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Mitracarpus hirtus (L.) DC. is a weed plant commonly used for the treatment of eczema. The potential of the plant to treat cancer has not been emphasized, hence the need to explore its anticancer potential. M. hirtus was extracted and subjected to petition with solvents of increasing polarity. Its cytotoxic potential was evaluated against MCF-7, HepG2, and HeLa cells using the Neutral red assay and further verified through morphological assessment and DNA fragmentation assay. Crude chloroform fraction (CCF) displayed a cytotoxic effect on all the cell lines with low IC50 concentrations ranging from 11–17.87 µg/mL. Morphological assessment of MCF-7 exposed to CCF indicates apoptotic cell death and is further confirmed by its DNA fragmentation. Our data suggest that M. hirtus is a potential source for mining anticancer agents. [ABSTRACT FROM AUTHOR]

Objective: In this work, phytochemical screening, acute toxicity and antifungal evaluation on the methanol extracts of different parts (leaves, seed and aerial part) of Mitracarpus hirtus against Candida albicans, Candida tropicalis, Aspergillus fumigatus, Aspergillus niger, Histoplasm capsulatum, Mucor sp, Microsporum canis, Microsporum gallinae, Trichophyton mentagrophyte, and Trichophyton rubrum using agar well diffusion and broth dilution techniques is investigated. Material and Methods: The phytochemical screening of the methanol extracts of different parts of the plant revealed the presence of tannins saponins, flavonoids, alkaloids, steroids, and terpenoids and the median lethal dose (LD50) was estimated to be greater than 5000 mg/kg which indicates that the plant is non-toxic. Results: Susceptibility test for the methanol extracts showed mean zone of inhibition ranging from 19.33 0.58-23.33 0.56 mm against the test organisms while the standard drug, Fulcin had 24.33 0.58 - 31.67 0.58 mm. The minimum inhibitory concentration (MIC) of the extracts ranges between 0.25-0.50 mg/mL while the minimum fungicidal concentration (MFC) ranges between 0.25-1.00 mg/mL against some of the fungal pathogens. Conclusion: The findings of this study have revealed the antifungal efficacy of methanol extracts of the different part of M. hirtus which supports the ethno-medicinal claim of the use of the plant in the treatment of fungal infections. [ABSTRACT FROM AUTHOR]

A phytochemical investigation of the aerial parts of Mitracarpus hirtus afforded thirteen compounds, including a new naphthoquinone di-glycoside ( 1 ), three isopentenyl isoflavones ( 2 - 4 ), four flavonoids ( 5 - 8 ), three iridoid glycosides ( 9  -  11 ) and two coumarins ( 12 and 13 ). Their structures were elucidated based on extensive spectroscopic analyses, chemical methods, and the comparison with the literature. Among them, compound 1 possesses a 2-(3-methylnaphthalen-2-yl)acetic acid core with two glucosyl groups, compounds 2 - 4 are the first three representatives from the Rubiaceae family, and compounds 9 - 11 and 13 were isolated from Mitracarpus genus for the first time. Additionally, compounds 2 - 4 displayed potent antibacterial activities against Helicobacter pylori G27/HP159/JRES00015 (MIC = 4-16 μg/mL) , comparable to metronidazole. To date, wighteone ( 2 ) is the most active isoflavone with favourable predicted ADMET properties reported against H. pylori .

Hairy root cultures of Mitracarpus hirtus L. were obtained after transforming leaf-disc explants with wild strain Agrobacterium rhizogenes A13. The root cultures of M. hirtus showed high efficiency of shoot formation in both transformed and non-transformed cultures when illuminated with light. However, transformed hairy root proliferation was approximately 3.8-5 times higher than the control in both solidified and liquid plant growth regulator free media. Putatively transformed roots were identified by the presence of the rol gene via PCR. Integration of the rol gene into the plant genome was confirmed via Southern blot analysis after 5 months with no detection in non-transformed roots. In addition, the effect of 2-chloro-4-pyridyl- N-phenylurea (CPPU), a synthetic cytokinin, when applied as an elicitor for hairy root cultures of M. hirtus was investigated. The 24-day-old hairy root cultures of high root proliferation line R107-3, were incubated for 48 h in media supplemented with 0 or 5 mg l CPPU. The methanolic extracts of root tissues were subsequently analyzed for biochemical constituents using Gas Chromatography Mass Spectrometry (GC-MS). The alteration of plant secondary metabolites produced after CPPU treatment was analyzed. Compared to the control (with quality higher than 80 %), six unique compounds were found, five original compounds absent, 11 with increased, and five with decreased contents. Increased contents of two metabolites, chrysophanol and 2-methoxy-4-vinylphenol, showed pharmaceutical potential. CPPU was also found to elicit the alkaloid compound, Eseroline, 7-bromo-, methylcarbamate (ester), which could not be detected in the non-treated sample. The findings of this study demonstrate the establishment of transgenic hairy root of M. hirtus and the application of CPPU as an elicitor to induce variations in plant secondary metabolite that shows its potential to apply for bio-reactor system. [ABSTRACT FROM AUTHOR]

Tetraploid plants were successfully induced for the first time in Mitracarpus hirtus L., by overnight immersion of shoot meristems in 0.1 % colchicine solution, followed by in vitro culture leading to plant regeneration. Examination of ploidy level by flow cytometric analysis and counting chromosome number at metaphase confirmed that original diploid plant (WT1) contained chromosome number as 2n = 2x = 28, whereas 2n = 4x = 56 was observed in the tetraploids induced with colchicine treatment (CC102 and CC110). Thicker root formation, larger stomata (1.3-2 times), and lower density of stomata (1.7-4 times) were observed in these tetraploid plants. After transplantation to the pot, tetraploid plant (CC110) showed higher fresh weights of aerial part and leaves (1.5 and 1.4 times respectively) than diploid. However, the methanolic extracts from leaves of tetraploid line CC102 showed inhibition against human pathogenic bacterium, S. aureus while WT1 and CC110 showed no activity. GC-MS revealed 40 unique compounds present in CC102, but absent in WT1 and CC110. Through hierarchical clustering analysis the 40 unique compounds in CC102 formed a cluster group found to correlate with anti- S. aurens activity. These results suggested that tetraploid M. hirtus CC102 created in this study provides a novel source of compounds useful in fighting infectious disease. [ABSTRACT FROM AUTHOR]

• Different extracts from Mitracarpus hirtus were investigated. • Chemical profile was determined via advanced chromatographic techniques. • Phenolics, pyrrolizidine alkaloids and triterpene acid were present in the extract. • Dichloromethane and ethyl acetate extracts showed highest phenolics and flavonoids. • Mitracarpus hirtus exhibited moderate in vitro antidiabetic and anti-tyrosinase activities. Mitracarpus hirtus (L.) DC. (Family: Rubiaceae) is a tropical annual herb commonly found in America and Mexico. In the present study, the methanol, ethyl acetate, dichloromethane and aqueous extracts of the plant were tested for total phenolic (TPC) and flavonoid content (TFC) and antioxidant activities were evaluated using a battery of assays including 2,2-diphenyl-1-picrylhydrazyl (DPPH), 2,2-azino-bis (3-ethylbenzothiazoline-6-sulfonic acid) (ABTS), ferric reducing antioxidant power (FRAP), cupric reducing antioxidant capacity, total antioxidant capacity (TAC) (phosphomolybdenum) and metal chelating. Enzyme inhibitory effects were investigated using acetylcholinesterase (AChE), tyrosinase, α-amylase and α-glucosidase as target enzymes. The phytochemical profile was obtained using liquid chromatography-diode array detection-electrospray ionization-mass spectrometry (LC-DAD-ESI-MSn), liquid chromatography-atmospheric pressure chemical ionization-mass spectrometry (LC-APCI-MSn) and nuclear magnetic resonance (NMR) experiments. Results showed that the dichloromethane and ethyl acetate extracts yielded the highest TPC (29.10 ± 0.07 mg gallic acid equivalent/g) and TFC (38.14 ± 0.91 mg rutin equivalent/g), respectively. Aqueous extract showed weak activity against tested enzymes but demonstrated the strongest ABTS scavenging activity (59.39 ± 1.19 mg trolox equivalent/g) and is the strongest Fe3+ reducer (59.42 ± 0.59 mg trolox equivalent/g). Phytochemical analysis revealed the presence of phenolics, pyrrolizidine alkaloids and triterpene acid. This is the first report gathering scientific data on antioxidant, enzyme inhibitory activities and phytochemical composition of M. hirtus and the obtained results can be used as starting point for further investigation on this traditional medicinal herb. [ABSTRACT FROM AUTHOR]