Quantification Analysis and <i>In Vitro</i> Anti-Inflammatory Effects of 20-Hydroxyecdysone, Momordin Ic, and Oleanolic Acid from the Fructus of <i>Kochia scoparia</i>

Yoo, Sae-Rom,Jeong, Soo-Jin,Lee, Na-Ri,Shin, Hyeun-Kyoo,Seo, Chang-Seob Medknow PublicationsMedia Pvt Ltd 2017 Pharmacognosy magazine Vol.13 No.51

<P><B>Background:</B></P><P>The fructus of <I>Kochia scoparia</I> Schrader (Chenopodiaceae) is a traditional herbal medicine that has been used for treating gonorrhea and dermatitis.</P><P><B>Objective:</B></P><P>We investigated the anti-inflammatory activities of three marker compounds, including 20-hydroxyecdysone, momordin Ic, and oleanolic acid, from the fructus of <I>K. scoparia</I>.</P><P><B>Materials and Methods:</B></P><P>The simultaneous analysis of three components was performed using high-performance liquid chromatography and high-performance thin-layer chromatography. We evaluated the anti-inflammatory effects of the nine marker compounds by determining their anti-inflammatory activities in the murine macrophage cell line RAW 264.7.</P><P><B>Results:</B></P><P>Among three marker compounds, momordin Ic, but not 20-hydroxyecdysone and oleanolic acid, had inhibitory effects on the production of inflammatory cytokines tumor necrosis factor-alpha (TNF-α) and interleukin-6 (IL-6) in LPS-treated RAW264.7 macrophages. The effects of three marker compounds on prostaglandin E<SUB>2</SUB>(PGE<SUB>2</SUB>) were also evaluated. All three compounds significantly reduced PGE<SUB>2</SUB> production in LPS-treated cells.</P><P><B>Conclusions:</B></P><P>We suggest that momordin Ic is the most potent phytochemical of the fructus of <I>K. scoparia</I> as an anti-inflammatory agent.</P><P><B>SUMMARY</B></P><P><P>Simultaneous analysis of three phenylpropanoids in the <I>Kochia scoparia</I> was established using HPLC-PDA system</P><P>The momordin Ic had inhibitory effects on production of inflammatory cytokines tumor necrosis factor-alpha (TNF-α) and interleukin-6 (IL-6) in LPS-treated RAW264.7 macrophages</P><P>The momordin Ic, 20-hydroxyecdysone, and oleanolic acid significantly reduced PGE2 production in LPS-treated cells.</P></P> >[FIG OMISSION]</BR><P><B>Abbreviations used:</B> HPLC: High-performance liquid chromatography; TNF-α: Tumor necrosis factor alpha; IL-6: Interleukin-6; PGE<SUP>2</SUP>: Pro-inflammatory mediator prostaglandin E<SUB>2</SUB>; LPS: Lipopolysaccharide.</P>

<i>Kochia scoparia</i> fruit attenuates allergic airway inflammation in ovalbumin (OVA)-induced murine asthma model

Lee, Mee-Young,Shin, In-Sik,Lim, Hye-Sun,Seo, Chang-Seob,Ha, Hyekyung,Shin, Hyeun-Kyoo Informa Healthcare 2011 Inhalation toxicology Vol.23 No.14

<P><I>Kochia scoparia</I> fruit has been used in Asia for a long time. It possesses anti-inflammatory, antiallergic, and antipruritic actions. We investigated the role of a <I>K. scoparia</I> fruit ethanolic extract (KSEE) in allergic airway inflammation in a mouse asthma model. BALB/c mice were sensitized with ovalbumin (OVA) and, upon OVA aerosol challenge, developed airway eosinophilia, mucus hypersecretion, elevations in cytokine, chemokine, and immunoglobulin levels, and upregulation of MMP-9, intercellular adhesion molecule-1 (ICAM-1), and vascular cell adhesion molecule-1 (VCAM-1) expression. Intragastric administration of KSEE significantly attenuated OVA-induced influx of total leukocytes, eosinophils, neutrophils, macrophages, and lymphocytes into lungs, as well as attenuating levels of interleukin (IL)-4 and IL-5 in a dose-dependent manner. KSEE also significantly reduced the serum levels of total and OVA-specific immunoglobulin (Ig)E and OVA-specific IgG1 release into the airspace. Histological studies showed that KSEE inhibited OVA-induced lung tissue eosinophilia and airway mucus production. Moreover, in whole lung tissue lysates, immunoreactivity showed that KSEE markedly attenuated the OVA-induced increase in expression of ICAM-1, VCAM-1, and MMP-9. These results show that KSEE possesses protective effects against allergic airway inflammation, acts as an MMP-9 inhibitor, and induces a reduction in ICAM-1 and VCAM-1 expression.</P>

Saponins from the Fructus of Kochia scoparia

Whang, Wan-Kyunn,Hahn, Dug-Ryong The Pharmaceutical Society of Korea 1991 Archives of Pharmacal Research Vol.14 No.2

Two new triterpenoidal saponins B(1) and C(2) were isolated from the fructus of Kochia scoparia. On the basis of chemico-spectral evidences, the structures of 1 and 2 were elucidated as oleanolic acid 3-O-$\beta$-D-ribopyranosyl-(1$\rightarrow$2)-.betha.-D-glucuronopyranoside and 3-O-$\beta$-D-xylopyranosyl-(1$\rightarrow$3)-$\beta$-D-glucuronopyranosyl-olean-12-en-28-O-$\beta$-D-glucopyranosyl ester, respectively.

Immunochemical and molecular characterization of allergenic profilin (Koc s 2) from Kochia scoparia pollen

Farnoosh Zarinhadideh,Akram Amini,Mohammad-Ali Assarehzadegan,Seyed-Hamid Borsi,Najmeh Sepahi,Hosein Ali-Sadeghi 한국응용생명화학회 2015 Applied Biological Chemistry (Appl Biol Chem) Vol.58 No.3

Kochia scoparia pollen has been demonstrated as an important cause of pollinosis in tropical and subtropical regions of the world. The aim of this study was to characterize the IgE-binding protein of the Kochia pollen extract and production of recombinant form of allergenic profilin of this weed. To predict its allergenic cross-reactivity with profilins of common allergenic plants, nucleotide sequence homology of Kochia profilin was evaluated. Specific ELISA and immunoblotting assay were applied to determine the IgE-binding reactivity of 28 sera collected from patients who were sensitized to Kochia pollen. In cloning procedure, the Kochia profilin-coding sequence was inserted into PTZ57R/T vector and expressed using pET-21b(?) vector. IgE-binding competence of purified recombinant Kochia profilin (rKoc s 2) was analyzed by in vitro assays. There were several protein bands in Kochia pollen extract with molecular weights approximately ranging from 14.5 to 85 kDa. Nucleotide sequencing revealed an open reading frame of 399 bp encoding for 133 amino acid residues which belonged to the profilin family; 15 patients (15/28, 53.1 %) had significant specific IgE levels for the rKoc s 2. Immunodetection and inhibition assays indicated that the purified rKoc s 2 might be the same as that in the crude extract. Koc s 2, the first allergen from the Kochia pollen was identified as a member of the family of profilins. High degree of homology was found among amino acid sequences of Kochia profilin and several profilin molecules from unrelated plant families.

Immunochemical and molecular characterization of allergenic profilin (Koc s 2) from Kochia scoparia pollen

Zarinhadideh, Farnoosh,Amini, Akram,Assarehzadegan, Mohammad-Ali,Borsi, Seyed-Hamid,Sepahi, Najmeh,Ali-Sadeghi, Hosein 한국응용생명화학회 2015 Applied Biological Chemistry (Appl Biol Chem) Vol.58 No.3

Kochia scoparia pollen has been demonstrated as an important cause of pollinosis in tropical and sub-tropical regions of the world. The aim of this study was to characterize the IgE-binding protein of the Kochia pollen extract and production of recombinant form of allergenic profilin of this weed. To predict its allergenic cross-reactivity with profilins of common allergenic plants, nucleotide sequence homology of Kochia profilin was evaluated. Specific ELISA and immunoblotting assay were applied to determine the IgE-binding reactivity of 28 sera collected from patients who were sensitized to Kochia pollen. In cloning procedure, the Kochia profilin-coding sequence was inserted into PTZ57R/T vector and expressed using pET-21b(+) vector. IgE-binding competence of purified recombinant Kochia profilin (rKoc s 2) was analyzed by in vitro assays. There were several protein bands in Kochia pollen extract with molecular weights approximately ranging from 14.5 to 85 kDa. Nucleotide sequencing revealed an open reading frame of 399 bp encoding for 133 amino acid residues which belonged to the profilin family; 15 patients (15/28, 53.1 %) had significant specific IgE levels for the rKoc s 2. Immunodetection and inhibition assays indicated that the purified rKoc s 2 might be the same as that in the crude extract. Koc s 2, the first allergen from the Kochia pollen was identified as a member of the family of profilins. High degree of homology was found among amino acid sequences of Kochia profilin and several profilin molecules from unrelated plant families.

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

Han, H.Y.,Lee, H.E.,Kim, H.J.,Jeong, S.H.,Kim, J.H.,Kim, H.,Ryu, M.H. Elsevier Ireland Ltd 2016 Journal of Ethnopharmacology Vol.192 No.-

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.

The Extract of Kochia scoparia Fruit Induces Programmed Necrosis in Oral Squamous Cell Carcinoma Cells

Hye-Yeon Han,Bong-Soo Bark,Hyung Joon Kim,Seung-Hwa Jeong,Jiyeon Kim,Sung-Hee Jeong,Gyoo Cheon Kim,Dae-Seok Hwang,Uk-Kyu Kim,Hyungwoo Kim,Mi Heon Ryu 대한구강악안면병리학회 2016 대한구강악안면병리학회지 Vol.40 No.6

The fruit of Kochia scoparia Scharder is traditionally used as a medicinal ingredient to treat allergic skin diseases and inflammatory diseases in China, Japan and Korea. Recently, several studies reported that K. scoparia had potential for the cytotoxicity of human cancer cells. To investigate the anti-cancer effect of K. scoparia on oral cancer and to determine the specific type of cell death induced by MEKS treatment. We investigated the anti-cancer effects of K. scoparia, methanol extract (MEKS) in HSC4 human oral cancer cells. We examined the effects of MEKS on the proliferation rate, cell cycle arrest, 7-AAD-ANNEXIN V double stain, reactive oxygen species (ROS) generation and activation of apoptosis and necroptosis-associated proteins in HSC4 cells. MTT assay results demonstrated that MEKS decreased the proliferation rates of HSC4 cells in a dose-dependent manner with an IC50 value of 45.3 μg/ml. MEKS at 50 μg/ml significantly increased the sub-G1 DNA contents of HSC4 cells to 84.8%, versus untreated cells. However, the activation of apoptosis-associated proteins such as cleaved caspase 3, cleaved caspase 8, cleaved caspase 9 and cleaved Poly (ADP-ribose) polymerase (PARP) did not detect. The level of Bax protein markedly increased in MEKS-treated HSC4 cells. In addition, the cell viability of the DPQ pre-treated HSC4 cells with MEKS treatment was significantly greater than that of MEKS treated-cells. These results suggest that MEKS inhibits cell proliferation and induces necroptosis in oral cancer cells and that MEKS may have potential chemotherapeutic value for the treatment of human oral cancer.

The Extract of Kochia scoparia Fruit Induces Programmed Necrosis in Oral Squamous Cell Carcinoma Cells

한혜연,박봉수,김형준,정승화,김지연,정성희,김규천,황대석,김욱규,김형우,유미현 대한구강악안면병리학회 2016 대한구강악안면병리학회지 Vol.40 No.6

The fruit of Kochia scoparia Scharder is traditionally used as a medicinal ingredient to treat allergic skin diseases and inflammatory diseases in China, Japan and Korea. Recently, several studies reported that K. scoparia had potential for the cytotoxicity of human cancer cells. To investigate the anti-cancer effect of K. scoparia on oral cancer and to determine the specific type of cell death induced by MEKS treatment. We investigated the anti-cancer effects of K. scoparia, methanol extract (MEKS) in HSC4 human oral cancer cells. We examined the effects of MEKS on the proliferation rate, cell cycle arrest, 7-AAD-ANNEXIN V double stain, reactive oxygen species (ROS) generation and activation of apoptosis and necroptosis-associated proteins in HSC4 cells. MTT assay results demonstrated that MEKS decreased the proliferation rates of HSC4 cells in a dose-dependent manner with an IC50 value of 45.3 μg/ml. MEKS at 50 μg/ml significantly increased the sub-G1 DNA contents of HSC4 cells to 84.8%, versus untreated cells. However, the activation of apoptosis-associated proteins such as cleaved caspase 3, cleaved caspase 8, cleaved caspase 9 and cleaved Poly (ADP-ribose) polymerase (PARP) did not detect. The level of Bax protein markedly increased in MEKS-treated HSC4 cells. In addition, the cell viability of the DPQ pre-treated HSC4 cells with MEKS treatment was significantly greater than that of MEKS treated-cells. These results suggest that MEKS inhibits cell proliferation and induces necroptosis in oral cancer cells and that MEKS may have potential chemotherapeutic value for the treatment of human oral cancer.

Anti-Rheumatoid Arthritis Effect of the Kochia scoparia Fruits and Activity Comparison of Momordin Ic, its Prosapogenin and Sapogenin

Choi, Jongwon,Lee, Kyung-Tae,Jung, Hyun-Ju,Park, Hee-Sun,Park, Hee-Juhn The Pharmaceutical Society of Korea 2002 Archives of Pharmacal Research Vol.25 No.3

MeOH extract of Kochia scoparia was fractionated into $CHCl_3-$, EtOAc- and BuOH extracts and the last fraction were hydrolyzed by 3%-NaOH ($MeOH-H_2O$) to compare the bioactivities on antinociceptive and anti-inflammatory effects. Silica gel column chromatography of BuOH fraction afforded a large amount of $3-Ο-{\beta}-D-xylopyranosyl {\;}(1{\rightarrow}3)-{\beta}-D-glucuronopyranosyl$ oleanolic acid (momordin Ic, 4) and that of acid hydrolysate of BuOH fraction gave $3-Ο-{\beta}-D-glucuronopyranosyl oleanolic$ acid (momordin Ib, 3), its 6'-Ο-methyl ester (2) and oleanolic acid (1). Silica gel column chromatography of alkaline hydrolysate afforded a large amount of 4. MeOH extract and both EtOAc- and BuOH fractions were active in the rheumatoidal rat induced Freund's complete adjuvant reagent (FCA) whereas $CHCl_3$ fraction was inactive. Compound 1 and 4 showed significant activities in the same assay but oleanolic acid 3-Ο-glucuronopyranoside (3) showed no activity. These fashions were also observed in carrageenan-induced edema of the rat and in the antinociceptive activity tests undertaken in hot plate- and writhing methods. These results suggest that momordin Ic and its aglycone, oleanolic acid, could be active principles for rheumatoid arthritis.

Apoptosis and Autophagy Induced by Methanol Extract of Kochia scoparia in Human Mucoepidermoid Carcinoma Cell Line

도미향,유미현,김욱규 대한구강악안면병리학회 2018 대한구강악안면병리학회지 Vol.42 No.6

Natural products are vastly utilized as a source of chemotherapeutic agents for human cancers. Kochia scopraia is traditionally used for the cure of urological and dermatological diseases. Recently, methanol extract of Kochia scoparia (MEKS) has been shown to have anti-cancer activity to various human cancers. However, there is no report demonstrating the anti-cancer activity of MEKS in human mucoepidermoid carcinoma (MEC) cells. In this study, the authors studied the effects of MEKS on the cell proliferation and underlying mechanism in YD15 human MEC cells. MEKS decreased YD15 cell proliferation proven by trypan blue exclusion assay and induced apoptosis, evidenced by cell cycle analysis and western blotting. Autophagy induction by MEKS was verified by western blotting. In addition, MEKS regulated the expression of phosphorylated Akt, phosphorylated p38 and Nrf2 protein. This results can imply that MEKS might be a potential candidate for the treatment of human MEC cells.