (MMP) and reactive oxygen species (ROS) induced by ultraviolet light (UV). Extracts of natural herbs, such as Kochia scoparia and Rosa multiflora, have a PPAR α/γ dual agonistic effect. Therefore, we investigated whether and how they have an antiaging effect on photoaging skin. Eighteen-week-old hairless mice were irradiated with UVA 14 J/cm² and UVB 40 mJ/cm² three times a week for 8 weeks. A mixture of extracts of Kochia scoparia and Rosa multiflora (KR) was topically applied on the dorsal skin of photoaging mice twice a day for 8 weeks. Tesaglitazar, a known PPAR α/γ agonist, and vehicle (propylene glycol:ethanol = 7:3, v/v) were applied as positive and negative controls, respectively. Dermal effects (including dermal thickness, collagen density, dermal expression of procollagen 1 and collagenase 13) and epidermal effects (including skin barrier function, epidermal proliferation, epidermal differentiation, and epidermal cytokines) were measured and compared. In photoaging murine skin, KR resulted in a significant recovery of dermal thickness as well as dermal fibroblasts, although it did not change dermal collagen density. KR increased the expression of dermal transforming growth factor (TGF)-ß. The dermal effects of KR were explained by an increase in procollagen 1 expression, induced by TGF-ß, and a decrease in MMP-13 expression. KR did not affect basal transepidermal water loss (TEWL) or stratum corneum (SC) integrity, but did decrease SC hydration. It also did not affect epidermal proliferation or epidermal differentiation. KR decreased the expression of epidermal interleukin (IL)-1α. Collectively, KR showed possible utility as a therapeutic agent for photoaging skin, with few epidermal side effects such as epidermal hyperplasia or poor differentiation.

Kochia scoparia induces apoptosis of oral cancer cells in vitro and in heterotopic tumors.

ETHNOPHARMACOLOGICAL RELEVANCE: Kochia scoparia grows commonly in China, Japan, and Korea and its mature fruit has been used throughout the area in traditional medicine to treat diseases including skin problems and inflammatory and allergic disease. More importantly, Kochia scoparia has been prescribed to treat the malignant tumor of head and neck region and breast mass. Although it has been proposed as an anti-cancer agent for several cancers, its exact in vivo anti-cancer properties and the molecular mechanisms underlying its effects are poorly understood. AIM OF THE STUDY: To evaluate the anti-cancer activity of the methanol extract of K. scoparia, mature fruit (MEKS) on oral squamous cell carcinoma (OSCC) and to explore its mode of action. MATERIALS AND METHODS: To assess proliferation inhibition and apoptosis induction by MEKS, MTT assays, cell analysis, ANNEXIN V and PI double staining, and Hoechst 33342 staining were performed. The activation of caspases and the MAP kinase p38 was evaluated using Western blot analysis. The anti-cancer properties of MEKS in vivo were elucidated in a heterotopic OSCC animal model. RESULTS: After OSCC cells were treated with MEKS, the numbers of sub-G1 accumulated cells and apoptotic bodies increased, indicating that MEKS inhibited OSCC cell proliferation selectively through induction of apoptosis. Apoptosis of MEKS-treated OSCC cells was induced in a dose-dependent manner by caspase-3 and -9 activation. In addition, pretreatment with p38 inhibitor SB203580 in combination with MEKS significantly prevented MEKS-induced apoptosis in OSCC cells and also decreased cleaved capase 3, 9, and cleaved PARP activity in western blotting. MEKS treatment significantly increased the apoptosis of OSCC and inhibited tumour growth in our animal model. CONCLUSION: Taken together, these results indicated that MEKS induced apoptosis of OSCC cells through caspase activation involving the p38 MAPK pathway. MEKS could be a promising anti-cancer candidate for OSCC treatment.

Anti-inflammatory activity of Kochia scoparia fruit on contact dermatitis in mice.

The mature fruit of Kochia scoparia (L.) Schrad. is widely administered in China and Korea as a medicinal herb for treatment of skin diseases, diabetes mellitus and rheumatoid arthritis. The present study investigated the effects of methanol extracts of K. scoparia dried fruit (MEKS) on ear swelling, histopathological changes (such as epidermal acanthosis, spongiosis and immune cell infiltration) and cytokine production in 1-fluoro-2,4-dinitrofluorobenzene (DNFB)-induced contact dermatitis mice. Topical application of MEKS inhibited DNFB-induced ear thickness and weight increases, as well as DNFB-induced epidermal acanthosis, spongiosis and immune cell infiltration. In addition, treatment with MEKS significantly decreased the levels of tumor necrosis factor-α, interferon-γ and monocyte chemotactic protein-1 in inflamed tissues. These data indicate that the mature fruit of K. scoparia has the potential to be administered for the treatment of inflammatory skin diseases and that the anti-inflammatory action of K. scoparia is involved in the inhibition of type 1 T helper cell skewing reactions.

A selective and sensitive method based on UPLC-MS/MS for quantification of momordin Ic in rat plasma: application to a pharmacokinetic study.

A selective and sensitive method was developed and validated based on ultra-performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS). This method was applied to quantify momordin Ic in rat plasma. Chromatographic separation was performed on a Hypersil GOLD HPLC C18 column (150mm×4.6mm, 5µm) using an isocratic mobile phase of acetonitrile/water (80:20, v/v) at a flow rate of 0.6mL/min. An electrospray ionization source was applied and operated in negative ion mode; selected reaction monitoring (SRM) mode was used for quantification by monitoring the precursor-to-product ion transitions of m/z 763.4→m/z 455.3 for momordin Ic, and m/z 649.4→m/z 487.3 for IS. Calibration curves showed good linearity over the range of 22.0-2200ng/mL for momordin Ic in rat plasma. The developed method was applied to a pharmacokinetic study of momordin Ic in rats after single intravenous doses at 0.52, 1.56, and 4.67mg/kg. The elimination half-life (t1/2) values were 1.22±0.39, 1.14±0.10, and 1.83±0.39h, respectively. The plasma concentration at 2min (C2min) and area under the curve (AUC) for the intravenous doses of momordin Ic were approximately dose proportional.

Evaluation of phytochemical composition of fresh and dried raw material of introduced Chamerion angustifolium L. using chromatographic, spectrophotometric and chemometric techniques.

Due to the wide spectrum of biological activities, Chamerion angustifolium L. as medicinal plant is used for the production of food supplements. However, it should be kept in mind that quality (biological activity) of the herb depends on its geographic origin, the way of raw material preparation or extraction and chemotype. The purpose of this study was to evaluate and compare the compositions of volatile, non-volatile compounds and antioxidant activities of C. angustifolium grown in Kaunas Botanical Garden after the introduction from different locations in Lithuania. The compositions of fresh and air-dried samples were compared. The profile of volatile compounds was analyzed using headspace solid phase microextraction coupled with GC/MS. trans-2-Hexenal (16.0-55.9% of all volatiles) and trans-anethole (2.6-46.2%) were determined only in the dried samples, while cis-3-hexenol (17.5-68.6%) only in fresh samples. Caryophyllenes (α- and ß-) were found in all analyzed samples, contributing together from 2.4% to 52.3% of all volatiles according to the origin and preparation (fresh or dried) of a sample. Total amount of phenolic compounds, total content of flavonoids and radical scavenging activity (using 2,2-diphenyl-1-picrylhydrazyl (DPPH)) were determined using spectrophotometric assays. The variation of total phenolic compounds content was dependent on the sample origin, moreover, drying reduced amount of phenolics 1.5-3.5 times. The DPPH free radical scavenging activity was in the range of 238.6-557.1mg/g (expressed in rutin equivalents) in the fresh samples and drastically reduced to 119.9-124.8 mg/g after drying. The qualitative analysis of phenolic compounds in the aqueous methanolic extracts of C. angustifolium was performed by means of HPLC with UV detection. Oenothein B and rutin were predominant in the samples; also caffeic and chlorogenic acids, and quercetin were determined. Chemometric methods, namely principal component analysis, hierarchical cluster analysis and K-means clustering analysis, were applied for evaluation of the results. Chemometric analysis showed existence of different chemotypes of C. angustifolium L. and their relation to the geographic origin.

Topical application of Kochia scoparia inhibits the development of contact dermatitis in mice.

ETHNOPHARMACOLOGICAL RELEVANCE: Kochia scoparia (Chenopodiaceae) has been reported to have anti-nociceptive, anti-inflammatory, anti-allergic, and anti-pruritic actions. This study investigated the anti-inflammatory effects of externally applied Kochia scoparia water extract (KSW) in 2,4-dinitrochlorobenzene (DNCB)-induced contact dermatitis mouse model. MATERIALS AND METHODS: To develop atopic dermatitis-like skin lesions, 100µL of 1% DNCB in acetone/olive oil (4:1) had been applied for three days on shaved dorsal skin. 1% KSW was topically applied to DNCB-induced mice. After KSW treatment, histological analysis was measured by hematoxylin eosin staining. The cytokine and pro-inflammatory expressions were examined using reverse transcription polymerase chain reaction and western blotting analysis. RESULTS: Histological studies showed that hyperplasia of the epidermis and dermis in the KSW treated group was markedly decreased as compared with the DNCB group. The expression levels of pro-inflammatory cytokine such as IL-1ß, and TNF-α mRNA were significantly reduced by topical application of KSW, whereas these cytokines were increased in DNCB-induced dorsal skin. In addition, NF-κB expression was inhibited by KSW treatment in DNCB-induced mice. Similarly, KSW treatment significantly suppressed the expression of several MAP kinases, including ERK1/2, p38, and JNK compared to their expression in DNCB-induced mice. CONCLUSIONS: These findings indicated that KSW ameliorates contact dermatitis via inhibition of the production of several inflammatory mediators. Therefore, external application of KSW may be used for the treatment of contact dermatitis as an alternative therapy.

A novel mechanism for momordin Ic-induced HepG2 apoptosis: involvement of PI3K- and MAPK-dependent PPARγ activation.

Momordin Ic is a natural triterpenoid saponin found in various Chinese and Japanese natural medicines such as the fruit of Kochia scoparia (L.) Schrad. Momordin Ic has been previously demonstrated to induce HepG2 cell apoptosis in a ROS-mediated PI3K and MAPK pathway-dependent manner. In the present study, the underlying mechanisms of PI3K and MAPK pathway-mediated PPARγ, and PGC-1α co-regulator activation, as well as the effects of downstream proteins, COX-2 and FoxO4, on cell apoptosis were investigated. The results demonstrated that momordin Ic activated PPARγ and inhibited COX-2. PGC-1α and FoxO4 expressions were increased by the PI3K or MAPK pathways. Furthermore, PPARγ inhibition decreased p-p38 and FoxO4 expression, and restored COX-2 expression. ROS inhibition exerted little effect on PPARγ, COX-2 and FoxO4 expression but affected PGC-1α expression. These results revealed the involvement of PI3K and MAPK-dependent PPARγ activation in momordin Ic-induced apoptosis, providing more detailed information underlying the pro-apoptotic mechanism of momordin Ic in HepG2 cell apoptosis.

Studies on the flavone glycosides from Fructus Kochiae.

A series of flavone glycosides were isolated from Fructus Kochiae for the first time, including two new flavone glycosides. The structures were established by interpretation of their spectroscopic data. Two new flavone glycosides are quercetin 3-O-ß-d-apiofuranosyl-(1 â†’ 2)-ß-d-galactopyranosyl-7-O-ß-d-glucopyranoside (1) and quercetin 3-O-α-l-rhamnopyranosyl-(1 â†’ 6)-ß-d-galactopyranosyl-7-O-ß-d-sophoroside (2). The others are quercetin 7-O-ß-d-glucopyranoside (3), quercetin 3-O-ß-d-apiofuranosyl-(1 â†’ 2)-ß-d-galactopyranoside (4), quercetin 3-O-ß-d-galactopyranosyl-7-O-ß-d-glucopyranoside (5), and quercetin 7-O-ß-d-sophoroside (6).

[Study on chemical constituents of Kochia scoparia].

OBJECTIVE: To investigate the chemical constituents of Kochia scoparia. METHODS: The constituents of EtOAc-soluble portion were isolated and purified by silica gel column chromatography. Their structures were identified by spectral features. RESULTS: Twelve compounds were isolated and identified as tectorigenin (1), pratensein (2), 5,2'-dihydroxy-6,7-methylenedioxyisoflavone (3), iriflogenin (4), 5-hydroxy-6, 7-methylenedioxyflavone (5), fumalicacid (6), N-trans-feruloylmethoxytyramine (7), N-transferuloyltyramine (8), stigmasterol (9), oleanolic acid (10), beta-stigmasterol (11), daucosterol (12). CONCLUSION: compounds 1-9 are isolated from this plant for the first time.

In vivo anthelmintic activity of Dryopteris crassirhizoma, Kochia scoparia, and Polygala tenuifolia against Dactylogyrus intermedius (Monogenea) in goldfish (Carassius auratus).

In order to find natural agents against Dactylogyrus intermedius in goldfish, petroleum ether, chloroform, ethyl acetate, acetone, and methanol extracts of three medicinal plants (Dryopteris crassirhizoma, Kochia scoparia, and Polygala tenuifolia) were screened for antiparasitic properties using in vivo anthelmintic efficacy assay. Among these extracts investigated, methanolic extract of D. crassirhizoma was observed the most effective with EC50 value of 22.97 mg L⁻¹ after 48 h of exposure, which exhibited a 100% efficacy against D. intermedius at 60.00 mg L⁻¹, followed by the methanolic extracts of K. scoparia and P. tenuifolia with EC50 values of 31.28 and 154.79 mg L⁻¹, showing 100% efficacy against D. intermedius at 60.00 and 500.00 mg L⁻¹, respectively. In addition, acute toxicity assay indicated that 48-h LC50 values of methanolic extracts of D. crassirhizoma, K. scoparia, and P. tenuifolia were 4.10-, 2.27-, and 5.00-fold higher than the corresponding EC50. The obtained results demonstrated that methanolic extracts of D. crassirhizoma, K. scoparia, and P. tenuifolia have the potential for the development of novel therapy for the control of D. intermedius in aquaculture.

[Normative research on bacteriostasis and relieving itching external therapeutic function of kochiae fructus].

OBJECTIVE: To normalize bacteriostasis and relieving itching external therapeutic function of Kochiae Fructus. METHODS: Itching guinea pig model caused by histamine, itching mice model, eczema guinea pig model caused by OVA, and inhibitory effect on pathogens in vitro were used to observe the itching threshold, symptoms and other related physiological index, as well as the inhibitory effect on the normal skin fungi by water extraction of Kochiae Fructus to evaluate the external therapeutic function of Kochiae Fructus. RESULTS: The itching threshold of guinea pig itching model treated by water extraction of Kochiae Fructus at high, medium and low three dosage level, could be significantly increased when compared with negative control group (P < 0.05 or P < 0.01); Red speckle of OVA guinea pig model treated by water extraction of Kochiae Fructus at high, medium and low three dosage level, could be significantly decreased when compared with negative control group (P < 0.05 or P < 0.01); The number of itching and total time of itching within 30 minutes of mice model caused by R-glycose anhydride treated by water extraction of Kochiae Fructus at high, medium and low three dosage level, could be significantly decreased when compared with negative control group (P < 0.05 or P < 0.01); Several common skin fungi could be significantly inhibited by the water extraction of Kochiae Fructus. MIC of the water extraction of Kochiae Fructus on Trichophyton mentagrophytes, Trichophyton rubrum, Microsporum canis, Trichophyton violaceum, and Trichophyton schoenleini were 3.12%, 0.78%, 0.78%, 0.78%, 0.78%, respectively. CONCLUSION: Kochiae fructus has the effect of bacteriostasis and relieving itching.

[Preparation of water in oil type cream with high content of water containing Kochia scoparia fruit and Cnidium monnieri fruit].

Kikisui is a herbal lotion containing Kochia scoparia Fruit and Cnidium monnieri Fruit that is clinically used as an antipruritic for itchy dry skin. However, this formulation is unsuitable for inducing a prolonged effect. Here, we attempted to change the formulation from a lotion to a cream. The cream we chose was a water-in-oil (W/O) type emulsion for enhancing skin compatibility. In addition, the high water content imparts a sensation of coolness. However, it is difficult to prepare a stable W/O type cream with high water content using a mechanical mixing method. Instead, we prepared the W/O type emulsion using liquid crystals. Water containing cocamidopropyl betaine was added to a dispersed phase comprising an oil phase of oleic acid and liquid paraffin that was constantly stirred. Addition of an aqueous solution containing Kochia scoparia Fruit and Cnidium monnieri Fruit decreased the stability of the cream. However, addition of glycerin as a humectant, and ethyl p-hydroxybenzoate/n-butyl p-hydroxybenzoate as preservatives enhanced the stability of the cream. The stability of the emulsion was correlated with the apparent viscosity of the cream. The final W/O type cream had a water content of 83% and was stable for more than 6 months at 4°C. Furthermore, ostol, which is one of the main biologically active herbal compounds, was also stable for more than 6 months.

Reduction of fat storage in mice fed a high-fat diet long term by treatment with saponins prepared from Kochia scoparia fruit.

The fresh fruit (Japanese name, Tonburi) of Kochia scoparia has been used as a food garnish in Japanese-style dishes from ancient times, and may prevent metabolic syndromes such as hyperlipidemia, hypertension, obesity and atherosclerosis. This study was performed to clarify whether an ethanol extract of K. scoparia fruit prevented obesity induced in mice by a high-fat diet for 9 weeks. The ethanol extract of K. scoparia fruit prevented the increases in body weight and parametrial adipose tissue weight induced by the high-fat diet. Furthermore, consumption of a high-fat diet containing 1% or 3% K. scoparia extract significantly increased the fecal content and the fecal triacylglycerol level at day 3 compared with those in the high-fat diet group. The ethanol extract (250 mg/kg) and total saponins (100 mg/kg) of K. scoparia inhibited the elevation of the plasma triacylglyccerol level 2 or 3 h after the oral administration of the lipid emulsion. Total saponins, momordin Ic, 2'-O-beta-d-glucopyranosyl momordin Ic and 2'-O-beta-d-glucopyranosyl momordin IIc isolated from K. scoparia fruit inhibited the pancreatic lipase activity (in vitro). These findings suggest that the anti-obesity actions of K. scoparia extract in mice fed a high-fat diet may be partly mediated through delaying the intestinal absorption of dietary fat by inhibiting pancreatic lipase activity.

Acaricidal activities of extracts of Kochia scoparia against Tetranychus urticae, Tetranychus cinnabarinus, and Tetranychus viennensis (Acari: Tetranychidae).

Extracts of an annual herbaceous plant, Kochia scoparia (L.) Schrad (Macrophomina), were bioassayed to determine their acaricidal activities against Tetranychus urticae Koch, Tetranychus cinnabarinus (Boisduval), and Tetranychus viennensis Zacher (Acari: Tetranychidae) in the laboratory. Extracts had both contact and systemic toxicity to these mites. Three solvents were tested for preparing crude extracts: petroleum ether, chloroform, and methanol. Methanol was the most effective solvent, extracting 3.11-4.53% of the acaricide. Petroleum ether was the least effective solvent, extracting 1.25-1.54%. However, extracts with chloroform resulted in the highest mite mortality (78.86%), and ultrasound-assisted extraction required the least time (10 min). Concentrated extracts were prepared using chloroform, methyl acetate, or distilled water as a solvent. Mite mortalities from the concentrated extracts by methyl acetate or distilled water were significantly lower than those by chloroform. The mean lethal concentrations (LC50) of the extracts by chloroform, methyl acetate, and distilled water to the mites were 0.71 +/- 0.06, 2.08 +/- 0.16 and 8.75 +/- 0.062 mg/ml, respectively. After liquid chromatography and thin layer chromatography, the concentrated extracts by chloroform were separated into seven groups of isolated fractions and tested for acaricidal activity.

Inhibition of methanol extract from the fruits of Kochia scoparia on lipopolysaccharide-induced nitric oxide, prostaglandin [correction of prostagladin] E2, and tumor necrosis factor-alpha production from murine macrophage RAW 264.7 cells.

In an attempt to search for bioactive natural products exerting antiinflammatory activity, we have evaluated the effects of the methanol extract of the fruits of Kochia scoparia (L.) CHARD. (Chenopodiaceae) on lipopolysaccharide (LPS)-induced nitric oxide (NO), prostaglandin E(2) (PGE(2)), and tumor necrosis factor (TNF)-alpha release by the macrophage cell line RAW 264.7. Our data indicate that this extract is a potent inhibitor of NO production and it also significantly decreased PGE(2) and TNF-alpha release. Consistent with these observations, the protein and mRNA expression level of inducible NO synthase (iNOS) and cyclooxygenase (COX)-2 was inhibited by MeOH extracts of Kochia scoparia (KSM) in a dose-dependent manner. Furthermore, KSM inhibited the LPS-induced DNA binding activity of nuclear factor-kappaB (NF-kappaB), which was associated with prevention of the inhibitor kappaB degradation. These results suggest that the methanol extract of K. scoparia inhibits LPS-induced iNOS and COX-2 expression by blocking NF-kappaB activation.