Search Results (14)

Momordica charantia, commonly known as bitter melon, is a fruiting plant that has been used for several diseases including infectious diseases. In this study, we report the antibacterial, antifungal, and antiviral activity of different bitter melon fruit parts originating from India and Saudi Arabia. The in vitro experiments are supported by the molecular docking of karavilosides to verify their role in the bioactivity. The antimicrobial assays revealed activity against Candida albicans, Escherichia coli, and Staphylococcus aureus. The extracts exhibited the potent inhibition of HIV-I reverse transcriptase, with an IC50 of 0.125 mg/mL observed for the pith extract originating from Saudi Arabia and the standard drug doxorubicin. The molecular docking of karavilosides exhibited a significant affinity to reverse transcriptase comparable to Rilpivirine and higher than that of doxorubicin. These outcomes encourage the precious bioactive components of the seed and pith of the Saudi bitter melon fruits to be further studied for isolation and structure elucidation. Full article

Momordica charantia (MC; commonly known as bitter melon) was fermented with Leuconostoc mesenteroides MKJW, MKSR, and KCTC 3719 (LM), and Leuconosoc citreum KCTC 3526 (LC), and their anti-diabetic, anti-dementia, and antioxidant activities were evaluated. The fermentation was performed for 24 h at 30 °C, and non-fermented MCs (CON1 and CON2) were included for comparison. All fermented MCs produced lactic acids, mannitol, dextran, and oligosaccharides. The highest amount of mannitol (34.76 mg/mL) and lactic acids (10.42 mg/mL) were produced in MKSR-MC, and the highest amount of dextran (22.37%) was produced in MKJW-MC. MKSR-MC showed complete α-glucosidase inhibition (99.91%), but it did not show a significant change in α-amylase inhibition (24.43%) compared to non-fermented MC (20.14%) (p > 0.05). It was also high in acetylcholinesterase inhibition (55.24%) compared to other fermented MCs (31.21–44.46%). Fermentation increased butyrylcholinesterase inhibition, but no significant differences were observed among the groups. Therefore, our results indicated that MKSR-fermented MC might be used as a non-dairy probiotic plant extract to achieve multi-health functional activities such as anti-diabetic, anti-dementia, and antioxidant activities. Full article

Momordica charantia Linn. (Cucurbitaceae), the wild variety of bitter melon, and Morinda lucida Benth (Rubiaceae) were commonly used as a popular folk medicine in Benin. This study aimed to appreciate the ethnopharmacological knowledge and evaluate the antioxidant and anti-inflammatory effects of M. charantia and M. lucida leaves extracts. Semi-structured surveys supported by individual interviews were conducted with herbalists and traditional healers in southern Benin. The antioxidant activities were evaluated by a micro-dilution technique using ABTS and FRAP methods. These activities were supported by cyclic voltammetry analysis. The anti-inflammatory activity was evaluated by the albumin denaturation method. The volatile compounds were analysed by GC-MS analysis. All the respondents involved in this study have good knowledge of the two plants. We identify 21 diseases grouped into five categories of condition. The two plants’ extracts possess variable antioxidant capacity. Indeed, all the active extracts of M. charantia presented an IC₅₀ < 0.078 mg/mL, while the extracts of M. lucida had an IC₅₀ up to 0.21 ± 0.02 mg/mL. For anti-inflammatory activity, a dose-response activity (p < 0.001) was observed in the protein denaturation inhibition rate of the extracts. It should be noted that the highest inhibition rate (98.34 ± 0.12) of the albumin denaturation was observed with M. lucida dichloromethane extract. A total of 59 volatile compounds were identified by GC-MS analysis in the extracts of the two plants. The M. charantia ethyl acetate extract shows the presence of 30 different compounds with a relative abundance of 98.83%, while that of M. lucida shows 24 compounds with a relative abundance of 98.30%. These plants are potential candidates to discover new compounds with therapeutic properties that could be used to solve public health problems. Full article

T2DM is a complex metabolic disorder characterized by hyperglycemia and glucose intolerance. It is recognized as one of the most common metabolic disorders and its prevalence continues to raise major concerns in healthcare globally. Alzheimer’s disease (AD) is a gradual neurodegenerative brain disorder characterized by the chronic loss of cognitive and behavioral function. Recent research suggests a link between the two diseases. Considering the shared characteristics of both diseases, common therapeutic and preventive agents are effective. Certain bioactive compounds such as polyphenols, vitamins, and minerals found in vegetables and fruits can have antioxidant and anti-inflammatory effects that allow for preventative or potential treatment options for T2DM and AD. Recently, it has been estimated that up to one-third of patients with diabetes use some form of complementary and alternative medicine. Increasing evidence from cell or animal models suggests that bioactive compounds may have a direct effect on reducing hyperglycemia, amplifying insulin secretion, and blocking the formation of amyloid plaques. One plant that has received substantial recognition for its numerous bioactive properties is Momordica charantia (M. charantia), otherwise known as bitter melon, bitter gourd, karela, and balsam pear. M. charantia is utilized for its glucose-lowering effects and is often used as a treatment for diabetes and related metabolic conditions amongst the indigenous populations of Asia, South America, India, and East Africa. Several pre-clinical studies have documented the beneficial effects of M. charantia through various postulated mechanisms. Throughout this review, the underlying molecular mechanisms of the bioactive components of M. charantia will be highlighted. More studies will be necessary to establish the clinical efficacy of the bioactive compounds within M. charantia to effectively determine its pertinence in the treatment of metabolic disorders and neurodegenerative diseases, such as T2DM and AD. Full article

The bitter melon, Momordica charantia L., was once an important food and medicinal herb. Various studies have focused on the potential treatment of stomach disease with M. charantia and on its anti-diabetic properties. However, very little is known about the specific compounds responsible for its anti-inflammatory activities. In addition, the in vitro inhibitory effect of M. charantia on pro-inflammatory cytokine production by lipopolysaccharide (LPS)-stimulated bone marrow-derived dendritic cells (BMDCs) has not been reported. Phytochemical investigation of M. charantia fruit led to the isolation of 15 compounds (1−15). Their chemical structures were elucidated spectroscopically (one- and two-dimensional nuclear magnetic resonance) and with electrospray ionization mass spectrometry. The anti-inflammatory effects of the isolated compounds were evaluated by measuring the production of the pro-inflammatory cytokines interleukin IL-6, IL-12 p40, and tumor necrosis factor α (TNF-α) in LPS-stimulated BMDCs. The cucurbitanes were potent inhibitors of the cytokines TNF-α, IL-6, and IL-12 p40, indicating promising anti-inflammatory effects. Based on these studies and in silico simulations, we determined that the ligand likely docked in the receptors. These results suggest that cucurbitanes from M. charantia are potential candidates for treating inflammatory diseases. Full article

Head and neck cancer (HNC) is one of the most aggressive cancers, and treatments are quite challenging due to the difficulty in early diagnosis, lack of effective chemotherapeutic drugs, adverse side effects and therapy resistance. We identified momordicine-I (M-I), a bioactive secondary metabolite in bitter melon (Momordica charantia), by performing liquid chromatography-high resolution electrospray ionization mass spectrometry (LC-HRESIMS) analysis. M-I inhibited human HNC cell (JHU022, JHU029, Cal27) viability in a dose-dependent manner without an apparent toxic effect on normal oral keratinocytes. Mechanistic studies showed that M-I inhibited c-Met and its downstream signaling molecules c-Myc, survivin, and cyclin D1 through the inactivation of STAT3 in HNC cells. We further observed that M-I was non-toxic and stable in mouse (male C57Bl/6) blood, and a favorable pharmacokinetics profile was observed after IP administration. M-I treatment reduced HNC xenograft tumor growth in nude mice and inhibited c-Met and downstream signaling. Thus, M-I has potential therapeutic implications against HNC. Full article

Salt stress severely reduces growth and yield of plants. Considering the positive effects of selenium (Se) and chitosan (Cs) separately against abiotic stress, in these experiments, we synthesized chitosan–selenium nanoparticles (Cs–Se NPs) and investigated their ability to reduce the negative effects of salt stress on growth and some biochemical parameters of bitter melon (Momordica charantia). Bitter melon plants were grown at three NaCl salinity levels (0, 50, and 100 mM) and a foliar spray of Cs–Se NPs (0, 10, and 20 mg L⁻¹) was applied. Some key morphological, biochemical, and physiological parameters in leaf samples and essential oil from fruit were measured at harvest. Salinity decreased growth and yield while foliar application of Cs–Se NPs increased these critical parameters. Furthermore, Cs–Se NPs enhanced bitter melon tolerance to salinity by increasing antioxidant enzyme activity, proline concentration, relative water content, and K⁺, and decreasing MDA and H₂O₂ oxidants and Na aggregation in plant tissues. Yield was also improved, as the highest amount of essential oils was produced by plants treated with Cs–Se NPs. Generally, the greatest improvement in measured parameters under saline conditions was obtained by treating plants with 20 mg L⁻¹ Cs–Se NPs, which significantly increased salinity tolerance in bitter melon plants. Full article

Background: Momordica charantia Linn. (Cucurbitaceae), the wild variety of bitter melon and Morinda lucida Benth (Rubiaceae) were commonly used as a popular folk medicine in Benin. This research focused to measure the antioxidant and enzyme inhibitory effects of M. charantia and M. lucida leaves and their antidiabetic activity. Methods: Antioxidant activities were evaluated by micro-dilution technique using DPPH free radical scavenging activity and β-carotene-linoleate bleaching assay. The α-amylase inhibition assay was carried out utilizing the 3,5-dinitrosalicylic acid procedure, while β-glucosidase inhibition assay was demonstrated using as substrate p-nitrophenyl-β-D-glucopyranoside (PNPG). HPLC-DAD analysis was realized using a high-performance liquid chromatography systems with diode-array detector, L-3000. Results: Chlorogenic acid, epicatechin, daidzein, rutin, naringin, quercetin, naringenin and genistein were identified as polyphenol compounds in the both plants extract. Dichloromethane and ethyl acetate extracts showed a good α-amylase inhibitory activity (56.46 ± 1.96% and 58.76 ± 2.74% respectively). M. lucida methanolic extract has shown IC₅₀ of 0.51 ± 0.01 mg/mL, which is the lowest for DPPH scavenging activity. M. lucida dichloromethane extract showed the highest inhibitory capacity of β-glucosidase activity (82.11. ± 2.15%). Conclusion: These results justify some traditional medicinal uses of both plants. The purified fractions could be used in future formulations, possibly incorporated in functional foods to combat certain diseases. Full article

Glioblastoma multiforme (GBM) is a type of cancer which has the highest mortality rate among brain cancers (1–2). Momordica charantia, known as bitter melon, is a plant its pharmacological activities and nutritional properties. Due to contains bioactive compounds, M. charantia is used for cancer treatments, inflammation-related diseases and diabetes (3–4). In this study, it was aimed to investigate the effects of M. charantia extract on cell viability, cytotoxicity and migration capacity in U87G cell line. U87G was cultured in DMEM-high glucose containing FBS 10% (v/v) and penisillin-streptomicin 1% (v/v). Cells were incubated at 37 °C in a humidified 5% CO₂ incubator. The cytotoxic effect of M. charantia extract was determined by MTT analysis, cell viability by survival analysis and migration by wound-healing analysis. The results were evaluated by using ANOVA and GraphPad Prism7.0 program (GraphPad Software, La Jolla, CA, USA) in three replicates. IC₅₀ value of M. charantia extract was found 750 μg/mL which is statistically significant (* p < 0.05). The extract had an increasing lethal effect at the 16.6% (24 h), 42.6% (48 h), 79.3% (72 h) and 91.6% (96 h). According to the wound-healing analysis, the wound closed at 24 h in the control group and the wound gradually increased depending on time in the extract treated group. According to the results, M. charantia extract has a cytotoxic and a significant anti-proliferative effect on U87G. It might be used as therapeutic agent against to GBM. However, in order to understand the effect of M. charantia in living organisms, in vivo experiments must be determined. Full article

Alpha-momorcharin (α-MMC), a member of the ribosome-inactivating protein (RIP) family, has been found in the seeds of Momordica charantia (bitter melon). α-MMC contributes a number of pharmacological activities; however, its inflammatory properties have not been well studied. Here, we aim to determine the inflammatory responses induced by recombinant α-MMC and identify the underlying mechanisms using cell culture and animal models. Recombinant α-MMC was generated in Rosetta™(DE3)pLysS and purified by the way of nitrilotriacetic acid (NTA) chromatography. Treatment of recombinant α-MMC at 40 μg/mL exerted sub-lethal cytotoxic effect on THP-1 monocytic cells. Transcriptional profiling revealed that various genes coding for cytokines and other proinflammatory proteins were upregulated upon recombinant α-MMC treatment in THP-1 cells, including MCP-1, IL-8, IL-1β, and TNF-α. Recombinant α-MMC was shown to activate IKK/NF-κB and JNK pathways and the α-MMC-induced inflammatory gene expression could be blocked by IKKβ and JNK inhibitors. Furthermore, murine inflammatory models further demonstrated that α-MMC induced inflammatory responses in vivo. We conclude that α-MMC stimulates inflammatory responses in human monocytes by activating of IKK/NF-κB and JNK pathways, raising the possibility that consumption of α-MMC-containing food may lead to inflammatory-related diseases. Full article

Momordica charantia (M. charantia), commonly known as bitter gourd, bitter melon, kugua, balsam pear, or karela, is a tropical and sub-tropical vine belonging to the Cucurbitaceae family. It has been used to treat a variety of diseases in the traditional medicine of China, India, and Sri Lanka. Here, we review the anti-obesity effects of various bioactive components of M. charantia established at the cellular and organismal level. We aim to provide links between various bioactive components of M. charantia and their anti-obesity mechanism. An advanced search was conducted on the worldwide accepted scientific databases via electronic search (Google Scholar, Web of Science, ScienceDirect, ACS Publications, PubMed, Wiley Online Library, SciFinder, CNKI) database with the query TS = “Momordica charantia” and “obesity”. Information was also obtained from International Plant Names Index, Chinese Pharmacopoeia, Chinese herbal classic books, online databases, PhD and MSc dissertations, etc. First, studies showing the anti-obesity effects of M. charantia on the cells and on animals were classified. The major bioactive components that showed anti-obesity activities included proteins, triterpenoids, saponins, phenolics, and conjugated linolenic acids. Their mechanisms included inhibition of fat synthesis, promotion of glucose utilization, and stimulation of auxiliary lipid-lowering activity. Finally, we summarized the risks of excessive consumption of M. charantia and the application. Although further research is necessary to explore various issues, this review establishes the therapeutic potential of M. charantia and it is highly promising candidate for the development of anti-obesity health products and medicines. Full article

Wild bitter melon (Momordica charantia L. var. Abbreviata Ser.) is a wild edible variety of M. charantia, often used in folk medicine. In this study, the biological activities of its extract and fractions were investigated in vitro. It was found that ethyl acetate (EA) fraction exhibited high 1,1-diphenyl-2-picryl-hydrazyl (DPPH) scavenging activity with a half maximal inhibitory concentration (IC₅₀) value of 0.43 ± 0.04 mg/mL, while the chloroform (CF), EA, and n-butanol (Bu) fractions had strong 2,2-azinobis-3-ethyl benzothiazoline-6-sulfonic acid (ABTS)⁺ scavenging ability with IC₅₀ values of 0.36 ± 0.04 mg/mL, 0.35 ± 0.02 mg/mL, and 0.35 ± 0.05 mg/mL, respectively. Moreover, the EA and Bu fractions exhibited the highest protective effect against H₂O₂-induced DNA damage in a concentration-dependent manner. Furthermore, the EA fraction was effective in the inhibition of enzyme α-amylase activity with an IC₅₀ value of 0.27 ± 0.029 mg/mL. Finally, it was observed that the production of nitric oxide (NO), a pro-inflammatory mediator, was significantly reduced from LPS-stimulated murine macrophage RAW 264.7 cells by the ethanol extract (ET) and the EA fraction. Therefore, wild bitter melon could be considered as a promising biomaterial for the development of pharmaceutical products. Full article

Porphyromonas gingivalis has been identified as one of the major periodontal pathogens. Activity-directed fractionation and purification processes were employed to identify the anti-inflammatory active compounds using heat-killed P. gingivalis-stimulated human monocytic THP-1 cells in vitro. Five major fractions were collected from the ethanol/ethyl acetate extract of wild bitter melon (Momordica charantia Linn. var. abbreviata Ser.) leaves and evaluated for their anti-inflammatory activity against P. gingivalis. Among the test fractions, Fraction 5 effectively decreased heat-killed P. gingivalis-induced interleukin (IL)-8 and was subjected to separation and purification by using chromatographic techniques. Two cucurbitane triterpenoids were isolated from the active fraction and identified as 5β,19-epoxycucurbita-6,23-diene-3β,19,25-triol (1) and 3β,7β,25-trihydroxycucurbita-5,23-dien-19-al (2) by comparing spectral data. Treatments of both compounds in vitro potently suppressed P. gingivalis-induced IL-8, IL-6, and IL-1β levels and the activation of mitogen-activated protein kinase (MAPK) in THP-1 cells. Both compounds effectively inhibited the mRNA levels of IL-6, tumor necrosis factor (TNF)-α, and cyclooxygenase (COX)-2 in P. gingivalis-stimulated gingival tissue of mice. These findings imply that 5β,19-epoxycucurbita-6,23-diene-3β,19,25-triol and 3β,7β,25-trihydroxycucurbita-5,23-dien-19-al could be used for the development of novel therapeutic approaches against P. gingivalis infections. Full article

Bitter melon (Momordica charantia L.) is a tropical fruit claimed to have medicinal properties associated with its content of phenolic compounds (TPC). The aim of the study was to compare water with several organic solvents (acetone, butanol, methanol and 80% ethanol) for its efficiency at extracting the TPC from freeze-dried bitter melon powder. The TPC of the extracts was measured using the Folin-Ciocalteu reagent and their antioxidant capacity (AC) was evaluated using three assays. Before optimisation, the TPC and AC of the aqueous extract were 63% and 20% lower, respectively, than for the best organic solvent, 80% ethanol. However, after optimising for temperature (80 °C), time (5 min), water-to-powder ratio (40:1 mL/g), particle size (1 mm) and the number of extractions of the same sample (1×), the TPC and the AC of the aqueous extract were equal or higher than for 80% ethanol. Furthermore, less solvent (40 mL water/g) and less time (5 min) were needed than was used for the 80% ethanol extract (100 mL/g for 1 h). Therefore, this study provides evidence to recommend the use of water as the solvent of choice for the extraction of the phenolic compounds and their associated antioxidant activities from bitter melon. Full article