Anti-inflammatory steroids from the stems of Solanum nigrum L.

Sixteen previously undescribed steroidal sapogenins along with two known ones were isolated from the stems of Solanum nigrum L. (Solanaceae). Their structures were identified using a combination of 1D and 2D NMR, HR-ESI-MS spectroscopy, the Mosher method, and X-ray diffraction analysis. Compounds 1-8 have an unusual F ring and 9-12 have a derived A ring, both of which are rare skeletons found in natural products. The biological evaluation showed that the isolated steroids exhibited inhibition of nitric oxide in the LPS-induced RAW 264.7 macrophages with IC50 values from 7.4 to 41.3 µM. Further studies revealed that compounds 6 and 10 exhibited anti-inflammatory activity by blocking the nuclear translocation of NF-κB, and down-regulating the expression of iNOS, COX-2, IL-1ß, and IL-6 in a concentration-dependent manner. These results suggest that the stems of S. nigrum may serve as a source of anti-inflammatory agents for use in healthy or medicinal products.

Analysis of steroidal glycoalkaloids and their metabolites in Solanum nigrum fruits based on liquid chromatography-tandem mass spectrometry and molecular networking.

Solanum nigrum fruit is like a treasure house for anticancer drugs because of its steroidal alkaloids. However, the clinical treatment of cancer mainly uses immature fruits, which can cause a toxic reaction if eaten directly, while mature fruits are eaten as fruit. In order to clarify the reasons for the differences in pharmacodynamics and toxicity between them, we studied the composition and metabolism of steroidal alkaloids in fruits of different maturities based on liquid chromatography-tandem mass spectrometry and molecular networking. As a result, 114 steroidal glycoalkaloids were identified. During fruit ripening, the aglycones of steroidal alkaloids mainly undergo hydroxylation and carboxylation, and the sugar side chains mainly undergo acylation and glycosylation reactions. Furthermore, 219 steroidal alkaloids were identified in a metabolism experiment in rats. Metabolic processes include deglycosylation, redox, sulfuric acid binding, acetyl binding, and glucuronic acid-binding. Steroidal alkaloids in mature fruits have high molecular weight and polarity, which are difficult to absorb, and most of them are excreted through feces and urine, which may be the reason for their poor efficacy. This study lays a foundation for research on the biosynthesis of steroidal alkaloids and provides potential candidates for the discovery of new steroidal alkaloid anticancer drugs.

[Two new steroidal alkaloids from ripe berries of Solanum nigrum].

Two previously undescribed steroidal alkaloids, compounds 1-2, along with two known ones(3-4), were isolated from the 80% ethanol extract of ripe berries of Solanum nigrum by chromatographic methods, including silica gel, ODS, and HPLC. Based on spectroscopic and chemical evidence, including IR, NMR, and HR-ESI-MS data, the structures of the isolated compounds were identified as 12ß,27-dihydroxy solasodine-3-O-ß-D-glucopyranoside(1), 27-hydroxy solasodine-3-O-ß-D-glucopyranosyl-(1→4)-α-L-rhamnopyranosyl-(1→2)-[α-L-rhamnopyranosyl-(1→4)]-ß-D-glucopyranoside(2), solalyraine A(3), and 12ß,27-dihydroxy solasodine(4). Compounds 1-2 were tested for their potential effects against the proliferation of A549 cells, which revealed that compounds 1-2 had weak cytotoxic activity.

Steroidal alkaloids from Solanum nigrum and their cytotoxic activities.

Eight undescribed, along with five known steroidal alkaloids were isolated from Solanum nigrum L., a plant used in traditional Chinese medicine. Their structures were elucidated by NMR, HR-ESI-MS, and IR spectroscopy. Two compounds displayed an unusual structure in steroidal alkaloids with an open E-ring and without an F-ring present. To evaluate their bioactivities, nine compounds were selected to intervene five human cancer cell lines including H1299, HepG2, HeLa, HCT116, and MCF7 respectively. All compounds exhibited inhibitory effects for the five cell lines, revealing potential anti-tumor activities from Solanum nigrum.

Aqueous extract of Solanum nigrum attenuates Angiotensin-II induced cardiac hypertrophy and improves cardiac function by repressing protein kinase C-ζ to restore HSF2 deSUMOlyation and Mel-18-IGF-IIR signaling suppression.

ETHNOPHARMACOLOGICAL RELEVANCE: Solanum nigrum, commonly known as Makoi or black shade has been traditionally used in Asian countries and other regions of world to treat liver disorders, diarrhoea, inflammatory conditions, chronic skin ailments (psoriasis and ringworm), fever, hydrophobia, painful periods, eye diseases, etc. It has been observed that S. nigrum contains substances, like steroidal saponins, total alkaloid, steroid alkaloid, and glycoprotein, which show anti-tumor activity. However; there is no scientific evidence of the efficacy of S. nigrum in the treatment of cardiac hypertrophy. AIM: To investigate the ability of S. nigrum to attenuate Angiotensin II - induced cardiac hypertrophy and improve cardiac function through the suppression of protein kinase PKC-ζ and Mel-18-IGF-IIR signaling leading to the restoration of HSF2 desumolyation. MATERIALS AND METHODS: Cardiomyoblast cells (H9c2) were challenged with 100 nM Angiotensin-II (AngII) for 24 h and were then treated with different concentration of S.nigrum or Calphostin C for 24 h. The hypertrophic effect in cardiomyoblast cells were determined by immunofluorescence staining and the modulations in hypertrophic protein marker along with Protein Kinase C-ζ, MEL18, HSF2, and Insulin like growth factor II (IGFIIR), markers were analyzed by western blotting. In vivo experiments were performed using 12 week old male Wistar Kyoto rats (WKY) and Spontaneously hypertensive rats (SHR) separated into five groups. [1]Control WKY, [2] WKY -100 mg/kg of S.nigrum treatment, [3] SHR, [4] SHR-100 mg/kg of S.nigrum treatment, [5] SHR-300 mg/kg of S.nigrum treatment. S. nigrum was administered intraperitoneally for 8 week time interval. RESULTS: Western blotting results indicate that S. nigrum significantly attenuates AngII induced cardiac hypertrophy. Furthermore, actin staining confirmed the ability of S. nigrum to ameliorate AngII induced cardiac hypertrophy. Moreover, S. nigrum administration suppressed the hypertrophic signaling mediators like Protein Kinase C-ζ, Mel-18, and IGFIIR in a dose-dependent manner and HSF2 activation (restore deSUMOlyation) that leads to downregulation of IGF-IIR expression. Additionally in vivo experiments demonstrate the reduced heart sizes of S. nigrum treated SHRs rats when compared to control WKY rats. CONCLUSION: Collectively, the data reveals the cardioprotective effect of S. nigrum inhibiting PKC-ζ with alleviated IGF IIR level in the heart that profoundly remits cardiac hypertrophy for hypertension-induced heart failure.

Solanum nigrum Line inhibits osteoclast differentiation and suppresses bone mineral density reduction in the ovariectomy­induced osteoporosis model.

Bone homeostasis is maintained by osteoclasts that absorb bone and osteoblasts that form bone tissue. Menopausal osteoporosis is a disease associated with aging and hormonal changes due to menopause causing abnormal activation of osteoclasts, resulting in a decrease in bone density. Existing treatments for osteoporosis have been reported to have serious side effects, such as jawbone necrosis and breast and uterine cancer; therefore, their use by patients is decreasing, whilst studies focusing on alternative treatments are increasingly popular. Solanum nigrum Line (SL) has been used as a medicinal plant that possesses several pharmacological effects, such as anti­inflammatory and hepatotoxic protective effects. To the best of our knowledge, however, its effects on osteoporosis and osteoclasts have not been demonstrated previously. In the present study, the anti­osteoporotic effect of SL was investigated using a postmenopausal model of osteoporosis in which Sprague­Dawley rat ovaries were extracted. In addition, the inhibitory effects on osteoclast differentiation and function of SL was confirmed using an osteoclast model treated with receptor activator of NF­κB ligand (RANKL) on murine RAW 264.7 macrophages. In vivo experiments showed that SL reduced the decrease in bone mineral density and improved changes in the morphological index of bone microstructure, such as trabecular number and separation. In addition, the number of tartrate resistant acid phosphatase­positive cells in the femur and the expression levels of nuclear factor of activated T­cells cytoplasmic 1 (NFATc1) and cathepsin K protein were inhibited. In vitro, SL suppressed RANKL­induced osteoclast differentiation and bone resorption ability; this was mediated by NFATc1/c­Fos, a key transcription factor involved in osteoclast differentiation, ultimately inhibiting expression of various osteoclast­associated genes. These experimental results show that SL may be an alternative treatment for osteoporosis caused by abnormal activation of osteoclasts in the future.

A network pharmacology perspective for deciphering potential mechanisms of action of Solanum nigrum L. in bladder cancer.

BACKGROUND: Solanum nigrum L. decoction has been used as a folklore medicine in China to prevent the postoperative recurrence of bladder cancer (BC). However, there are no previous pharmacological studies on the protective mechanisms of this activity of the plant. Thus, this study aimed to perform a systematic analysis and to predict the potential action mechanisms underlying S. nigrum activity in BC based on network pharmacology. METHODS: Based on network pharmacology, the active ingredients of S. nigrum and the corresponding targets were identified using the Traditional Chinese Medicines for Systems Pharmacology Database and Analysis Platform database, and BC-related genes were screened using GeneCards and the Online Mendelian Inheritance in Man database. In addition, ingredient-target (I-T) and protein-protein interaction (PPI) networks were constructed using STRING and Cytoscape, Gene Ontology (GO) terms and Kyoto Encyclopedia of Genes and Genomes (KEGG) pathway enrichment analyses were conducted, and then the pathways directly related to BC were integrated manually to reveal the pharmacological mechanism underlying S. nigrum-medicated therapeutic effects in BC. RESULTS: Seven active herbal ingredients from 39 components of S. nigrum were identified, which shared 77 common target genes related to BC. I-T network analysis revealed that quercetin was associated with all targets and that NCOA2 was targeted by four ingredients. Besides, interleukin 6 had the highest degree value in the PPI network, indicating a hub role. A subsequent gene enrichment analysis yielded 86 significant GO terms and 89 significant pathways, implying that S. nigrum had therapeutic benefits in BC through multi-pathway effects, including the HIF-1, TNF, P53, MAPK, PI3K/Akt, apoptosis and bladder cancer pathway. CONCLUSIONS: S. nigrum may mediate pharmacological effects in BC through multi-target and various signaling pathways. Further validation is required experimentally. Network pharmacology approach provides a predicative novel strategy to reveal the holistic mechanism of action of herbs.

The Cytotoxic, Apoptotic Induction, and Cell Cycle Arrest Activities of Solanum nigrum L. Ethanolic Extract on MCF-7 Human Breast Cancer Cell.

OBJECTIVE: The purpose of this research was to evaluate the cytotoxic, cell cycle arrest, and apoptotic induction activities of the fruit of S. nigrum L. ethanolic-70% extract against MCF-7 human breast cancer cell. METHODS: S. nigrum L. ripe fruit was blended and macerated with ethanol 70% and the filtrate was evaporated. The semisolid extract was then analyzed phytochemically. Cytotoxic analysis was performed using MCF-7 cancer and Vero normal cell by MTT method and followed by apoptotic and cell cycle arrest analysis using flow cytometry. RESULTS: The phytochemical analysis resulted that extract contained total phenolic and flavonoid compounds with the level of 1.545±0.080% and 0.212±0.002%, respectively. Glycitin was the highest level of isoflavone compound, namely, 375.0844 mg/100 g extract. The cytotoxic evaluation revealed that the extract exhibited a selectively toxic effect between cancer and normal cell. The extract inhibited MCF-7 proliferation with IC50 value about 40.77±4.86 µg/mL and conversely toward Vero cell at lower cytotoxic activity with an IC50 value of 298.96±27.28 µg/mL. Evaluation of MCF-7 cell cycles demonstrated that the extract arrested the cell cycle in the S phase and continued to the G2/M phase at the half of the IC50 value. The extract induced apoptotic of MCF-7 cell about 43.31% in which this activity was nearly the same with doxorubicin as a positive control (59.14%). However, solamargine was predicted as the most active anticancer compounds by a molecular docking study so that it was suggested to measure the level of this compound. CONCLUSION: It can be concluded that the fruit of S. nigrum L. ethanolic-70% extract demonstrated cytotoxic activity toward MCF-7 breast cancer cell and nontoxic on Vero normal cell. Solamargine was predicted as the most active anticancer compound. This extract had an opportunity to be developed as a potential anticancer agent to overcome breast cancer diseases.

Immunomodulatory effects of a polysaccharide from Solanum nigrum Linne through TLR4-MyD88 signaling pathway.

Solanum nigrum Linne polysaccharide (SNLP), an active ingredient from Solanum nigrum Linne, has been proposed to inhibit tumor growth and display immunomodulatory activity. However, the molecular mechanism related to immune regulation remains unclear. In the present study, a homogeneous polysaccharide (SNLP-1) was extracted, the immune effects and the underlying molecular mechanisms were investigated. The immunomodulatory activity assay in vitro showed that SNLP-1 promoted the release of NO and TNF-α and IL-6 secretion in macrophages. In tumor-bearing mice, SNLP-1 could improve immune function including increasing the spleen index, thymus index and inducing Th1 responses mediated by IL-2, IFN-γ, and TNF, as well as decreasing the tumor weight. Furthermore, SNLP-1 elevated the expression of the critical nodes in the TLR4-Myd88 signaling pathways in vitro and in vivo. These results indicated that TLR4-MyD88 signal pathway may be one of the signal pathways of immune regulation of SNLP-1.

Solanum nigrum Linne improves DNCB­induced atopic dermatitis­like skin disease in BALB/c mice.

The present study aimed to investigate the effects of Solanum nigrum Linne (SNL) in a model of 1­chloro­2,4­dinitrobenzene (DNCB)­induced atopic dermatitis (AD) and in TNF­α/IFN­Î³­stimulated HaCaT cells. AD is a chronic inflammatory skin disease and is characterized by erythema, edema, increased pruritus and eczema. Steroids are most commonly used for anti­inflammatory therapy; however, their long­term use is limited due to side­effects, such as osteoporosis, brittle skin, muscle weaknesses and diabetes. Therefore, patients with AD require alternative treatment strategies. In previous studies, SNL has been reported to be effective against oxidants and cancer. However, to the best of our knowledge, the effects of SNL on AD have not yet been investigated. The present study examined the effects of SNL ethanol extract on a model of DNCB induced AD and on TNF­α/IFN­Î³­stimulated HaCaT cells. The skin tissue was sectioned to measure the thicknesses of the epidermis and dermis, as well as the numbers of eosinophils, mast cells and CD8 infiltration by H&E, toluidine blue, Masson's trichrome and IHC staining. ELISA was performed using serum to measure IgE levels. The present study also examined the expression of various inflammatory cytokines, MAPK and NF­κB in TNF­α/IFN­Î³­stimulated HaCaT cells. SNL significantly reduced the levels of cytokines released from HaCaT cells stimulated with TNF­α/IFN­Î³. SNL also significantly reduced the levels of p­p38 at 30 min and significantly reduced the activation of NF­κB in a time course experiment. In addition, SNL significantly reduced the level of serum IgE and dermal thickness and the infiltration of mast cells and CD8 in the BALB/c mouse model of DNCB­induced AD. The results of the current study suggest that SNL exerts a suppressive effect on pro­inflammatory cytokines in vitro and in vivo through the regulation of the immune system.

Antiulcerogenic effects of selected African nightshades (Solanum nigrum Linn. ) genotypes on the rat stomach: a morphologic and morphometric study / Efectos antiulcerogénicos de genotipos seleccionados de solanáceas Africanas (Solanum nigrum Linn. m) en el estómago de ratas: un estudio morfológico y morfométrico

Solanum nigrum (SLN), commonly known as African nightshade, is used as a vegetable as well as in the management and treatment of various ailments including gastric ulcers. We analyzed, both grossly and microscopically using H&E, Masson's trichrome and PSA staining methods, the protective effects of aqueous leaf extracts of three Kenyan SLN genotypes namely S. scabrum (SSB), S. sarrachoides (SSR) and S. villosum (SVL) on ethanol-induced gastric lesions in rats. There was evidence of gastro-protection by all the three genotypes with the SSB showing the highest ulcer inhibition score (76.37 %) followed by SSR (72.51 %) and SVL (63.30 %). SLN-pretreated rats showed less areas of gastric mucosal surface erosion. Additionally in the pretreated animals, the depth of the ulcers were markedly reduced, reaching only the gastric pit region except in those treated with SVL where the ulcers penetrated slightly more deeply to affect the gastric glands. Compared with controls, the mean microscopic ulcer index decreased 5.07, 3.55 and 2.37-fold in rats pretreated with SSB, SSR and SVL extracts respectively. Results of this work show extracts of the three SLN genotypes to have antiulcerogenic potential but at varied strengths, thus confirming earlier reports that phytoconstituents and hence the efficacy of a medicinal plant may be influenced by genetic factors.

Solanum nigrum (SLN), comúnmente conocida como la solanácea africana, se usa como vegetal, para el tratamiento de diversas dolencias incluyendo las úlceras gástricas. Analizamos de forma macro y microscópica, de forma macroscópica y microscópica, utilizando para ello tinciones de H&E, tricrómico de Masson y PSA los efectos protectores de extractos acuosos de hojas de tres genotipos SLN de Kenia: S. scabrum (SSB), S. sarrachoides (SSR) and S. villosum (SVL) en lesiones gástricas inducidas por etanol en ratas. Hubo evidencia de gastroprotección por parte de los tres genotipos con el SSB mostrando el puntaje más alto de inhibición de la úlcera (76,37 %) seguido de SSR (72,51 %) y SVL (63,30 %). Las ratas tratadas previamente con SLN mostraron menos áreas de erosión de la superficie de la mucosa gástrica. Además, en los animales pretratados, la profundidad de las úlceras se redujo notablemente, llegando solo a la región del fondo gástrico, excepto en aquellos tratados con SVL donde las úlceras penetraron un poco más profundamente para afectar las glándulas gástricas. En comparación con los controles, el índice medio de úlcera microscópica disminuyó 5,07, 3,55 y 2,37 veces en ratas pretratadas con extractos de SSB, SSR y SVL, respectivamente. Los resultados de este trabajo muestran que los extractos de los tres genotipos de SLN tienen potencial antiulcerogénico en diferentes concentraciones, lo que confirma informes anteriores que los fitoconstituyentes y la eficacia de una planta medicinal pueden estar influenciados por factores genéticos.

[Study on molecular mechanism of Solanum nigrum in treatment of hepatocarcinoma based on network pharmacology and molecular docking].

This study aimed to explore the main active ingredients and potential targets of Solanum nigrum(SN), so as to reveal the potential molecular mechanism of SN in the treatment of hepatocellular carcinoma(HCC) based on network pharmacology and molecular docking. First,the main active ingredients and predictive targets of SN were collected in the traditional Chinese medicine systems pharmacology database and analysis platform(TCMSP). Then,the targets relating to HCC were collected through retrieval of integrated bio-pharmacological network database for traditional Korean medicine(PharmDB-K), oncogenomic database of hepatocellular carcinoma(OncoDB.hcc). The common targets of disease-drug component were selected through intersection between predictive targets and disease targets. Next, based on the String platform, protein-protein interaction network(PPI) model of the potential anti-HCC targets was constructed using the software Cytoscape 3.7.1. ClueGO and CluePedia APP in Cytoscape were used to analyze the gene function of SN in the treatment of HCC, and construct the main active ingredients-potential targets-signal pathways topology network of SN. Finally,DISCOVERY STUDIO software was applied in verifying the molecular docking between the key active ingredient and potential protein target. The results showed that there were 4 main active ingredients of SN, involving 22 potential targets relating to HCC and 7 signal pathways relating to potential anti-HCC targets of SN. Network analysis showed that SN may play a therapeutic role in HCC by acting on key targets, such as EGFR, TP53, MYC, CCND1 and CTNNB1. Molecular docking results showed that quercetin and EGFR could bind stably and interact through amino acid residues LEU718, LYS745 and GLN791. This study revealed the potential active ingredients and the possible molecular mechanism of SN for treatment of HCC, providing scientific basis for follow-up exploration of the molecular mechanism of SN against HCC.

Purification and antioxidant capacity analysis of anthocyanin glucoside cinnamic ester isomers from Solanum nigrum fruits.

In a recent study, anthocyanins, which have a strong free radical-scavenging activity, were examined for their potential to effectively prevent cancer. However, clinical trials are limited by the purity of the anthocyanin. Multiple methods are used to extract and purify anthocyanins. Based on previous work on Solanum nigrum, which is a widely distributed plant, in this study, DM130 macroporous resin, Sephadex LH20, and a C18 column were used to separate cis-trans anthocyanin isomers. These anthocyanins constitute the majority of total S. nigrum anthocyanins. The results showed that this "DM130-LH20-C18 system" can be used to obtain a cinnamic acid-derived cis-trans anthocyanin, petunidin-3-(p-coumaroyl)-rutinoside-5-glucoside, with a purity of 98.5%, for effective quantitation. In order to determine the antioxidant ability of the petunidin-3-(p-coumaroyl)-rutinoside-5-glucoside cis-trans isomers, three ordinary methods were adopted. The maximum antioxidant ability of the cis-trans anthocyanin was dozens of times higher than that of vitamin C.

Accumulation of Anthocyanins through Overexpression of AtPAP1 in Solanum nigrum Lin. (Black Nightshade).

Black nightshade (Solanum nigrum) belongs to the Solanaceae family and is used as a medicinal herb with health benefits. It has been reported that the black nightshade plant contains various phytochemicals that are associated with antitumor activities. Here we employed a genetic approach to study the effects of overexpression of Arabidopsis thaliana production of anthocyanin pigment 1 (AtPAP1) in black nightshade. Ectopic expression of AtPAP1 resulted in enhanced accumulation of anthocyanin pigments in vegetative and reproductive tissues of the transgenic plants. Analysis of anthocyanin revealed that delphinidin 3-O-rutinoside-5-O-glucoside, delphinidin 3,5-O-diglucoside, delphinidin 3-O-rutinoside, petunidin 3-O-rutinoside (cis-p-coumaroyl)-5-O-glucoside, petunidin 3-(feruloyl)-rutinoside-5-glucoside, and malvidin 3-(feruloyl)-rutinoside-5-glucoside are highly induced in the leaves of AtPAP1 overexpression lines. Furthermore, ectopic expression of AtPAP1 evoked expression of early and late biosynthetic genes of the general phenylpropanoid and flavonoid pathways that include phenylalanine ammonia-lyase (PAL), cinnamate-4-hydroxylase (C4H), 4-coumarate CoA ligase (4CL), chalcone isomerase (CHI), and quinate hydroxycinnamoyl transferase (HCT), which suggests these genes might be transcriptional targets of AtPAP1 in black nightshade. Concomitantly, the total content of anthocyanin in the transgenic black nightshade plants was higher compared to the control plants, which supports phenotypic changes in color. Our data demonstrate that a major anthocyanin biosynthetic regulator, AtPAP1, can induce accumulation of anthocyanins in the heterologous system of black nightshade through the conserved flavonoid biosynthesis pathway in plants.

Solanum nigrum polyphenols reduce body weight and body fat by affecting adipocyte and lipid metabolism.

Obesity, being overweight and deposition of body fat are critically associated with metabolic disorders. The number of adipocytes and their lipid content, and the molecules involved in lipid metabolism are involved in obesity comorbidity. The food, Solanum nigrum L. (SN), has medical benefits in many aspects. In our recent report, SN was shown to reduce hepatic fat accumulation and oxidative stress, thus attenuating liver damage. However, it has not yet been explored whether SN is effective for weight loss and body fat reduction. Hence, we aimed to investigate if SN water extract (SWE) and the derived polyphenols (SNPE) are able to prevent obesity. Mice fed a high fat diet (HFD) and 3T3L1 cells model were used. The in vivo experiments showed SWE decreased serum triacylglyceride, cholesterol, and low-density lipoprotein (LDL)-cholesterol induced by a HFD. SWE promoted hepatic lipolysis by increasing PPARα and CPT-1, and inhibited lipogenesis by decreasing FaS and HMG-CoR. The expression of AMPK was enhanced, but sterol regulatory element binding proteins (SREBPs) were reduced by SWE, especially at 5%. In vitro analysis revealed that SNPE decreased the amount and lipid content of adipocytes. SNPE, especially at 0.5 mg mL-1, promoted lipolysis while inhibiting lipogenesis. In comparison with the doses applied in vivo and in vitro, the effect of SN could be attributed to the composition of the polyphenols. The results showed that SNPE is suggested to be an anti-obesity agent that is able to reduce body weight and body fat, by decreasing the amount and lipid content of adipocytes, and regulating lipid metabolism.

Antimicrobial and catalytic activities of biosynthesized gold, silver and palladium nanoparticles from Solanum nigurum leaves.

The field of nanobiotechnology and nanomedicine paves way for the use of several nanoparticles. Especially, in biomedical applications, the silver nanoparticles (AgNPs), gold nanoparticles (AuNPs) and palladium nanoparticles (PdNPs) are found most vital and promising, among other nanoparticles. The biomedical activities of these particles mostly depend on their shape, size and distribution. Preparation of these particles in an eco-friendly method is an immediate need of the society. Herein, AuNPs, AgNPs and PdNPs (MNPS) were synthesized by Solanum nigrum Leaves (SNL) extract. The structural and morphological studies were carried out by using TEM, XRD and EDAX, while the optical and chemical properties were studied using UV-visible spectrum and FTIR spectroscopy. The particles obtained were found to possess a FCC (Face Centered Cubic) structure. TEM images of Ag, Au and PdNPs showed spherical well dispersed nanoparticles with average size of 3.46 nm, 9.39 nm and 21.55 nm respectively. The FTIR spectra confirmed polyphenols and antioxidants in SNL extract act as reducing and capping agents respectively in the synthesis of MNPs. The EDX technique confirmed the presence of silver, gold and palladium nanoparticles. Antimicrobial studies noted that the AgNPs have effective inhibition against E. coli. The complete reduction of 4-Nitrophenol and the formation of 4-Aminophenol with the presence of NaBH4 was chosen for the study of catalytic activities of the prepared MNPs. The reduction time of Au and Pd catalyst were smaller compared to that of Ag. This viable preparation method for producing small spherical shaped nanoparticles expected to the applied to the fields of nanomedicine.

Steroidal alkaloid glycosides and phenolics from the immature fruits of Solanum nigrum.

Solanum nigrum L. (also called as European black nightshade) has been traditionally used as folk medicine and food in some regions. Phytochemical investigations of the immature fruits of S. nigrum yielded five steroidal alkaloid glycosides (1-5), including an unprecedented nor-spirosolane type steroidal alkaloid with a five-membered ring A (1) and two novel spirosolane type steroidal alkaloid glycosides (2, 3), together with eight known phenolic compounds (6-13). Their structures were elucidated on the basis of spectroscopic and chemical methods, including IR, NMR, HR-ESI-MS, and GC analyses. Five steroidal alkaloid glycosides were tested for their potential antiproliferative effects against HL-60, U-937, Jurkat, K562, and HepG2 cell lines and inhibitory activities on nitric oxide (NO) production induced by lipopolysaccharide (LPS) in a macrophage cell line RAW 264.7. Compound 1 exhibited significant inhibition on NO production with an IC50 value of 23.4 ±â€¯2.0 µM, compared to positive control indomethacin (IC50, 47.40 ±â€¯4.50 µM). Compound 4 exhibited significant cytotoxicity against all tested cell lines.

Preparative isolation and purification of steroidal glycoalkaloid from the ripe berries of Solanum nigrum L. by preparative HPLC-MS and UHPLC-TOF-MS/MS and its anti-non-small cell lung tumors effects in vitro and in vivo.

Overcoming epidermal growth factor receptor resistance is a critical problem that needs to be solved in clinical practice. Drugs that downregulate the fatty acid synthase-epidermal growth factor receptor will become novel treatments for non-small cell lung cancer. Solanum nigrum, extracted with water at 4°C, shows strong cytotoxic activity and inhibits tumor growth in Lewis tumor bearing-mice in a dose-dependent manner. A novel active compound in S. nigrum, solaoiacid, was successfully separated and purified from S. nigrum by preparative high-performance liquid chromatography with mass spectrometry and ultra high performance liquid chromatography with time-of-flight tandem mass spectrometry. The IC50 of solaoiacid on lung cancer cells was 2.3 µmol/L, which was significantly lower than that of the known steroidal glycoalkaloid. Label-free proteomics and STRING Network analysis were used to identify significantly deregulated proteins in lung cancer cells that were treated with the fresh ripe fruit extracts of S. nigrum. S. nigrum regulates multiple signal pathways, including the epidermal growth factor receptor pathway. S. nigrum downregulated 24 main proteins with direct roles in fatty acid biosynthesis. Both S. nigrum and solaoiacid showed strong downregulation of the fatty acid synthase-epidermal growth factor receptor and anti-non-small cell lung cancer effects, and thus will become a novel drug for the treatment of non-small cell lung cancer.

Alkaloids, flavonoids, polyphenols might be responsible for potent antiarthritic effect of Solanum nigrum.

OBJECTIVE: To evaluate in vitro and in vivo antiarthritic potential of Solanum nigrum (S. nigrum). METHODS: Aqueous methanolic (70∶30) extract of S. nigrum was prepared. The in vitro antiarthritic effect was evaluated in terms of its inhibition of protein denaturation and membrane stabilization. While, formaldehyde, complete Freund's adjuvant (CFA) and Collagen induced arthritis rat models were used to study in vivo antiarthritic activities of S. nigrum at dose level of 200, 400 and 800 mg/kg. RESULTS: The extract exhibited inhibition of protein denaturation and protected red blood cell by stabilizing the membranes in a concentration dependent manner, with maximum effect attained at 800 µg/mL. Moreover, there was a marked reduction in paw edema observed in extract treated animals, when compared to arthritic control animals in all in vivo models and 800 mg/kg dose got maximum reduction of paw edema. In CFA and collagen models, plant extract restored body weight, hematologic parameters, radiographic and histopathologic alterations towards normal. CONCLUSION: It could be concluded that S. nigrum holds antiarthritic potential, supporting its traditional use in treatment of rheumatoid arthritis.

Emerging themes of regulation of oncogenic proteins by Solanum nigrum and its bioactive molecules in different cancers.

Research over the decades has sequentially and systematically provided a near-complete resolution of multifaceted and therapeutically challenging nature of cancer. Drug discovery from plants has enjoyed a renaissance in the past few years. Natural products have provided many of the lead structures, which are currently being used as templates for the design and synthesis of novel compounds with biologically enhanced properties. With the maturity and diversification of technologies, there is a growing need to design high-throughput functional assays for the evaluation of the myriad of compounds being catalogued. This review sheds light on the tumor suppressive properties of Solanum nigrum and its bioactive ingredients. Several worthy of mention include uttroside B, solanine, solamargine, and physalins, which have been tested for efficacy in cancer cell lines and xenografted mice. We have summarized the most recent findings related to S. nigrum-mediated regulation of intracellular protein network in different cancers. α-Solanine, an active component of S. nigrum, is involved in the regulation of microRNA-21 (miRNA-21) (oncogenic) and miRNA-138 (tumor suppressor) in prostate cancer. However, this is the only available evidence that gives us a clue related to the tumor suppressive effects exerted by components of S. nigrum at a posttranscriptional level. More interestingly, S. nigrum and its components exerted inhibitory effects on different pathways including PI3K/AKT, JAK-STAT, VEGF/VEGFR, and matrix metalloproteinases in different cancers. We also provide an overview of new tools, methodologies, and approaches, which will allow researchers to extract as much information as possible out of the tremendous data sets currently being generated. The use of computational tools will be helpful in processing structurally complex natural products and also in prediction of their macromolecular targets.