Brain acetylcholinesterase activity and the protective effect of Gac fruit on scopolamine-induced memory impairment in adult zebrafish.

Gac fruit (Momordica cochinchinensis) belongs to the Cucurbitaceae family. This study aimed to investigate the anti-memory impairment effect of Gac fruit aril extract and brain acetylcholinesterase activity in adult zebrafish (Danio rerio). The behavioral test was performed using a color-biased appetite conditioning T-maze test and an inhibitory avoidance test to evaluate memory performance. The time spent in the green arm in the T-maze test was recorded, and latency time was recorded in the inhibitory avoidance test. Brain acetylcholinesterase (AChE) enzyme activity was measured using a 96-well microplate reader based on Ellman's method. Zebrafish that received rivastigmine and Gac extract had significantly increased time spent in the green arm and latency time when compared to the SCO group. Zebrafish that received rivastigmine and Gac fruit extract at 200 mg/kg had lower AChE activity than the SCO groups; however, there were no statistically significant differences between the groups. These findings suggest that Gac fruit extract has anti-memory impairment activity and may be beneficial for the development of health products to prevent Alzheimer's disease.

The complete plastome sequence of Momordica cochinchinensis (Cucurbitaceae).

Momordica cochinchinensis (Lour.) Spreng. is an important medicinal plant that is used to treat various diseases in South and Southeast Asia. In this study, the complete plastome of M. cochinchinensis was sequenced and found to exhibit a total length of 158,955 bp, with a large single copy (LSC) region of 87,924 bp and a small single copy (SSC) region of 18,479 bp, as well as with two inverted repeats (IRs) that were both 26,726 bp in length. In total, 129 genes were detected, comprising 86 protein-encoding genes, 8 ribosomal RNA (rRNA) genes, and 35 transfer RNA (tRNA) genes. Furthermore, the inferred phylogenetic tree confirmed that M. cochinchinensis belongs to the genus Momordica in the Cucurbitaceae family. The research results will be used for authenticating M. cochinchinensis plant materials and for analyzing the genetic diversity and phylogenetic relationships in Momordica.

Stem Extract from Momordica cochinchinensis Induces Apoptosis in Chemoresistant Human Prostate Cancer Cells (PC-3).

Natural compounds have been recognized as valuable sources for anticancer drug development. In this work, different parts from Momordica cochinchinensis Spreng were selected to perform cytotoxic screening against human prostate cancer (PC-3) cells. Chromatographic separation and purification were performed for the main constituents of the most effective extract. The content of the fatty acids was determined by Gas Chromatography-Flame Ionization Detector (GC-FID). Chemical structural elucidation was performed by spectroscopic means. For the mechanism of the apoptotic induction of the most effective extract, the characteristics were evaluated by Hoechst 33342 staining, sub-G1 peak analysis, JC-1 staining, and Western blotting. As a result, extracts from different parts of M. cochinchinensis significantly inhibited cancer cell viability. The most effective stem extract induced apoptosis in PC-3 cells by causing nuclear fragmentation, increasing the sub-G1 peak, and changing the mitochondrial membrane potential. Additionally, the stem extract increased the pro-apoptotic (caspase-3 and Noxa) mediators while decreasing the anti-apoptotic (Bcl-xL and Mcl-1) mediators. The main constituents of the stem extract are α-spinasterol and ligballinol, as well as some fatty acids. Our results demonstrated that the stem extract of M. cochinchinensis has cytotoxic and apoptotic effects in PC-3 cells. These results provide basic knowledge for developing antiproliferative agents for prostate cancer in the future.

Muyin extract inhibits non-small-cell lung cancer growth by inducing autophagy and apoptosis in vitro and in vivo.

BACKGROUND: Non-small cell lung cancer (NSCLC) is a major subtype of lung cancer with a higher mortality rate. Both apoptosis and autophagy are crucial processes in the pathophysiology of NSCLC. Muyin extract (MSE) is a combination of Momordica cochinchinensis (Lour.) Spreng seeds and Epimedium brevicornu Maxim extract, with an optimal ratio of 1:1. Our previous research has firstly shown that MSE exerts a good anti-tumor activity, especially for NSCLC. PURPOSE: This study aims to evaluate the inhibitory effect of MSE on NSCLC and explore the underlying mechanism. METHODS: In vitro, cell proliferation was examined by MTT and colony formation. Apoptosis was detected by annexin V-FITC/PI assay while autophagy was assessed by Acridine orange (AO) and Monodansylcadaverine (MDC) staining. In vivo, Lewis lung cancer cell transplanted mice model was established to measure the effect of MSE on tumor growth. Hematoxylin eosin (H & E) staining was used to observe the pathological changes of the tumor after MSE treatment. The apoptosis in tumor tissue was detected by TUNEL assay. Meanwhile, the cellular proliferation marker Ki67 and autophagy marker LC3Ⅱ were observed by immunohistochemistry staining. The IL-4 and IFN-γ concentrations in blood were tested by Elisa. The apoptosis related factors (Bcl-2, Bax Caspase-3, cleaved Caspase-3, Caspase-9 and p53), autophagy marker proteins (Atg-5, Becline-1, LC3Ⅱ/Ⅰand p62) as well as Akt/mTOR pathway were detected by western blotting. RESULTS: Present study showed that MSE greatly inhibited the proliferation of NSCLC in vitro and in vivo, together with apoptotic rate increasing. P53 and cleaved Caspase-3 levels were up-regulated while Bcl-2/Bax ratio, Caspase-3 and Caspase-9 levels were significantly down-regulated treated with MSE. Meanwhile, MSE activated autophagy, Atg-5, Becline-1 as well as the ratio of LC3Ⅱ/Ⅰ were notably up-regulated while p62 was down-regulated after MSE treatment. Importantly, MSE significantly blocked Akt/mTOR pathway, which is a common upstream signal triggered by autophagy and apoptosis. Furthermore, when co-treated with specific autophagy inhibitor, the inhibitory rate and anti-apoptotic Bcl-2 level were significantly reversed. Impressively, MSE remarkably increased IFN-γ/ IL-4 ratio while VP16 did not in animal model, and the inhibition rate in tumor weight after MSE treatment was higher than xiaojin pill. CONCLUSION: Taken together, it is proved that MSE may be a promising oral TCM candidate for NSCLC therapy with immunity improvement. The underlying mechanisms could be associated with the induction of apoptosis and autophagy through blocking Akt/mTOR pathway, meanwhile, it may promote crosstalk between autophagy and apoptosis.

Development and Evaluation of a Hydrogel containing Momordica cochinchinensis Spreng Extract for Topical Applications

Abstract The purpose of this research was to develop a hydrogel containing the extract of Gac fruit (Momordica cochinchinensis Spreng) with appropriate physicochemical properties and good dermatological efficacy. The Gac aril fruit was extracted by maceration in dichloromethane, and its antioxidant activity was determined through a DPPH assay. The very low water-solubility of the Gac extract is responsible for its incompatibility with the hydrogel. To overcome this drawback, LabrafacTM PG and Tween 60 were used to develop the hydrogel due to their potent potential for solubilizing the Gac extract. The prepared hydrogels displayed good physical properties, a homogenous orange gel, appropriate pH, and viscosity. After storage in an accelerated condition for six months, the hydrogels of the Gac extract had physical stability and high remaining amounts of beta-carotene and lycopene within the range of 90.25 - 94.61%. The skin efficacy of hydrogel containing the Gac fruit extract was found using 14 healthy female volunteers over a 30-day period of daily application. Topical application of the hydrogel containing the Gac fruit extract, which contains antioxidants, significantly moisturizes the skin and enhanced its elasticity (p ≤ 0.05; ANOVA). This makes it suitable for use as a skin care product

Momordica cochinchinensis Aril Ameliorates Diet-Induced Metabolic Dysfunction and Non-Alcoholic Fatty Liver by Modulating Gut Microbiota.

Obesity and its associated conditions, such as type 2 diabetes mellitus (T2DM) and nonalcoholic fatty liver disease (NAFLD), are a particular worldwide health problem at present. Momordica cochinchinensis (MC) is consumed widely in Southeast Asia. However, whether it has functional effects on fat-induced metabolic syndrome remains unclear. This study was conducted to examine the prevention effect of Momordica cochinchinensis aril (MCA) on obesity, non-alcoholic fatty liver and insulin resistance in mice. MCA protected the mice against high-fat diet (HFD)-induced body weight gain, hyperlipidemia and hyperglycemia, compared with mice that were not treated. MCA inhibited the expansion of adipose tissue and adipocyte hypertrophy. In addition, the insulin sensitivity-associated index that evaluates insulin function was also significantly restored. MCA also regulated the secretion of adipokines in HFD-induced obese mice. Moreover, hepatic fat accumulation and liver damage were reduced, which suggested that fatty liver was prevented by MCA. Furthermore, MCA supplementation suppressed hepatic lipid accumulation by activation of the AMP-activated protein kinase (AMPK) and peroxisome proliferator-activated receptor-alpha (PPAR-alpha) signaling pathway in the human fatty liver HuS-E/2 cell model. Our data indicate that MCA altered the microbial contents of the gut and modulated microbial dysbiosis in the host, and consequently is involved in the prevention of HFD-induced adiposity, insulin resistance and non-alcoholic fatty liver disease.

Anti-Inflammatory and anti-proliferative oleanane-type triterpene glycosides from the vine of Momordica cochinchinensis.

This research isolated two new oleanane-type triterpene glycosides, named mocochinosides A (1) and B (2), together with ten known compounds as chikusetsusaponin IVa ethyl ester (3), momordin Ib (4), momordin IIb (5), momordin II (6), calenduloside G (7), calenduloside H (8), elatoside A (9), elatoside C (10), calendulaglycoside C 6'-O-7-butyl ester (11), and hederagenin 3-O-ß-D-glucuronopyranoside (12) and characterized them from the vines of Momordica cochinchinensis. The new structures of both glycosides 1-2 were elucidated by spectroscopic analysis including 2 D NMR and MS, followed by an analysis of their anti-inflammatory and cytotoxic activities. Compounds 1, 4, and 11 showed moderate inhibitions for NO production on RAW264.7 macrophages induced by LPS at IC50 5.41 ∼ 11.28 µM. Compounds 3, 4, and 7 (IC50 8.42 ∼ 19.74 µM) exhibited potential anti-proliferative activities against both of WiDr and MCF-7 human tumor cell lines.

Anticancer activity of Momordica cochinchinensis (red gac) aril and the impact of varietal diversity.

BACKGROUND: Momordica cochinchinensis (Cucurbitaceae) is a nutritionally and medicinally important fruit restricted to South East Asia with diverse morphological and genetic variations but there is limited information on its medicinal potential. METHODS: M. cochinchinensis aril from 44 different samples in Australia, Thailand and Vietnam were extracted using different solvents and tested for its anticancer potential. Anticancer activity of M. cochinchinensis aril on breast cancer (MCF7 and BT474) and melanoma (MM418C1 and D24) cells were compared to control fibroblasts (NHDF). The cytotoxicity of the cells following treatment with the aril extract was determined using CCK-8 assay. Biochemical and morphological changes were analysed using flow cytometry, confocal and transmission electron microscopy to determine the mechanism of cell death. RESULTS: The water extract from the aril of M. cochinchinensis elicited significantly higher cytotoxicity towards breast cancer and melanoma cells than the HAE extract. The IC50 concentration for the crude water extract ranged from 0.49 to 0.73 mg/mL and induced both apoptotic and necrotic cell death in a dose- and time-dependant manner with typical biochemical and morphological characteristics. The greatest cytotoxicity was observed from Northern Vietnam samples which caused 70 and 50% melanoma and breast cancer cell death, respectively. CONCLUSIONS: The water extract of M. cochinchinensis aril caused significant apoptosis and necrosis of breast cancer and melanoma cells, with varieties from Northern Vietnam possessing superior activity. This highlights the potential of this fruit in the development of novel anticancer agents against such tumours, with specific regions on where to collect the best variety and extraction solvent for optimum activity.

The Effects of Triterpenoid Saponins from the Seeds of Momordica cochinchinensis on Adipocyte Differentiation and Mature Adipocyte Inflammation.

Obesity is a medical condition in which abnormal or excessive fat accumulates to an extent that is associated with various diseases. In our ongoing research to figure out natural products with anti-obesity effects, a phytochemical investigation of the EtOH extract of the seeds of Momordica cochinchinensis was carried out, which resulted in the isolation of two major triterpenoid saponins: gypsogenin 3-O-ß-d-galactopyranosyl(1→2)-[α-l-rhamnopyranosyl (1→3)]-ß-d-glucuronopyranoside (1) and quillaic acid 3-O-ß-d-galactopyranosyl(1→2)-[α-l-rhamnopyranosyl(1→3)]-ß-d-glucuronopyranoside (2). Then, the effects of the isolated triterpenoid saponins (1 and 2) on adipocyte differentiation were evaluated, and it was demonstrated that the isolated saponin (1) showed inhibitory effects on adipogenesis. In mature adipocytes, the isolated saponin (1) reversed tumor necrosis factor α (TNFα)-induced proinflammatory cytokine gene expression. Additionally, the isolated saponin (1) reduced lipolytic gene expression leading to decreased basal lipolysis activity. Collectively, these findings suggest that saponin (1) of M. cochinchinensis exerts beneficial effects in the regulation of adipogenesis and adipocyte inflammation and could be a potential therapeutic alternative in the treatment of obesity-induced metabolic diseases.

New cytotoxic constituents in the water-soluble fraction from Momordicae Semen.

Two new lignans mubezhisol (1) and mubezhisal (2), together with twenty six known compounds (3-28) were isolated from water-soluble fraction from the semens of Momordica cochinchinensis. In the subsequent action evaluation, four saponins (4, 6, 13, 27), six lignans (1, 2, 16, 17, 22, 23), and one naphthoquinone (24) exhibited the significant cytotoxicity. The results indicated that various saponins and lignans were mainly responsible for the antitumor activities of Momordicae Semen.

Cytotoxic and anti-inflammatory constituents from Momordica cochinchinensis seeds.

Five new lignans mubiesins A - E (1-5), together with twenty-seven known compounds (6-32), were isolated from the cytotoxicity and anti-inflammation portions of Momordica cochinchinensis seeds which were widely used for various tumors and inflammations. Their structures were elucidated by extensive spectroscopic analyses (HR-MS, UV, CD, IR, 1D-NMR, and 2D-NMR). Their cytotoxic and anti-inflammatory activities were evaluated in vitro. Various lignans and saponins showed the significant activities, they could obviously inhibit the growth of tumor cells and the release of NO and TNF-α in RAW 264.7 cells induced by LPS.

Behind the Myth of the Fruit of Heaven, a Critical Review on Gac (Momordica cochinchinensis Spreng.) Contribution to Nutrition.

Gac, Momordica cochinchinensis (Lour.) Spreng. belongs to the Cucurbitaceae family. It is more considered as a super fruit. The demand for this plant is growing in countries where its reputation is high, including traditional countries of gac culture and countries fond of super fruits and food supplements. In these latter countries, the industrial strategy aims at producing high added value in food supplements or nutritional rich preparations. However, when marketing is not the driving force and claims have to be related to scientific data, the situation of gac is less "heavenly", mainly because its most remarkable properties are in the field of micronutrients. These latter components are indeed very important for health but their supplementation on healthy populations brings no significant advantage. This paper proposes to review aspects important for the nutritional reputation of this plant: where it comes from, how it is cultured to have an optimal nutritional composition, what is its composition and how it can impact health of consumers, in which products it is used and what are the regulations to use it in different markets. One important goal of this review is to give a critical and scientific approach to confirm data on this fruit, which has been promoted by marketing departments injecting so many wrong and unverified information. Missing data will be highlighted and potential positive applications are proposed all along the text.

Phytochemistry, Pharmacological Activities, Toxicity and Clinical Application of Momordica cochinchinensis.

Momordica cochinchinensis (Lour.) Spreng (M. cochinchinensis) is a deciduous vine that grows in Southeast Asia. It is known as gac in Vietnam and as Red Melon in English. Gac is reputed to be extremely benificial for health and has been widely used as food and folk medicine in Southeast Asia. In China, the seed of M. cochinchinensis (Chinese name: Mu biezi) is used as traditional Chinese medicine (TCM) for the treatment of various diseases. More than 60 chemical constituents have been isolated from M. cochinchinensis. Modern pharmacological studies and clinical practice demonstrate that some chemical constituents of M. cochinchinensis possess wide pharmacological activities, such as anti-tumor, anti-oxidation, anti-inflammatory, etc. This paper reviews the phytochemistry, pharmacological activities, toxicity, and clinical application of M. cochinchinensis, aiming to bring new insights into further research and application of this ancient herb.

Antioxidant compounds and capacities of Gac (Momordica cochinchinensis Spreng) fruits

Objective: To identify and determine the composition of antioxidant compounds, and to evaluate the antioxidant abilities of Gac fruit parts (peel, pulp, seed and aril) grown in Malaysia.Methods: LC-MS/MS was used for identification of antioxidant compounds and UV-Vis for estimation of the contents of phenolics, flavonoids, and carotenoids. Lycopene and β-carotene were quantified using high-performance liquid chromatography. DPPH (2, 2-diphenyl-1-picrylhydrazyl) and ferric reducing antioxidant power assays were employed to evaluate antioxidant capacities.Results: Phytochemicals were found amongst all the fruit parts. Notably, significant amounts of carotenoids [(107.4 ± 4.5), (85.7 ± 4.4), (110.6 ± 2.1) mg/100 g dry weight (DW)], and relatively high levels of both phenolics [(27.3 ± 1.7), (28.9 ± 2.4), (30.8 ± 2.7) mg/100 g DW]and flavonoids [(38.1 ± 2.2), (8.8 ± 1.3), (24.5 ± 3.3) mg/100 g DW] were found in the fruit's peel, pulp and aril, respectively. Seed part also showed a relatively high level of flavonoids [(18.1 ± 2.3) mg/100 g DW]. Lycopene and β-carotene were found to be significantly high (P < 0.05)in aril [(579.3 ± 22.7) and (621.0 ± 35.0) μg/g DW], followed by peel [(51.0 ± 7.5) and (210.0 ± 12.5) μg/g DW] and pulp [(37.6 ± 10.9) and (205.6 ± 22.1) μg/g DW)]. Antioxidant assays revealed that aril possessed the highest scavenging activity (IC50 = 865 μg/mL), while the peel possessed the highest ferric reducing power of 140 μmol FeSO4/μg.Conclusions: The current results demonstrate that Gac fruit grown in Malaysia is a rich source of phytochemicals, especially carotenoids, and possesses antioxidant activities. Thus, such findings suggest Gac fruit as a source of an antioxidant plant.

Antioxidant compounds and capacities of Gac (Momordica cochinchinensis Spreng) fruits

Objective: To identify and determine the composition of antioxidant compounds, and to evaluate the antioxidant abilities of Gac fruit parts (peel, pulp, seed and aril) grown in Malaysia. Methods: LC-MS/MS was used for identification of antioxidant compounds and UV-Vis for estimation of the contents of phenolics, flavonoids, and carotenoids. Lycopene and β-carotene were quantified using high-performance liquid chromatography. DPPH (2, 2-diphenyl-1-picrylhydrazyl) and ferric reducing antioxidant power assays were employed to evaluate antioxidant capacities. Results: Phytochemicals were found amongst all the fruit parts. Notably, significant amounts of carotenoids [(107.4 ± 4.5), (85.7 ± 4.4), (110.6 ± 2.1) mg/100 g dry weight (DW)], and relatively high levels of both phenolics [(27.3 ± 1.7), (28.9 ± 2.4), (30.8 ± 2.7) mg/100 g DW] and flavonoids [(38.1 ± 2.2), (8.8 ± 1.3), (24.5 ± 3.3) mg/100 g DW] were found in the fruit's peel, pulp and aril, respectively. Seed part also showed a relatively high level of flavonoids [(18.1 ± 2.3) mg/100 g DW]. Lycopene and β-carotene were found to be significantly high (P < 0.05) in aril [(579.3 ± 22.7) and (621.0 ± 35.0) μg/g DW], followed by peel [(51.0 ± 7.5) and (210.0 ± 12.5) μg/g DW] and pulp [(37.6 ± 10.9) and (205.6 ± 22.1) μg/g DW)]. Antioxidant assays revealed that aril possessed the highest scavenging activity (IC

Bioactive Composition, Antioxidant Activity, and Anticancer Potential of Freeze-Dried Extracts from Defatted Gac (Momordica cochinchinensis Spreng) Seeds.

Background: Gac (Momordica cochinchinensis Spreng) seeds have long been used in traditional medicine as a remedy for numerous conditions due to a range of bioactive compounds. This study investigated the solvent extraction of compounds that could be responsible for antioxidant activity and anticancer potential. Methods: Defatted Gac seed kernel powder was extracted with different solvents: 100% water, 50% methanol:water, 70% ethanol:water, water saturated butanol, 100% methanol, and 100% ethanol. Trypsin inhibitors, saponins, phenolics, and antioxidant activity using the 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) diammonium salt (ABTS), the 2,2-diphenyl-1-picrylhydrazyl (DPPH) and the ferric reducing antioxidant power (FRAP) assays; and anticancer potential against two melanoma cancer cell lines (MM418C1 and D24) were analysed to determine the best extraction solvents. Results: Water was best for extracting trypsin inhibitors (581.4 ± 18.5 mg trypsin/mg) and reducing the viability of MM418C1 and D24 melanoma cells (75.5 ± 1.3 and 66.9 ± 2.2%, respectively); the anticancer potential against the MM418C1 cells was highly correlated with trypsin inhibitors (r = 0.92, p < 0.05), but there was no correlation between anticancer potential and antioxidant activity. The water saturated butanol had the highest saponins (71.8 ± 4.31 mg aescin equivalents/g), phenolic compounds (20.4 ± 0.86 mg gallic acid equivalents/g), and antioxidant activity, but these measures were not related to anticancer potential. Conclusions: Water yielded a Gac seed extract, rich in trypsin inhibitors, which had high anticancer potential against two melanoma cell lines.

Optimisation of the Microwave-Assisted Ethanol Extraction of Saponins from Gac (Momordica cochinchinensis Spreng.) Seeds.

BACKGROUND: Gac (Momordica cochinchinensis Spreng.) seeds contain saponins that are reportedly medicinal. It was hypothesised that the extraction of saponins from powdered Gac seed kernels could be optimised using microwave-assisted extraction (MAE) with ethanol as the extraction solvent. The aim was to determine an appropriate ethanol concentration, ratio of solvent to seed powder and microwave power and time for extraction. Whether or not defatting the Gac seed powder had an impact on the extraction of saponins, was also determined. RESULTS: A four-fold higher total saponin content (TSC) was obtained in extracts from full-fat Gac seed kernel powder than from defatted powder (100 vs. 26 mg aescin equivalents (AE) per gram of Gac seeds). The optimal parameters for the extraction of saponins were a ratio of 30 mL of 100% absolute ethanol per g of full-fat Gac seed kernel powder with the microwave set at 360 W for three irradiation cycles of 10 s power ON and 15 s power OFF per cycle. CONCLUSIONS: Gac seed saponins could be efficiently extracted using MAE. Full-fat powder of the seed kernels is recommended to be used for a better yield of saponins. The optimised MAE conditions are recommended for the extraction of enriched saponins from Gac seeds for potential application in the nutraceutical and pharmaceutical industries.

[Studies on liposoluble constituents from Momordicae Semen].

The liposoluble constituents in Momordicae Semen were investigated in the present study. By silica gel, Sephadex LH-20 column chromatography, and semi-preparative HPLC, 22 compounds were isolated and purified from dichloromethane and ethyl acetate fraction. Based on NMR and MS spectra analyses, these compounds were identified as lupeol (1), 5-(1'-hydroxypentyl)-5H-furan-2-one (2), palmitic acid (3), viscumamide (4), clavatustide C (5), laxanol (6), threo-1-(4-hydroxyphenyl)-2-{4-[2-formyl-(E)-vinyl]-2-methoxyphenoxyl}-propane-1, 3-diol (7), α-spinasterol-3-O-ß-D-glucoside (8), chushizisin F (9), ehletianol C (10), tanegool (11), (7R, 8R, 8'R)-4'-guaiacylglyceryl-evofolin B (12), ligballinone (13), (7R, 8S, 8'R)- 4, 4', 9-trihydroxy- 7, 9'-epoxy- 8, 8'-lignan (14), chushizisin I (15), chushizisin A (16), chushizisin G (17), p-coumaraldehyde (18), α-spinasterol (19), p-hydroxybenzoic acid (20), chushizisin E (21), and 3-[2-(4-hydroxyphenyl)-3-hydroxyphenyl-2, 3-dihydro-1-benzofuran-5-yl] propane-1-ol (22), respectively. Compounds 1-17 were isolated from Momordica cochinchinensis for the first time. Compound 2 was a new natural product while compounds 4 and 5 were first found in the terrestrial organism.

Gac fruit extracts ameliorate proliferation and modulate angiogenic markers of human retinal pigment epithelial cells under high glucose conditions

To investigate the impact of the extracts of Gac fruit parts (peel, pulp, seed, and aril) on the cell viability and angiogenesis markers of human retinal pigment epithelial (ARPE-19) cells under high glucose conditions.Methods: The effect of the extracts of Gac fruit peel, pulp, seed and aril on the ARPE-19 cells was determined using MTT viability assay, Trypan blue dye and morphological changes were observed using light microscopy. Enzyme-linked immunosorbent-based assay was performed to evaluate the effect of Gac fruit parts on the reactive oxygen species (ROS), vascular endothelial growth factor (VEGF) and pigmented epithelium-derived factor (PEDF) secretions.Results: High glucose (HG) at 30 mmol/L increased ARPE-19 cell viability and ROS and VEGF secretions. While, the exposure of ARPE-19 cells in high glucose condition to Gac fruit extracts led to inhibition of cell viability, induced morphological changes, decreased ROS and VEGF secretions, and increased PEDF level. Gac pulp, seed, and aril at 1000 μg/mL showed significant inhibition activities [(7.5 ± 5.1)％, (2.7 ± 0.5)％, (3.2 ± 1.1)％, respectively] against HG-induced ARPE-19 cell viability. The findings also demonstrated that Gac aril at 250 μg/mL significantly decreased ROS and VEGF levels [(40.6 ± 3.3) pg/mL, (107.4 ± 48.3) pg/mL, respectively] compared to ROS [(71.7 ± 2.9) pg/mL] and VEGF [(606.9 ± 81.1) pg/mL] in HG untreated cells. Moreover, 250 μg/mL of Gac peel dramatically increased PEDF level [(18.2 ± 0.3) ng/mL] compared to that in HG untreated cells [(0.48 ± 0.39) ng/mL].Conclusions: This study indicates that the extracts of Gac peel, pulp, seed and aril reduced cell viability, minimized ROS generations and showed angiogenic activities. Therefore, our findings open new insights into the potentiality of Gac fruit against HG-related diabetic retinopathy disease.

Studies on liposoluble constituents from Momordicae Semen / 中国中药杂志

The liposoluble constituents in Momordicae Semen were investigated in the present study. By silica gel, Sephadex LH-20 column chromatography, and semi-preparative HPLC, 22 compounds were isolated and purified from dichloromethane and ethyl acetate fraction. Based on NMR and MS spectra analyses, these compounds were identified as lupeol (1), 5-(1'-hydroxypentyl)-5H-furan-2-one (2), palmitic acid (3), viscumamide (4), clavatustide C (5), laxanol (6), threo-1-(4-hydroxyphenyl)-2-{4-[2-formyl-(E)-vinyl]-2-methoxyphenoxyl}-propane-1, 3-diol (7), α-spinasterol-3-O-β-D-glucoside (8), chushizisin F (9), ehletianol C (10), tanegool (11), (7R, 8R, 8'R)-4'-guaiacylglyceryl-evofolin B (12), ligballinone (13), (7R, 8S, 8'R)- 4, 4', 9-trihydroxy- 7, 9'-epoxy- 8, 8'-lignan (14), chushizisin I (15), chushizisin A (16), chushizisin G (17), p-coumaraldehyde (18), α-spinasterol (19), p-hydroxybenzoic acid (20), chushizisin E (21), and 3-[2-(4-hydroxyphenyl)-3-hydroxyphenyl-2, 3-dihydro-1-benzofuran-5-yl] propane-1-ol (22), respectively. Compounds 1-17 were isolated from Momordica cochinchinensis for the first time. Compound 2 was a new natural product while compounds 4 and 5 were first found in the terrestrial organism.