Integrating medicinal plants into healthcare supports the Sustainable Development Goals (SDGs) and facilitates the development of new drugs. Anisotesis a genus of medicinal plants traditionally used to treat various diseases, including diabetes, hepatitis, jaundice, gallstones, and other hepatic disorders. The genus comprises 19 species that are widely distributed in tropical eastern and southern Africa, Madagascar, and the Arabian Peninsula. Among them, Anisotestrisulcus and A. sessiliflorus are the most extensively studied species. Phytochemical investigations reveal that pyrroloquinazoline alkaloids, such as vasicine, vasicinone, anisotine, and trisulcusine derivatives, are dominant constituents, with several exhibiting potent biological activities. The purpose of this review is to provide information on the traditional uses, chemical constituents, spectral data of isolated alkaloids, and biological activities of Anisotesspecies. The reported biological properties inflammatory, cytotoxic, and antihyperglycemic activities, largely attributed to their alkaloidal content. By documenting the traditional uses and biological activities of Anisotesspecies, we aimed to support new research on these plants, especially on those species whose biological potential has not yet been studied.
Abstract Background Highlighting affordable alternative crops that are rich in bioactive phytoconstituents is essential for advancing nutrition and ensuring food security. Amaranthus blitum L. (AB) stands out as one such crop with a traditional history of being used to treat intestinal disorders, roundworm infections, and hemorrhage. This study aimed to evaluate the anthelmintic and hematologic activities across various extracts of AB and investigate the phytoconstituents responsible for these activities. Methods In vitro anthelmintic activity against Trichinella spiralis was evaluated in terms of larval viability reduction. The anti-platelet activities were assessed based on the inhibitory effect against induced platelet aggregation. Further, effects on the extrinsic pathway, the intrinsic pathway, and the ultimate common stage of blood coagulation, were monitored through measuring blood coagulation parameters: prothrombin time (PT), activated partial thromboplastin time (aPTT), and thrombin time (TT), respectively. The structures of isolated compounds were elucidated by spectroscopic analysis. Results Interestingly, a previously undescribed compound (19), N-(cis-p-coumaroyl)-ʟ-tryptophan, was isolated and identified along with 21 known compounds. Significant in vitro larvicidal activities were demonstrated by the investigated AB extracts at 1 mg/mL. Among tested compounds, compound 18 (rutin) displayed the highest larvicidal activity. Moreover, compounds 19 and 20 (N-(trans-p-coumaroyl)-ʟ-tryptophan) induced complete larval death within 48 h. The crude extract exhibited the minimal platelet aggregation of 43.42 ± 11.69%, compared with 76.22 ± 14.34% in the control plasma. Additionally, the crude extract and two compounds 19 and 20 significantly inhibited the extrinsic coagulation pathway. Conclusions These findings extend awareness about the nutritional value of AB as a food, with thrombosis-preventing capabilities and introducing a promising source for new anthelmintic and anticoagulant agents.
Ethyl acetate fraction column chromatographic analysis was used to isolate eleven compounds (numerically tagged 1–10) from Cassia occidentalis L. in this study. Two unique metabolites, including a neolignan compound designated as occidentalignan I (9) and a flavonoidal glycoside, chrysin-7-O-α-L-rhamnopyranosyl (10), were identified, while silybin A (8) was the first flavonolignan to be isolated from the Fabaceae family. Four compounds, including β-sitosterol-3-O-β-D-glucopyranoside (1), stigmasterol-3-O-β-D-glucopyranoside (2), betulinic acid (3), and vanillic acid (4) were isolated from C. occidentalis for the first time. In addition, four known compounds, cinnamic acid (5), p-hydroxybenzoic acid (6), β- resorcylic acid (7), and citric acid (11), were also detected. The in-vitro cytotoxicity assessment of the methanolic extract of C. occidentalis on seven cancer cell lines, including A-549, Colo-205, Huh-7, HCT-116, PANC-1, SKOV-3, and BNL, demonstrated its selective potent cytotoxicity on lung cancer cells without affecting normal BNL cells. In contrast, the methanolic extract showed moderate activity on Colo-205 and Huh-7 and nearly no activity on HCT-116, PANC-1, and SKOV-3 cell lines. These results suggest that the methanolic extract of C. occidentalis is an excellent candidate with potential antiproliferative activity against lung cancer; however, further studies are necessary to clarify its mechanism of action.
Ethnopharmacological relevance: Gmelina philippensis CHAM is an ornamental plant that is distributed in South Asia and warm regions of the Mediterranean area. The plant is traditionally applied in folk medicine for the treatment of diabetes. Aim of the study: To evaluate the cytotoxic and the antidiabetic activities of the ethanolic extract of G. philippensis aerial parts. To isolate the metabolite(s) responsible for these activities and to elucidate the mechanism of action by molecular docking study.Materials and methods: Compounds (1-11) were isolated using various chromatographic techniques and their structures were determined by NMR spectroscopic and mass spectrometric analysis. The cytotoxic effect was tested using viability test and MTT assay. Antidiabetic activity was evaluated by measuring the inhibitory activity of the ethanolic extracts and compounds against alpha-glucosidase and alpha-amylase activities. Modeling and docking simulations were performed using Molecular Operating Environment software and the crystal structure of protein kinases CDK2, (1PYE) and AKT1 (4GV1), in addition to alpha-glucosidase (3TOP) and alpha-amylase (2QV4).Results: Compounds 2, 3 and 8 were isolated for the first time from the plant and identified as: gmelinol (2), apigenin (3) and tyrosol (8). While beta-sitosterol-3-O- beta-D-glucopyranoside (4) vicenin-II (7), rhoifolin (9), isorhoifolin (11) were isolated for the first time from the genus, along with and the new iridoid 6-O-alpha-L-(2 ''-Obenzoyl-4 ''-O-trans-p-methoxycinnamoyl)rhamnopyranosyl-1 alpha- beta-D-glucopyranoside catalpolgenin (6). In addition, to the previously reported compounds: mixture of beta -sitosterol and stigmasterol (1), and 6- O- alpha-L(2 '',3 '',4 ''-tri-O -benzoyl)rhamnopyranosylcatalpol (5) and 6-O-alpha-L-(2 ''-O-trans-p-methoxycinnamoyl)rhamnopyranosylcatalpol (10). The cytotoxic activity against hepatocellular carcinoma (HepG-2) cell lines for compounds 2, 5, 7, 9 and 11 was conducted using cisplatin as a standard. Gmelinol (2) exhibited strong cytotoxic activity against HepG-2 cell lines with IC 50 value of 3.6 +/- 0.1 mu g/ml which is more potent than the standard cisplatin IC 50 = 8.7 +/- 0.9 mu g/ml. Molecular modeling of 2 against diverse targets of protein kinases suggested that CDK-2 and AKT-1 could be the dual probable kinase targets for its cytotoxic action. Compound 2 showed alpha-amylase inhibition activity with IC 50 value of 60.9 (mu g/ml) while, compounds 5 showed strong alpha-glucosidase inhibition activity with IC 50 values of 41.7 (mu g/ml) compared to acarbose with IC 50 value of 34.7, 30.6 (mu g/ml). Molecular docking of compounds 2 and 5 on alpha-glucosidase (3TOP) and alpha-amylase (2QV4) enzymes revealed high binding affinity and active site interactions comparable to native ligand acarbose. Conclusion: The ethanolic extract of G. philippensis CHAM aerial parts is effective against HepG-2 cell lines, alpha-amylase and alpha-glucocidase activities. Biologically guided isolation indicated that compounds 2 and 5 are responsible for these activities. These results were supported by DMF calculations that detected the molecular areas responsible for protein interactions shown via docking studies.
Autism spectrum disorders are a neurodevelopmental condition characterized by disturbances in social interaction and communication, as well as repetitive and restricted behaviors. No efficient treatment plans have been found so far. The neurodevelopmental effects of antiandrogens on developmental milestones were examined in rats following a single intraperitoneal injection of adult pregnant female rats with valproic acid (VPA) (600 mg/kg) on gestation day 12.5. Control females were injected with physiological saline at the same time. The offspring of set 1 (which received physiological saline) was divided into 2 groups (groups 1&2) and the offspring of set 2 (which received VPA) were divided into 5 groups (groups 3-7). Thus, the seven groups were organized as follows: Group 1, the control group in which pups did not receive any treatment. Group 2, pups were given sesame oil vehicle. Group 3 pups did not receive any further treatment. Group 4 in which the pups were given sesame oil. Group 5 in which the pups received 1 mg/day testosterone propionate subcutaneously. Group 6 in which the pups received flutamide 1 mg/kg subcutaneously. Group 7 in which the pups received finasteride 50 mg/kg subcutaneously. Our results demonstrated that VPA-induced retardation in sensorimotor reflexes, but did not affect physical landmarks while antiandrogens improved developmental milestones. In conclusion, our finding confirms that androgen contributes partially towards VPA-induced neurodevelopmental insults.
Cassia occidentalis L., from Fabaceae family phytochemical screening, revealed several biologically active principles mainly flavonoids and anthraquinones. GLC analysis of the lipoidal matter afforded 12 hydrocarbons: 9dodecyl-tetradecahydro-anthracene (48.97 %), 9-dodecyl-tetradecahydro-phenanthrene (14.43 %), and 6 sterols/triterpenes: isojaspisterol (11.99%) and fatty acids were palmitic acid (50 %), and Linoleic acid (16.06%). Column chromatography led to the isolation of fifteen compounds (1-15), elucidated using spectroscopic evidence. First report of undecanoic acid (4) from the family Fabaceae, while p-dimethyl amino-benzaldehyde (15) was first time isolated from a natural origin. Eight compounds isolated for the first time from C. occidentalis L.; beta-amyrin (1), beta-sitosterol (2), stigmasterol (3), camphor (5), lupeol (6), chrysin (7), pectolinargenin (8), and 1, 2, 5-trihydroxy anthraquinone (14) besides five known compounds previously isolated; apigenin (9), kaempferol (10), chrysophanol (11), physcion (12), and aloe-emodin (13). In-vivo evaluation of anti-inflammatory and analgesic effects of C. occidentalis L. extracts where the n-butanol and total extracts showed the highest activities. The percentage of the inhibitory effect of the n-butanol extract was 29.7 at a dose of 400 mg/Kg. Furthermore, identified phytoconstituents were docked into the active sites of enzymes nAChRs, COX-1, and COX-2 to evaluate binding affinity. Phyto-compounds Physcion, aloe-emodin, and chrysophanol were found to have a good affinity for targeted receptors compared to co-crystalized inhibitors, validating the analgesic and anti-inflammatory effects of the phytochemicals.
Several Amaranthus vegetables (Amaranthaceae) have been recognized as valuable sources of minerals, vitamins, proteins, and phytonutrients, with health-promoting characteristics. In this study, three edible Amaranthus species, namely A. hybridus (AH), A. blitum (AB), and A. caudatus (AC), were chemically characterized using non-targeted liquid chromatography-tandem mass spectrometry (LC-MS/MS) technique. Further, multivariate chemometric analyses were conducted, including principal component analysis (PCA) and correlation-covariance plot (C-C plot). As a result, forty-one diverse compounds were identified, which varied in distribution and abundance across the investigated species. Amino acids and flavonoid glycosides were the most prevalent metabolites. Other identified compounds comprised nucleoside, chlorogenic acids, hydroxy cinnamoyl amides, and triterpenoid saponins. The most discriminant metabolites were flavonoid glycosides and hydroxy cinnamoyl amides, giving each species a chemotaxonomic identity. Advancing the chemotaxonomy of Amaranthaceae, adenosine nucleoside and N-coumaroyl-ʟ-tryptophan were first reported from this family. Isorhamnetin and tricin glycosides were uniquely identified in AC, offering useful chemotaxonomic markers for this species. Notably, AB and AH profiles shared most metabolites, yet with varying abundance. These include adenosine, nicotiflorin, dicaffeoylquinic acids, and N-trans-feruloyl-4-O-methyldopamine. However, N-coumaroyl-ʟ-tryptophan and kaempferol dirhamnoside were exclusively found in AB, separating it from AH. In conclusion, the applied analytical techniques established molecular fingerprints for the included species, identified specific biomarkers, and investigated their interconnections.
Unlike synthetic medications, natural-source compounds have fewer side effects, are less expensive, come from renewable sources, and have a higher level of acceptance due to their long history of use.Many of today's medications are based on
BackgroundThe aim of the present study was to identify neurophysiologic markers to differentiate between Alzheimer dementia (AD), Vascular dementia (VaD), and Parkinson's disease dementia (PDD), and to examine their relationship to levels of transforming growth factor β1 (TGFβ1).MethodsThe study included 15 patients with each type of dementia (AD, VaD, PDD) and 25 control subjects. Dementia patients were diagnosed according to the Diagnostic and Statistical Manual of Mental Disorders 4th edition-revised (DSM-IV-R). Modified Mini Mental State Examination (MMMSE), motor cortex excitability including resting and active motor thresholds (rMT, aMT), input-output (I/O) curve, contralateral and ipsilateral silent periods (cSP, iSP), short-interval intracortical inhibition (SICI) at 1,2 and 4ms, and serum levels of TGFβ1 were examined.ResultsThere were no significant differences between groups with regards to age, sex, education or socioeconomic level. There was significant neuronal hyperexcitability in the form of reduced rMT and aMT and a shallower I/O curve in all three groups of dementia compared with the control group. The durations of cSP and iSP were longer in AD and PDD groups compared with the control group, whereas there were no significant differences in VaD. SICI was less effective in the three dementia groups than in the control group at intervals of 4ms. Serum levels of TGFβ1 were significantly elevated in all dementia groups in comparison with the control group. There was a significant negative correlation between serum level of TGFβ1 and cSP, iSP, and SICI across all patients and a significant negative correlation between serum level of TGFβ1 and iSP duration in AD.ConclusionAlthough motor thresholds were reduced in all patients, measures of SICI, cSP and iSP could distinguish between dementia groups. Serum level of TGFβ1 negatively correlated with iSP specifically in the AD group. This suggests that levels of TGFβ1 may relate to GABAergic dysfunction in dementia.
Background: There are currently few biomarkers to assist in early diagnosis of dementias. Objective: To distinguish between different dementias: Alzheimer’s disease (AD), vascular dementia (VaD), and Parkinson’s disease dementia (PDD) using simple neurophysiologic (P300) and laboratory markers (transforming growth factor β1 “TGF-β1”). Methods: The study included 15 patients for each type of dementia and 25 age- and sex-matched control subjects. Dementia patients were diagnosed according to the Diagnostic and Statistical Manual of Mental Disorders 4th edition-revised (DSM-IV-R). Modified Mini-Mental State Examination (3MS), Memory Assessment Scale (MAS), P300, and TGF-β1 were examined for each participant. Results: There were no significant differences between groups as regard to age, sex, and education, social, and economic levels. Significant differences between groups were observed in registration and naming variables of the 3MS. Compared with the control group, P300 latency was prolonged in all groups, although to a greater extent in AD and PDD than in VaD. A serum level of TGF-β1 was significantly elevated in all groups but was significantly higher in AD and VaD than in PDD. 3MS tended to correlate with P300 more than TGF-β1, and to be stronger in AD than the other groups. Conclusion: Measurements of P300 latency and serum levels of TGF-β1 can help distinguish AD, PDD, and VaD. P300 was more prolonged in AD and PDD than VaD whereas TGF-β1 was significantly higher in AD and VaD than PDD. Thus P300 and TGF-β1 may be useful biomarkers for detection and evaluation of the extent of cognitive dysfunction.
Therapeutic alternatives are being searched for trichomoniasis as a result of the increased prevalence of metronidazoleresistant infections.Mangifera indica L. (Anacardiaceae) is an important tree with a long history in medicine.Traditionally, it has been used as an anti-diarrheal and anti-diabetic, and recently, its gallotannin-rich leaves and stem bark extracts have shown antiparasitic activities against various parasites.Aiming at exploring the anti-Trichomonas vaginalis activity of mango's gallotannins, an aqueous ethanol extract of fresh kernels of M. indica was phytochemically investigated.Based on a simple gel chromatographic procedure, ethyl gallate (2), a group of five isomeric tetragalloyl-glucoses (3-7), and a pentagalloylglucose (8) were simultaneously isolated from a single fraction by a preparative Reversed-phase-high performance liquid chromatography.The isolates were identified based on spectroscopic analyses and comparison with reported data.They showed structural-dependent inhibitory effects on the growth of T. vaginalis trophozoites in an in vitro investigation.Ethyl gallate and 1,2,4,6-tetra-O-galloyl-β-D-glucose (7) exhibited elevated anti-T.vaginalis activity (IC 50 = 1.3, 2.4 μg/ml, respectively).This is the first report exploring the potential of gallotannins as trichomonacidal agents.
Two new polycyclic pyrroloquinazoline alkaloids with unprecedented skeleton, anisulcusines A (1) and B (2), along with four known compounds (3-6), were identified from the aerial parts of Anisotes trisulcus (Forssk.) Nees. To our knowledge, anisulcusines A and B are the first polycyclic pyrroloquinazoline alkaloids that possess a unique N-methyl-1,2-dihydro-1'H-spiro[benzo[d][1,3]oxazine moiety. The chemical structures of the new compounds were elucidated through extensive spectroscopic analyses and high-resolution mass spectroscopy. Anisulcusine B (2) exerted moderate cytotoxic effect on cultured human hepatoma (HuH7) cells, whereas compounds 1 and 3-5 exhibited mild cell proliferative or growth stimulatory activity. HIGHLIGHTS Two new polycyclic pyrroloquinazoline alkaloids from Anisotes trisulcus. Structures were elucidated on the basis of 1D- and 2D-NMR and HR-ESI-MS spectra. Compound (2) exerted moderate cytotoxic effect against human hepatoma (HuH7) cells. Compounds (1, 3-5) exhibited mild cell proliferative or growth stimulatory activity.
Background: Alhagi maurorum, commonly used in folk medicine, has been reported to have several biological activities. Objective: We have studied the antioxidant chemical components from A. maurorum to determine their in vitro antiproliferative and hepatoprotective activities. Materials and Methods: The alcoholic extract of A. maurorum root was subjected to a successive solvent fractionation and various chromatographic techniques guided by the 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging assay to isolate their antioxidant active compounds. The structures of the isolated compounds were identified through the extensive use of nuclear magnetic resonance and mass spectroscopy coupled with correlation to known compounds. The antioxidant and cytotoxic activities of the isolated compounds were quantified using DPPH and 3-(4,5-dimethyl-2-thiazolyl)-2,5-diphenyl-2H-tetrazolium bromide assays, respectively. The hepatoprotective activity of each extract and the total flavonoid fraction were assessed quantitatively on carbon tetrachloride (CCl4)-induced hepatotoxicity in rats. Results: Fourteen flavonoids, including four aglycones (1-4) and ten glycosides (5-14), were isolated. The flavonoid glycosides (6-14) are being reported for the first time to our knowledge. The free aglycones, those of the flavonol type, exhibited strong antioxidant and antiproliferative activities. The flavonoid glycosides exhibited weak cytotoxic activity against the hepatocellular carcinoma cell line. The total flavonoid fraction showed the strongest hepatoprotective activity against CCl4-induced hepatotoxicity. Conclusion: A total of 14 flavonoids were identified from A. maurorum; nine of them were isolated for the first time. Flavonoids were the main chemical group identified from the A. maurorum root extracts, and they are responsible for the hepatoprotective activity. The findings set up a scientific explanation for the folkloric administration of A. maurorum in the treatment of hepatic disorders.
Background: Leukemia is the most common cause of disease-related death in childhood despite significant improvement in survival and modern risk stratification. Prognostic significance of absolute lymphocytic count (ALC) recovery was studied in pediatric patients with acute lymphoblastic leukemia (ALL). Methods: One hundred twenty one patients newly diagnosed asALL ≤ 18 yearstreated at pediatric oncology department, South Egypt Cancer Institute from 2011 to 2015 were enrolled. Age, sex, initial total leucocytic count, immunophenotyping, central nervous system (CNS) involvement, mediastinal mass, bone marrow (BM) response on day fifteen and after finishing induction remission were compared to ALC recovery on day 15 (ALC-15) and day 29 (ALC-29) of induction response. Also, prognostic impact of ALC recovery on event free survival (EFS) and overall survival (OS) was evaluated. Results: ALC didn’t show any significant relation to known patients’ prognostic factors. Patients with low ALC didn’t show significant lower response on day 15 and post induction evaluation from those with high ALC (p = 0.74, 0.6 respectively). ALC-15 ≥ 500 cells/uL showed a prognostic significance as patients with ALC-15 500 cells/uL had a poorer outcome (4- EFS 47.8% ± 0.12%) than patients with ALC-15 ≥ 500 cells/uL who carried a better outcome (4-EFS 66.3% ± 0.05%). Neither ALC-500 (day 29) nor ALC-350 (day 15 & day 29) had impact on OS or EFS. In multivariate analysis, ALC-15 500 cells/uL still had a poor impact on outcome (OR 2.56, 95% CI 1.27 - 5.14) with d15-BM response (OR 2.99, 95% CI 1.35 - 6.61) and age 10 (OR 1.96, 95% CI 1.01 - 3.69). Conclusions: ALC-15 has an independent prognostic impact on outcome as well as simple, inexpensive, and easy to interpret. Although, it’s utility in risk stratification of ALL still need a confirmation through a multicenter study with uniform variables, large cohort and long duration of follow up.
Gmelina philippensis Cham.Family Lamiaceae, sometimes placed in family Verbenaceae, is one of the ornamental and medicinal plants, known as parrot's peak, as it produces yellow flowers from a long tube-shaped structure comprised of overlapping bracts.It is a sprawling thorny shrub that was formerly taxonomically classified to family Verbenaceae.It is native to Philippines, Burma and distributed in tropical and subtropical countries.The present investigation attempts to study the pharmacognostical features of the aerial parts (leaves, stems and inflorescence) of Gmelina philippensis Cham.which could be helpful in authentication of the plant and establishing pharmacognostical standard measurements which help in its identification in both entire and powdered forms.
As claimed by Snell (2009), "if you are not online, you don't exist'' [30]. The remarkable global phenomenon of this age is social networks sites (SNSs) that are web pages with social features. Computing students tend to use SNS extensively for communicating during their learning or for sharing their learning outputs. There are five broad major areas of extensive work in SNSs that are (i) Impression management and Friendship performance, (ii) networks structure and visualizations of link data in SNSs, (iii) bridging online and offline networks, (iv) the issue of Privacy, and (v) the relationship of SNSs with cultural values. Drawing on literature review and digital human interaction reports, as well as on theoretical behavioral sources, this paper examines the factors of SNSs that diffuse through different variables to determine the transformation of the educational sector with the use of SNS. In particular, the paper proposes a conceptual model based on extensive literature review and the supporting data collection for assessing the role of SNS in Computing Education (CE). The paper discusses a multi-methodological approach in interpretive-inductive research where quantitative tools (e.g. surveys with computing students) are intertwined with qualitative ones (e.g. ethnography of student Facebook pages and focus group). The paper presents a comprehensive model investigating the relationship between SNSs and key dimensions affecting digital readiness process in education. The research is focused on research carried out in Egyptian social media, therefore the proposal and subsequent findings will be in the first instance consider Egyptian education.