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Objectives: Hypertension is the number one risk factor and primary contributor of cardiovascular diseases. Caesalpinia benthamiana is a valuable medicinal plant with unvalidated anti-hypertensive activity. This study was carried out to explore the antihypertensive effect of C. benthamiana on uninephrectomized hypertensive rats., Methods: Fifty rats were grouped into five groups, each containing 10 animals: Group A-normal control (normotensive); B-uninephrectomized control; C-uninephrectomized treated with 50 mg/kg C. benthamiana extract; D-uninephrectomized treated with 100 mg/kg C. benthamiana ; and E- uninephrectomized treated with 10 mg/kg of Lisinopril., Results: Significant increases were observed in systolic, diastolic and mean blood pressure of uninephrectomized control rats. Furthermore, markers of oxidative stress (malondialdehyde, hydrogen peroxide, protein carbonyl, myeloperoxidase and the advanced oxidative protein products) increased significantly while antioxidant status (reduced glutathione, glutathione peroxidase, glutathione S-transferase and superoxide dismutase), reduced significantly in uninephrectomized hypertensive rats. Histopathology revealed thrombosis and occlusion of coronary vessels in the heart, and congestion in the kidney. However, the observed high blood pressure parameters were remarkably normalized together with reduction in markers of oxidative stress and improvement in antioxidant defence system of uninephrectomized hypertensive rats treated with C. benthamiana extract similar to normotensive rats., Conclusions: C. benthamiana extract exhibited antihypertensive action, strong antioxidant ability, attenuated oxidative stress-mediated hypertension and lessened the development of cardiac and renal damage associated with hypertension induced by uninephrectomy and high dietary intake of salt. Together, C. benthamiana extract might be useful in the management of hypertension due to volume overload in the cardiovascular system., (© 2020 Walter de Gruyter GmbH, Berlin/Boston.)

Caesalpinia ferrea C. Mart. , popularly known as "Jucá" or "Pau-ferro", belongs to the Fabaceae family, and is classified as a native and endemic species in Brazil. Numerous studies that portray its ethnobotany, chemical composition, and biological activities exist in the literature. The present study aimed to systematically review publications addressing the botanical aspects, uses in popular medicine, phytochemical composition, and bioactivities of C. ferrea . The searches focused on publications from 2015 to March 2020 using the Scopus, Periódicos Capes, PubMed, Google Scholar, and ScienceDirect databases. The leaves, fruits, seeds, and bark from C. ferrea are used in popular medicine to treat disorders affecting several systems, including the circulatory, immune, cardiovascular, digestive, respiratory, genitourinary, musculoskeletal, and conjunctive systems. The most commonly found chemical classes in phytochemical studies are flavonoids, polyphenols, terpenoids, tannins, saponins, steroids, and other phenolic compounds. The biological properties of the extracts and isolated compounds of C. ferrea most cited in the literature were antibacterial, antifungal, antioxidant, antiproliferative, anti-inflammatory, and healing potential. However, further studies are still needed to clarify a link between its traditional uses, the active compounds, and the reported pharmacological activities, as well as detailed research to determine the toxicological profile of C. ferrea .

Two dimeric cassane diterpenoids with an unprecedented 6/6/6/6/6/5/6/6/6 nonacyclic framework, pterolobirins A and B ( 1 and 2 ), were isolated from the fruits of Pterolobium macropterum . Their structures were assigned by interpreting the spectroscopic data. The absolute configuration of 1 was unequivocally confirmed by single-crystal X-ray diffraction data. A putative biosynthetic pathway is proposed based on a regular intermolecular Diels-Alder reaction and an intramolecular nucleophilic addition.

: To understand the RBC protecting efficiency and antiplatelet activity of methanolic extract of Caesalpinia crista coat (MECCC). RBC-protecting activity of MECCC was evaluated using assays, such as DPPH, level of lipid peroxidation, protein carbonyl content, superoxide dismutase and catalase as a marker of oxidative stress whereas, platelet aggregation inhibition was performed using human platelet-rich plasma (PRP). MECCC showed about 76% of DPPH-scavenging activity, with an IC50 value of 71.89 μg/ml. The MECCC reduced the level of lipid peroxidation and protein carboxylation in RBC caused by NaNO2 in a dose-dependent manner. In addition, MECCC normalized the levels of superoxide dismutase (SOD) and catalase (CAT) in oxidative stress-induced RBC in a dose-dependent manner. This suggested the protective effect of MECCC on RBC against oxidative stress. Furthermore, MECCC also exhibited mild antiplatelet activity by inhibiting both ADP and epinephrine agonists that induced platelet aggregation. The noticed inhibition percentage was found to be 28 and 23%, respectively at the concentration of 150 μg. Interestingly, MECCC did not hydrolyse the RBC suggesting its nontoxic properties. MECCC possesses protective effect of RBC against NaNO2 (10 mmol/l) induce oxidative stress and inhibits platelet aggregation.

Influenza virus infections can lead to viral pneumonia and acute respiratory distress syndrome in severe cases, causing significant morbidity and mortality and posing a great threat to human health. Because of the diversity of influenza virus strains and drug resistance to the current direct antiviral agents, there have been no effective drugs as yet to cure all patients infected by influenza viruses. Natural products from plants contain compounds with diverse structures that have the potential to interact with multiple host and virus factors. In this study, we identified the ethanol extract of Caesalpinia decapetala (Roth) Alston (EEC) as an inhibitor against the replication of a panel of influenza A and B viruses both on human pulmonary epithelial A549 and human monocytic U937 cells. The animal study revealed that EEC administration reduces the weight loss and improves the survival rate of mice infected with lethal influenza virus. Also, EEC treatment attenuated lung injury and reduced virus titer significantly. In conclusion, we showed that EEC has antiviral activity both in vitro and in vivo, suggesting that the plant C. decapetala has the potential to be further developed as a resource of new anti-influenza drugs.

Three dimeric cassane diterpenoids, caesalpanins A-C, were isolated from the seeds of Caesalpinia sappan L., as well as three known compounds. Their structures were determined via analysis of 1D-, 2D-NMR, and HR-ESI-MS data. Caesalpanins A and B were the second and third compounds that presented a nitrogen-containing cassane diterpenoid dimer linked through one ether bond between C-19 and C-20'. Caesalpanin B exhibited moderate cytotoxic activity against MCF-7 cell lines with IC 50 value of 29.98 μm. Caesalpanins A and B had weak inhibitory effects against LPS-induced nitric oxide (NO) production in RAW 264.7 macrophages at 50 μm with inhibitory rate of 36.01 % and 32.93 %, respectively., (© 2020 Wiley-VHCA AG, Zurich, Switzerland.)

Ten new cassane diterpenoids, caesalpulcherrins A-J ( 1 - 10 ), together with 11 known analogues ( 11 - 21 ) were isolated from the aerial parts of Caesalpinia pulcherrima . Their structures and relative stereochemistry were elucidated by spectrometric and spectroscopic methods, including one-dimensional (1D) and two-dimensional (2D) NMR, high-resolution electrospray ionization mass spectrometry (HRESIMS), and single-crystal X-ray diffraction analysis. Compounds 1 - 4 represent the first examples of 2,5-dimethoxyfuranocassane diterpenoids. Results of the antifeedant activity indicated that isovouacapenol C ( 12 ) and pulcherrin N ( 14 ) exhibited remarkable antifeedant activity against Mythimna separate with EC 50 values of 3.43 and 4.20 μg/cm 2 , respectively. Meanwhile, pulcherrimin C ( 13 ) and 12-demethyl neocaesalpin F ( 18 ) exerted significant antifeedant activity against Plutella xylostella with an EC 50 data of 4.00 and 3.05 μg/cm 2 , respectively. Some of the compounds showed obvious toxic activity against the plant-feeding generalist insect herbivores, M. separate and P. xylostella , at 0.8 mg/mL (800 ppm). Furthermore, the structure-activity relationships of antifeedant and insecticidal activities are also discussed in the article.

Background: Porcine reproductive and respiratory syndrome (PRRS) caused by PRRS virus (PRRSV) results in economic losses in the swine industry globally. Several studies have investigated the use of plant extracts in the prevention and control of PRRS outbreaks. Thai medicinal plants may be useful for treating PRRSV infection in pigs. Therefore, we investigated the in vitro anti-PRRSV and antioxidant properties of seven Thai medicinal plants: Caesalpinia sappan Linn., Garcinia mangostana Linn., Houttuynia cordata, Perilla frutescens, Clinacanthus nutans, Phyllanthus emblica, and Tiliacora triandra., Results: Using antiviral screening, we observed that T. triandra extract strongly inhibited PRRSV infectivity in MARC-145 cells [virus titer 3.5 median tissue culture infective dose (TCID 50 )/ml (log10)] at 24 h post-infection, whereas C. sappan extract strongly inhibited PRRSV replication [virus titer 2.5 TCID 50 /ml (log10)] at 72 h post-infection. C. sappan extract had the highest total phenolic content [220.52 mM gallic acid equivalent/g] and lowest half-maximal inhibitory concentration [1.17 mg/ml in 2,2-diphenyl-1-picrylhydrazyl and 2.58 mg/ml in 2,2-azino-bis (3-ethylbenzothiazo-line-6-sulfonic acid) diammonium salt]., Conclusion: T. triandra extract could inhibit PRRSV infectivity, whereas C. sappan extract was the most effective in inhibiting PRRSV replication in MARC-145 cells. This study elucidates the antiviral activities of Thai medicinal plant extracts in vivo. The results promise that Thai medicinal plant extracts, particularly T. triandra and C. sappan extracts, can be developed into pharmaceutical drugs for the prevention of PRRS in pigs.

Caesalpinia bonduc has been used in herbal medicines for the treatment of a wide range of diseases from decades. The present study has explored the remedial potential and underlying mechanism of polyphenol extract of Caesalpinia bonduc in alloxanized diabetic rats. HPLC/MS analysis confirmed the presence of phenolics in considerable concentrations in Caesalpinia bonduc extract. Administration of different doses (250 and 500 mg/kg) of CPP extract to hyperglycemic rats for 8 weeks restored blood and serum glucose, insulin, glycosylated hemoglobin, leptin, amylin, and carbohydrate metabolizing enzymes level towards normal compared to alloxanized diabetic group. The effect of CPP extract on various genes such as Pdx-1, Ins-1, ngn-3, GLUT-4, and IRS-1 in insulin signaling pathway and Traf-4, Traf-6, and Mapk-8 in MAPK downstream JNK cascade was examined through qRT-PCR to access the core molecular mechanism involved in CPP-induced recovery of diabetes. Results have revealed that CPP extract reduced oxidative stress in pancreatic β cells by restoring free radical scavenging potential, reducing the mRNA expression of Mapk-8, Traf-4, and Traf-6, and increasing the Pdx-1, Ins-1, ngn-3, GLUT-4, and IRS-1 expression ensuing regeneration of β cells and subsequent insulin release from pancreas. The results obtained in this study recommend that CPP extract may be a promising therapeutic restorative agent in the treatment of diabetes mellitus., Competing Interests: The authors declare no conflict of interest., (Copyright © 2020 Asra Iftikhar et al.)

In this paper, chemical investigation on the chloroform soluble fraction of seed kernels of Caesalpinia bonduc resulted in the isolation of five new cassane diterpenoids: norcaesalpinin O (1), norcaesalpinin P (2), caesalpinin MQ (3), caesall O/P (4/5) and seven known compounds (6-12). Compounds structures were elucidated by 1 H NMR, 13 C NMR, 2D NMR, HR-MS and ECD (electronic circular dichroism) spectral analysis. The characters for new compounds with the presence of an aromatized C ring or demethyl group at C-17 position in the structures were found. By means of bioactive screenings, the inhibitory effect on type-4 phosphodiesterase (PDE4, the target protein of asthma disease) and nuclear factor-kappa B (NF-κB) expression were valued. Compound 1 was found to exhibit moderate inhibitory activity on PDE4 and much better binding affinity than other structures by docking studies for interaction analyzing. Compounds 6, 10 and 11 displayed considerable inhibitory strength against NF-κB expression with inhibitory ratio 48.6%, 42.9% and 37.1% at 10 µM, respectively. The isolation of cassane-type diterpenoids with anti-inflammation activity from C. bonduc implied that this plant might be a good source for anti-inflammation agents finding., Competing Interests: Declaration of Competing Interest The authors declared that there is no conflict of interest., (Copyright © 2020 Elsevier Inc. All rights reserved.)

Background: The dried heartwood of Caesalpinia sappan L. is traditionally prescribed in the formula of traditional Chinese medicine (TCM) for the treatment of acute myeloid leukemia (AML), while nothing is yet known of the active fractions and the underlying mechanisms., Purpose: This study aims to investigate the effect of the ethyl acetate extract of the dried heartwood of Caesalpinia sappan L. (C-A-E) on induction of apoptosis and promotion of differentiation in vitro and anti-AML activity in vivo., Study Design/methods: The aqueous extract was sequentially separated with solvents of increasing polarity and the active fraction was determined through the inhibition potency. The inhibition of the active fraction on cell viability, proliferation and colony formation was performed in different AML cells. Induction of apoptosis and the promotion of differentiation were further determined. Then, the level of the reactive oxygen species (ROS) and its potential role were assessed. Finally, anti-AML activity was evaluated in NOD/SCID mice., Results: C-A-E exhibited the highest inhibition on the cell viability of HL-60 cells. Meanwhile, C-A-E significantly suppressed the proliferation and the colony formation ability of HL-60 and Kasumi-1 cells. Moreover, C-A-E significantly induced the apoptosis, which was partially reversed by Z-VAD-FMK. C-A-E also reduced the level of mitochondrial membrane potential, promoted the release of cytochrome C, decreased the Bcl-2/Bax ratio, and promoted the cleavage of caspase-9 and -3. In addition, Mdivi-1 (mitochondrial fission blocker) remarkably reduced the apoptosis caused by C-A-E. Meanwhile, C-A-E also induced the expression of Mff and Fis1 and increased the location of Drp1 in mitochondria. Furthermore, C-A-E obviously promoted the differentiation of AML cells characterized by the typic morphological changes, the increased NBT positive cells, as well as the increased CD11b and CD14 levels. Notably, C-A-E significantly enhanced the intracellular ROS level. Moreimportantly, C-A-E-mediated apoptosis and differentiation of HL-60 cells was significantly mitigated by NAC. Additionally, C-A-E also exhibited an obvious anti-AML effect in NOD/SCID mice with the injection of HL-60 cells., Conclusions: C-A-E exhibited an inhibitory effect on AML cells by inducing mitochondrial apoptosis and promoting differentiation, both of which were highly correlated to the activation of ROS., Competing Interests: Declaration of Competing Interest The authors declare that there are no conflicts of interest., (Copyright © 2019 Elsevier GmbH. All rights reserved.)

Libidibia ferrea (juca) is a plant belonging to the Fabaceae (Leguminosae) family, whose antioxidant activity has been widely described in the literature. We evaluated this parameter of Aqueous ethanol extract (AE), ethyl acetate (ACO), chloroform (CLO) and hexane (HEX) extracts of L. ferrea. We then tested the most active extract for its toxicity and ability to inhibit migratory activity in the ACP02 gastric adenocarcinoma cell line in vitro. The AE and ACO extracts both had antioxidant activity, the AE extract showing greater potential. This may reflect that both extracts contained phenolic compounds. Although AE extract showed no cytotoxic, mutagenic or genotoxic effect, it altered cell morphology and migration activity. Analysis of apoptosis/necrosis indicated that this parameter does not appear to account for the apparent ability of AE to inhibit cancer cell migration. We speculate that the morphological changes in AE-treated cells could be due to cytoskeleton alterations related to the presence of myo-inositol in AE extract. Together, our results demonstrate this extract of L. ferrea can act as an exogenous antioxidant and might prove useful in efforts to fight secondary tumors., Competing Interests: The authors have declared that no competing interests exist.

Background: Cassane-type diterpenoids are widely distributed in the medical plants of genus Caesalpinia. To date, plenty of cassane diterpenoids have been isolated from the genus Caesalpinia, and some of them were documented to exhibit multiple biological activities. However, the effects of these compounds on autophagy have never been reported., Objective: To investigate the effects and mechanisms of the cassane diterpenoids including Phanginin R (PR) on autophagy in Non-Small Cell Lung Cancer (NSCLC) A549 cells., Methods: Western blot analysis and immunofluorescence assay were performed to investigate the effects of the compounds on autophagic flux in A549 cells. The pathway inhibitor and siRNA interference were used to investigate the mechanism of PR. MTT assay was performed to detect cell viability., Results: PR treatment upregulated the expression of phosphatidylethanolamine-modified microtubule-associated protein Light-Chain 3 (LC3-II) in A549 cells. Immunofluorescence assay showed that PR treatment increased the production of red-fluorescent puncta in mRFP-GFP-LC3 plasmid-transfected cells, indicating PR promoted autophagic flux in A549 cells. PR treatment activated the c-Jun N-terminal Kinase (JNK) signaling pathway while it did not affect the classical Akt/mammalian Target of Rapamycin (mTOR) pathway. Pretreatment with the JNK inhibitor SP600125 or siRNA targeting JNK or c-Jun suppressed PR-induced autophagy. In addition, cotreatment with the autophagy inhibitor Chloroquine (CQ) or inhibition of the JNK/c-Jun signaling pathway increased PR-induced cytotoxicity., Conclusion: PR induced cytoprotective autophagy in NSCLC A549 cells via the JNK/c-Jun signaling pathway, and autophagy inhibition could further improve the anti-cancer potential of PR., (Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.net.)

The extract of Caesalpinia pulcherrima (C. pulcherrima) is one of the common herbal drugs which have a key role in treating pyretic, microbial infections, cancer and for several other traditional systems of treatment. In our present work, we demonstrate the bioactivities of extracts and cytotoxicity of synthesized silver nanoparticles on HCT116 cell line. The qualitative phytochemical tests indicated the presence of some adequately required metabolites as follows; the total phenolic content in the aqueous extract contains a higher amount of phenolic compounds (815 ± 0.013 μgmg -1 ). The DPPH quenching activity of the aqueous extract showed an IC 50 value of 18.7 μg which was equivalent to the IC 50 value of ascorbic acid (15 μg) and methanolic extract (51 μg). The test extracts showed 4.6% haemolytic activity that attributes to its protective and non-toxic nature. The zone of inhibition of aqueous extract shown against the growth of E.coli was 25 mm. Further, silver nanoparticles synthesis was carried out with the extract and was characterized by X-ray diffraction, particle size analyzer, zeta potential, TEM- EDAX and UV spectroscopy. XRD analysis indicated the crystalline nature of silver nanoparticles with a face-centered cubic structure. The data obtained from the particle size analyzer demonstrated as 155.4 nm of the size of the synthesized silver nanoparticles. The values of zeta potential (-23.4 mV) revealed that the nanoparticles were extremely stable in colloidal form. SEM indicated the spherical shape of silver nanoparticles with the size range between 177.9 nm to 251.1 nm. Beside the efficient bioactivities, the synthesized C. pulcherrima silver nanoparticles showed significant cytotoxicity effect of 77.5% on a human colon cancer cell line. Therefore, along with antioxidant, antibacterial, haemolytic activity; C. pulcherrima also accomplished satisfactory cytotoxic property in anticancer mechanism as proven by this study., (Copyright © 2019 Elsevier B.V. All rights reserved.)

Three new compounds, (3S)-dihydrobonducellin 8-O-β-D-glucopyranoside (1), 3',5'-dimethoxy-jezonolid (2), and latisilinoid (3), along with 16 known compounds, were isolated from the twigs of Caesalpinia latisiliqua (Leguminosae). The known compounds were identified as flavonoids, stilbenes, and phenolics as determined by extensive spectroscopic methods, including 1D and 2D NMR. All the isolated compounds were evaluated for their antiviral activity in HRV1B-, CVB3-, and EV71-infected cells. Among the tested compounds, three flavonoids (4-6) and two stilbenes (12 and 14) exhibited significant antiviral activity. This is the first phytochemical investigation of C. latisiliqua twigs.

Galactomannans are neutral polysaccharides isolated from the endosperm of some Leguminosae seeds. They consist of a (1 → 4) linked β-mannopyranosyl backbone partially substituted at O-6 with α-d-galactopyranosyl side groups. C. pulcherrima have anti-inflammatory and muco-adhesive proprieties. Acute gastritis is an inflammatory disease triggered by use of non-steroidal anti-inflammatory drugs. We investigated the gastroprotective effect of galactomannan obtained from the seeds of Caesalpinia pulcherrima L. (GM-CP) in acute gastritis model induced by indomethacin. Gastritis was induced with indomethacin (30 mg/kg, P.·O.) in female Swiss mice. Animal groups (n = 7) were pretreated with saline-dissolved GM-CP (3 mg/kg, 10 mg/kg, 30 mg/kg, P.O.) or vehicle 1 h before gastritis induction. Mice were euthanized seven hours after the induction. The stomach and blood samples were collected for analysis. At 10 mg/kg, GP-CP reduced the extension of macroscopic lesion and the loss of superficial cells by alleviating inflammatory symptoms (neutrophil infiltration, migration and adhesion of mesenteric leukocytes, production of TNF-α and thiobarbituric acid reactive species (TBARS) and helping to maintain mucin labeling of the tissue. Thus, the findings of the study suggest that GM-CP exhibits gastroprotective effects., (Copyright © 2019 Elsevier B.V. All rights reserved.)

Antimicrobial resistance has been increasing in recent years and is most frequently found in pathogenic microorganisms resistant or multiresistant to drugs. The secondary metabolites of plants have been evaluated as alternatives for control and treatment of these microorganisms. The aim of this study was to isolate and identify the secondary metabolites with antibacterial activity from Caesalpinia coriaria (Jacq) Willd fruit. Hydroalcoholic extract (CCHA), was subjected to a bipartition with ethyl acetate giving two fractions an aqueous (Aq-F) and an organic (EtOAc-F). The isolation of bioactive fraction (EtOAc-F) allowed obtain two important compounds, methyl gallate (1) and gallic acid (2). These compounds were identified by high-performance liquid chromatography (HPLC) and nuclear magnetic resonance (NMR). The CCHA, both fractions and the isolated compounds were evaluated in vitro to determine their Minimal Inhibitory Concentration (MIC) and Minimal Bactericidal Concentration (MBC) against Escherichia coli, Pseudomonas aeruginosa, Salmonella typhi, Listeria monocytogenes and Staphylococcus aureus. Gallic acid (2) showed the lowest MIC on S. typhi, (0.156 mg/mL), L. monocytogenes and S. aureus (1.25 mg/mL), while methyl gallate (1) had the best inhibitory effect against E. coli and P. aeruginosa (1.25 mg/mL). On the other hand, methyl gallate (1) showed the best MBC on P. aeruginosa (2.50 mg/mL), and gallic acid (2) had the lowest MBC on P. aeruginosa and L. monocytogenes. In conclusion, methyl gallate (1) and gallic acid (2) are the compounds responsible for the antibacterial activity of Caesalpinia coriaria fruit., (Copyright © 2019 Elsevier Ltd. All rights reserved.)

Objective: The objective of the work was to optimize the extraction conditions of Caesalpinia sappan L. heartwood in order to maximize the brazilin content and antibacterial activity of the extract., Methods: Two independent factors were studied: extraction temperature (45-95 °C) and extraction time (30-60 min). In addition, five dependent factors were monitored, including extraction yield, brazilin content, and clear zones against Staphylococcus aureus TISTR 1466, Staphylococcus epidermidis TISTR 518 and Propionibacterium acnes DMST 14961. The brazilin content was quantified by high-performance liquid chromatography and antibacterial activity was determined by disk diffusion assay., Results: The high temperature provided high total extract yield as well as brazilin content, while extraction time had little effect on yield or brazilin content. Extraction time had a positive effect, while extraction temperature had little effect on clear zone against S. aureus. The largest clear zone against S. epidermidis was achieved at low extraction temperature and long extraction time. Conversely, short extraction time and high extraction temperature provided the largest clear zone against P. acnes. The optimal conditions providing the highest brazilin content was an extraction temperature and extraction time of 95 °C and 30 min, respectively. The same optimal conditions also provided the simultaneous greatest antibacterial activity against the three bacteria. Modeled optimal conditions were validated be conducting extraction using these values. Yield and antibacterial activity of the resulting extract demonstrated that the model had a low percentage error., Conclusion: The optimal condition will be used as a standard condition for extraction of C. sappan heartwood to maximize brazilin content and antibacterial activity., (Copyright © 2019 Shanghai Changhai Hospital. Published by Elsevier B.V. All rights reserved.)

Carboxymethyl tara gum (CMTG) was synthesized from the reaction between tara gum (TG) and monochloroacetic acid (MCA) in the presence of sodium hydroxide. The modification reaction was optimized in terms of the MCA/NaOH ratio, reaction time and temperature evaluated for degree of substitution (DS). The etherification was confirmed by FTIR and 13 C NMR spectroscopy, and it was characterized by different analyses. After carboxymethylation, CMTG showed new bonds at 1592, 1413 and 1320 cm -1 by FTIR and a new peak at δ = 178 ppm by 13 C NMR in response to the insertion of the carbonyl group. The microscopy showed higher degradation on the surface of the CMTG particles, and XRD indicated low crystallinity of the CMTG. Static light scattering demonstrated a reduction in the molar mass of tara gum after carboxymethylation. Thermal analysis (TGA and DSC) revealed a lower thermal stability of carboxymethylated gum compared to that of unmodified gum. Despite the insertion of negative charges demonstrated by the potential-zeta, CMTG and TG presented pseudoplastic behavior according to the rheological analyses, and CMTG presented lower viscosity at the concentrations that were studied., (Copyright © 2019 Elsevier B.V. All rights reserved.)

Background: Caesalpinia mimosoides, a vegetable consumed in Thailand, has been reported to exhibit in vitro antioxidant properties. The in vivo antioxidant and anti-aging activities have not been investigated. The aim of this research was to study the antioxidant activity of C. mimosoides extracts in Caenorhabditis elegans, a widely used model organism in this context., Methods: C. elegans were treated with C. mimosoides extracts in a various concentrations. To investigate the protective effects of the extract against oxidative stress, wild-type N2 were used to determine survival rate under oxidative stress and intracellular ROS. To study underlying mechanisms, the mutant strains with GFP reporter gene including TJ356, CF1553, EU1 and LD4 were used to study DAF-16, SOD-3, SKN-1 and GST-4 gene, respectively. Lifespan and aging pigment of the worms were also investigated., Results: A leaf extract of C. mimosoides improved resistance to oxidative stress and reduced intracellular ROS accumulation in nematodes. The antioxidant effects were mediated through the DAF-16/FOXO pathway and SOD-3 expression, whereas the expression of SKN-1 and GST-4 were not altered. The extract also prolonged lifespan and decreased aging pigments, while the body length and brood size of the worms were not affected by the extract, indicating low toxicity and excluding dietary restriction., Conclusions: The results of this study establish the antioxidant activity of C. mimosoides extract in vivo and suggest its potential as a dietary supplement and alternative medicine to defend against oxidative stress and aging, which should be investigated in intervention studies.

Cassane diterpenoids (CAs), recognized as main constituents of many medical plants of the genus Caesalpinia, exhibit diverse bioactivities, including anti-inflammatory and immunomodulatory activity, and also showed a therapeutic effect on rheumatoid arthritis (RA) according to previous work, including ours. In this study, 102 CA compounds were selected to explore the possible molecular mechanism of this class of natural products on anti-inflammatory and immunomodulatory activity using RA as a disease model through a series of in silico methods: chemical-similarity-based target prediction, molecular docking, and molecular dynamics (MD) simulation. As a consequence, four signaling pathways (TCR signaling pathway, TLR signaling pathway, VEGF signaling pathway, and osteoclast differentiation pathway) by which CAs exert their effect on inflammation and immunomodulation were identified. Furthermore, the binding modes of CAs complexing with several crucial targets, which were picked out by credible docking results and took part in these signaling pathways, were explored by MD simulations. This is the first time that the molecular mechanism of the anti-RA activity of natural CAs has been investigated with in silico methods, and these findings might explain the activity of CAs on anti-inflammation and immunomodulation, which could supply a valuable reference for drug design research on CAs.

Gastrointestinal nematodes (GIN) are responsible for enormous economic losses worldwide. The use of anthelmintic drugs reduces the parasitic burden in ruminants. However, the excessive use of these drugs triggers anthelmintic resistance in these parasites, which leads to a worrisome inefficacy of most of the commercially available antiparasitic drugs. Caesalpinia coriaria is an arboreal legume possessing medical properties, although the antiparasitic potential of this plant against animal parasitic nematodes has not yet been studied. The aim of this study was to assess the in vitro ovicidal activity of a hydro-alcoholic extract (HA-E) from C. coriaria fruits against GIN and to identify the compounds responsible for this activity through an egg hatch inhibition (EHI) assay. GIN eggs obtained from cattle faeces were used in bio-guided assays. The HA-E was subjected to a liquid-liquid extraction using water and ethyl acetate to obtain two fractions, an organic fraction (EtOAc-F, 27% yield) and an aqueous (Aq-F, 73% yield) fraction. The chromatographic fractionation of the EtOAc-F (2 gr) was performed on a glass column packed with silica gel and eluted with dichloromethane/methanol with 10% ascending polarity. The bioactive compounds were analysed using high-performance liquid chromatography (HPLC) with UV detection, nuclear magnetic resonance (NMR) spectroscopy and mass spectroscopy (MS). The HA-E extract and the EtOAc-F showed ovicidal activity at a LC 50 of 0.92 and 0.16 mg/mL, respectively. A concentration-dependant effect was observed in both treatments. Chromatographic fractionation of the EtOAc-F, allowed for the isolation and characterisation of three important compounds: methyl gallate (1), gallic acid (2) and an unidentified compound (UC). The bioactive molecules (2 and UC) displayed an ovicidal activity close to 100% at 1 mg/mL concentration. The results of this work show that gallic acid (2) isolated from C. coriaria fruits is responsible for its ovicidal activity. The use of Caesalpinia coriaria could be explored in future studies as an environmentally-friendly alternative for the control of GIN in ruminants., (Copyright © 2019. Published by Elsevier Inc.)

Natural products, especially diterpenoids, are enriched with numerous compounds with a broad spectrum of therapeutic indications, suggesting that functional moieties serve as a core pharmacophore. Cassane diterpenoids (CAs), as the main and characteristic constituents of medical plants in the Caesalpinia genus, have been widely studied due to their bioactivities, and >450 compounds have been reported since the 1960s, including 283 compounds that have been reported in the past decade. There are five main types of structures for these compounds: tricyclic cassane diterpenoids with a fused furan ring (I) or butanolide lactone (II), tricyclic cassane diterpenoids (III), norcassane diterpenoids (IV), and other types (V). CAs derivatives have a wide range of biological properties, including anti-inflammatory, antimalarial, antitumour, antiviral, antimicrobial, antinociceptive, and antioxidant effects. This review highlights the role of the biosynthetic pathway, including those with abnormal skeletons, as well as advances in structure, pharmacological activities and primarily mechanisms of CAs obtained from the Caesalpinia genus. The findings herein provide new insights into the development of this kind of natural diterpenoids., (Copyright © 2019 Elsevier B.V. All rights reserved.)

Six previously undescribed cassane diterpenoids, named caesalminaxins O-T (1-6), together with 28 known compounds (7-34), were isolated from the seeds of Caesalpinia minax Hance. Their structures, including their absolute configurations were elucidated by extensive spectroscopic analysis, X-ray diffraction, and quantum chemical calculations. Among the undescribed diterpenoids, compound 6 that possessed an unusual enol group at C-7 with a highly deshielded 1 H NMR signal was the first example in cassane diterpenoids. All of the isolates were evaluated for their inhibitory activity against lipopolysaccharide-activated NO production in RAW264.7 cells. Compound 16 showed moderate inhibitory activity with an IC 50 value of 17.3 μM, which was more potent than the positive control (indomethacin, IC 50  = 29.7 μM)., (Copyright © 2019 Elsevier B.V. All rights reserved.)

Background: Libidibia ferrea (L. ferrea) has been used in folk medicine to treat several conditions and to prevent cancer. This study performed a chromatographic analysis of the crude aqueous extract of Libidibia ferrea (Mart. ex. Tul.) L.P. Queiroz (LfAE) leaves and evaluated its in vivo antioxidant and anti-inflammatory potential., Methods: Polyphenols present in LfAE were characterized by high performance liquid chromatography (HPLC). Anti-inflammatory activity was studied in an experimental model of zymosan-induced intra-articular inflammation, conducted in Wistar rats treated with LfAE at the doses of 100, 200 and 300 mg/kg by gavage. Synovial fluid was collected for global leukocyte count, for spectrocopical UV/VIS analysis of myeloperoxidase (MPO) activity, total glutathione and malondialdehyde (MDA), and for quantification of inflammatory cytokines IL1-β and TNF-α by enzyme-linked immunosorbent assay. Synovial membrane was collected for histological analysis. The level of statistical significance was p < 0.05., Results: HPLC detected concentrations of 1.56 (0.77) %m/m for ellagic acid and 1.20 (1.38) %m/m for gallic acid in LfAE leaves. Treatment with LfAE at all doses significantly decreased the leukocyte influx into the synovial fluid (p < 0.001) and myeloperoxidase activity (p < 0.001), an important marker of neutrophils. LfAE at doses of 100 (p < 0.05), 200 and 300 mg/kg (p < 0.001) also reduced the levels of MDA. LfAE at doses of 200 and 300 mg/kg significantly decreased the levels of IL-1β (p < 0.05) and TNF-α (p < 0.001). All doses of LfAE resulted in increased levels of total glutathione (p < 0.001). Histopathological findings confirmed a reduction of the inflammatory infiltrate in the rats treated with LfAE at a dose of 200 mg/kg (p < 0.05)., Conclusion: LfAE has an important anti-oxidant and anti-inflammatory effect on intra-articular inflammation.

Two new cassaine-type diterpenoids, namely erythrofordins D (1) and E (2), sourced from a Cameroon collection of Erythrophleum suaveolens were isolated and assessed for anti-tumor activity. In the NCI-60 cancer cell assay, erythrofordins D (1) and E (2) were found to be cytotoxic in the low micro molar ranges with a mean GI 50 value of 2.45 and 0.71 µM, mean TGI value of 9.77 and 2.29 µM, and a mean LC 50 of 26.92 and 11.48 µM for 1 and 2 respectively. Using the COMPARE algorithm, the new compounds were found to have similar NCI-60 response profiles to the known cardiac glycosides hyrcanoside and strophanthin. In addition, in an assay examining the viability and contractile function in human cardiomyocytes derived from induced pluripotent stem-cells, erythrofordins showed cardiotoxicity effects at concentrations as low as 0.03 µg/mL., (Copyright © 2018 Elsevier Ltd. All rights reserved.)

A polysaccharide characterized as galactomannan (GMann) with a molecular weight of 117.76 kDa was isolated from the aqueous extract of Caesalpinia gilliesii (C. gilliesii) seeds then assessed for antiproliferative potential against human hepatocellular carcinoma cell line (HepG2). Further, HCC was induced in Wister albino rats by Diethylnitrosamine (DEN) ip injection (200 mg/kg bw), and CCl4 orally (2 ml/kg bw) for two months then subjected to GMann orally treatment (2 mg/kg bw) for one month. In results, isolated GMann is constituted of sugars (89.99 ± 2.3%), moisture (6.89 ± 0.45%), ash (0.06 ± 0.2%), and protein (2.81%) and composed mainly of mannose and galactose in ratio M/G 3.79. In vitro study, data revealed a concentration-dependent potency of GMann to induce cell death of HepG2 cells with IC 50 value of 0.375 µg/ml. Mechanistic studies revealed the potential of GMann to arrest cell cycle at G2/M phase with induction of apoptosis. Biochemical results in vivo showed a significant reduction in serum transaminases (ALT and AST) as well as hepatic malondialdehyde (MDA) and nitric oxide (NOx). Molecular analysis declared a significant down-regulation in mRNA gene expression of both nuclear factor kappa-B (NF-κB) and tumor necrosis factor (TNF-α). Furthermore, a significant down-regulation in the cellular oncogene-fos (C-fos) and marked up-regulation in Glycogen synthase kinase-3 (GSK-3β) level were observed. These results were supported with histopathological investigation. Whereas GMann improved inflammatory and apoptotic markers, it could be a promising new therapeutic agent for HCC suppression and this warrant further development as a possible drug candidate for HCC.

A hitherto unknown polyoxygenated flavonol robinobioside (gossypetin-3- O - β -d-robinobioside) was isolated from the leaves of Caesalpinia gilliesii along with thirteen known phenolic secondary metabolites. The isolated compounds were characterized using spectroscopic analysis, including 1D and 2D NMR and mass spectrometry (MS) analyses. The extract reduced the level of liver damage in CCl₄-induced liver injury in rats. A decrease of the liver biomarkers-aspartate aminotransferase (AST) and alanine aminotransferase (ALT) and an increase of total antioxidant capacity (TAC) levels-were observed similar to the liver protecting drug silymarin. In addition, the extract showed promising activity against carrageenan-induced paw edema in rats and protected their stomachs against ethanol-induced gastric ulcers in a concentration dependent fashion. The observed activities could be attributed to the high content of antioxidant polyphenols. Our results suggest that the C. gilliesii has the capacity to scavenge free radicals and can protect against oxidative stress, and liver and stomach injury.

Saraca asoca (Roxb.) De Wilde (Caesalpiniaceae) is a highly traded IUCN red listed tree species used in Ayurvedic medicines for the treatment of various disorders, especially gynaecological problems. However, information about the genetic variations between populations and corresponding variation in specialized metabolites of S. asoca remains unclear. To address this issue, we analysed 11 populations of S. asoca with 106 accessions collected from Western Ghats of India using ISSR markers along with selected phytocompounds using RP-HPLC. Twenty primers were screened, out of which seven were selected for further analysis based on generation of clear polymorphic banding patterns. These seven ISSR primers produced 74 polymorphic loci. AMOVA showed 43% genetic variation within populations and 57% among the populations of S. asoca. To estimate the genetic relationships among S. asoca populations, UPGMA and Bayesian Models were constructed, which revealed two clusters of similar grouping patterns. However, excluding minor deviations, UPGMA and dissimilarity analysis showed close association of genotypes according to their geographical locations. Catechin (CAT), epicatechin (EPI) and gallic acid (GA) were quantified from bark and leaf samples of corresponding genotypes collected from 106 accessions. ROC plots depicted the sensitivity and specificity of the concentrations of tested phytocompounds at various cut-off points. Although, multiple logistic regression analysis predicted some association between few loci with GA, EPI and CAT, but PCA for phytochemical data failed to distinguish the populations. Overall, there were no significant trends observed to distinguish the populations based on these phytocompounds. Furthermore, the study advocates the delineate provenance regions of S. asoca genotypes/chemotype snapshots for in-situ conservation and ex-situ cultivation., (Copyright © 2018 Elsevier Ltd. All rights reserved.)

Seven undescribed hydroxylated cassane-type furanoditerpenoids were isolated from pupal cases formed from the secretion/excretion of the larvae of the wild bruchid seed beetle Sulcobruchus sauteri in infested Caesalpinia decapetala seeds, and their structures were elucidated by interpreting their spectra. The hydroxylated furanoditerpenoids found in the pupal cases were not present in the seeds of the host plant. Caesalacetal and caesaljapin obtained from the intact seeds exhibited larvicidal activity against the larvae of Aedes albopictus, while the hydroxylated furanoditerpenoids isolated from the pupal cases were inactive. The larvae of S. sauteri are proposed to detoxify larvicidal diterpenoids that occur in the seeds of the host plant by regiospecific hydroxylation., (Copyright © 2018 Elsevier Ltd. All rights reserved.)

Crude seed coat extracts from Abrus precatorius and Caesalpinia crista were purified into four different fractions namely phenolic acids, flavonols, flavanols and anthocyanin which were then examined for their polyphenol contents and antimicrobial potentials. The fractions derived from seed coat of A. precatorius were found more potent with high phenolic and flavonoid contents as compared to C. crista fractions. The significant antibacterial activity was observed against all strain tested by the fractions of both samples apart from anthocyanin fraction. It was interesting to note that the phenolic acid fractions of both samples was found more active against gram-negative bacteria, while gram-positive bacteria were found to be more sensitive towards flavonol fractions. The phenolic acid and flavonol fractions being potent antibacterial were selected to demonstrate the antifungal capacity of two samples. Among them, phenolic acid fraction of both samples was found active towards all the fungal strain.

The aim of this study was to evaluate the in vitro lethal effect of a methanolic extract (ME) from Caesalpinia coriaria fruits against Haemonchus contortus eggs and infective larvae. The anthelmintic activity was assessed using the egg hatching inhibition assay (EHI) and the mortality test. The ME was assessed using five concentrations as follows: 6.15, 3.12, 1.56, and 0.78 mg/mL to eggs and 150, 100, 75, and 50 mg/mL to larvae, respectively. Ivermectin (5 mg/mL) was used as positive control and 4% methanol and distilled water were used as negative controls. The data of ovicidal and larvicidal effect were analyzed with a completely randomized design through ANOVA analysis using the general linear model (GLM) and lethal concentrations (LC 50 and LC 90 ) were estimated through a Probit analysis using the SAS program. A clear ME increased concentration dependence effect was observed in the EHI and mortality tests. The highest activity of the methanolic extract was observed at the highest concentration (P < 0.05) to obtain a similar effect to the positive control (ivermectin), with LC 50 = 78.38 and 0.00064 mg/mL and LC 90 =235.63 and 0.024 mg/mL, respectively, for larvae and eggs. The results indicate that the C. coriaria fruit ME possesses in vitro ovicidal and larvicidal properties (gallotannins: methyl gallate) against H. contortus that needs to be investigated more in vivo for the control of gastroenteric nematodes in ruminants.

Ethnopharmacological Relevance: Seed kernel of the plant Ceasalpinia bonducella Linn (Caesalpiniacaeae) are used for the treatment of asthma in folk medicine and ancient books., Aim of Study: To assess the pharmacological efficacy of the plant in asthma and to confine and describe the synthetic constituents from the seeds that are in charge of the action., Material and Methods: The viability of petroleum ether, ethanol extract and ethyl acetate fraction from ethanol extract of C. bonducella seeds were screened for the treatment of asthma by various methods viz. effect of test drug on clonidine and haloperidol induced catalepsy, milk-induced leukocytosis and eosinophilia, mast cell stabilizing activity in mice and studies on smooth muscle preparation of guinea pig ileum (in-vitro). Column chromatography of active extract was done to pinpoint the active compound followed by structure elucidation by FTIR, GCMS and NMR spectroscopic methods., Results: Ethyl acetate fraction from ethanol extract of C. bonducella seeds exhibited antihistaminic activity at the dose of 50 and 100 mg/kg, inhibited clonidine-induced catalepsy but not haloperidol-induced catalepsy. Ethyl acetate fraction from ethanol extract significantly inhibited increased leukocyte and eosinophil count due to milk allergen and showed maximum protection against mast cell degranulation by clonidine. The results of guinea pig ileum indicated that the compound 2 methyl, 1 hexadecanol isolated from ethyl acetate fraction of ethanol extract relaxed significantly the ileum muscle strips pre-contracted by which suggests the involvement of β 2 -agonists on the relaxation of the tissue. All the results are dose dependent. Active ethyl acetate fraction from ethanol extract showed presence of anti-asthmatic compound, 2-methyl, 1-hexadecanol., Conclusion: The ethyl acetate fraction from ethanol extract of seeds of the plant C. bonducella can inhibit parameters linked to asthma disease., (Copyright © 2017 Elsevier B.V. All rights reserved.)

Two new cassane ditepenoid lactams, caesmimotam A (1) and B (2), along with eight known compounds (3-10) were isolated from the fruits of Caesalpinia mimosoides Lam. Their structures were identified by 1D and 2D NMR spectral data. Compounds 1 and 2 were evaluated for their cytotoxicity on HL-60, SMMC-7721, A-549, MCF-7 and SW-480 human cancer cell lines, but they were inactive.

Four fractions were prepared from the crude extract of Caesalpinia minax Hance and the inhibitory activity of nitric oxide (NO) production release of RAW 264.7 cells stimulated by lipopolysaccharide (LPS) was evaluated. The ethyl acetate (EtOAc) fraction showed obvious inhibitory effect. Bioassay-guided fractionation led to the isolation of three new cassane diterpenes, caesalmin X (1), caesalmin Y (2) and caesalmin Z (3), together with 19 known cassane diterpenoids (4-22). Their structures were mainly characterised on the basis of extensive spectroscopic analyses and comparison with reported data. Moreover, three compounds (20-22) which possessed furanditerpenoid 7,17-lactone structures, displayed moderate activities, with IC 50 value of 29.85, 27.38 and 25.40 μM, respectively.

A new compound 1 was isolated from the methanolic extract of the stems of the Caesalpinia pulcherrima Linn. along with a reported compound (2) 3-O-β-D-glucopyranosyl-(1→4)-β-D-xylopyranosyl-(1→3)-α-L-rhamnopyranosyl-(1→2)-α-L-arabinopyranosyl hederagenin 28-O-β-D-glucopyranosyl-(1→6)-β-D-glucopyranosyl ester. The new compound 1 has m.p. 272-274°C, m.f. C 46 H 74 O 17 , [M] + m/z 898. It was characterised as 3-O-β-D-glucopyranosyl-(1→4)-α-L-arabinopyranosyl hederagenin 28-O-β-D- xylopyranosyl ester by various colour reactions, chemical degradations and spectral analyses. Antibacterial activity of compound 1 was screened against various Gram-positive and Gram-negative bacteria and showed significant results.

Caesalpinia sappan L., belonging to the family Leguminosae, is a medicinal plant that is distributed in Southeast Asia. The dried heartwood of this plant is used as a traditional ingredient of food, red dyes, and folk medicines in the treatment of diarrhea, dysentery, tuberculosis, skin infections, and inflammation. Brazilin is the major active compound, which has exhibited various pharmacological effects, including anti-platelet activity, anti-hepatotoxicity, induction of immunological tolerance, and anti-inflammatory and antioxidant activities. The present study aimed to evaluate the antioxidant activity and expression of antioxidant enzymes of C. sappan L. extract and its major compound, brazilin, in human epidermal keratinocytes exposed to UVA irradiation. Our results indicated that C. sappan L. extract reduced UVA-induced H 2 O 2 production via GPX7 activation. Moreover, brazilin exhibited antioxidant effects that were similar to those of C. sappan L. via glutathione peroxidase 7 (GPX7), suggesting that C. sappan L. extract and its natural compound represent potential treatments for oxidative stress-induced photoaging of skin., (Copyright © 2018 China Pharmaceutical University. Published by Elsevier B.V. All rights reserved.)

To evaluate phenolic compounds and whether the combination of a tanniferous fruit and soybean oil could improve the performance, meat characteristics, and fatty acid (FA) profile in lambs, an experiment was conducted over 40 days with twenty creole male lambs (23.71 ± 3.46 kg). The lambs were allotted in a completely randomised design, with factorial arrangement 2 × 2, with the following dietary treatments: (1) control diet, (2) 2% Caesalpinia coriaria ground fruit dry matter (DM), (3) 2% soybean oil DM, and (4) 2% Caesalpinia coriaria fruit plus 2% soybean oil. The concentration of condensed tannins (CT) in Caesalpinia coriacea was 21.71 g/kg DM. No interactions were detected ( P > 0.05) among soybean oil and Caesalpinia coriaria , and there were no differences in daily gain, intake, and feed conversion. Soybean oil reduced ( P < 0.05) DM digestibility (68.05 versus 59.56%). In fat from the longissimus thoracis et lumborum (LTL) muscle, only linoleic acid presented differences ( P < 0.05) between treatments. The combination of Caesalpinia coriacea fruit and soybean oil did not improve lamb performance at the included levels.

From the previous findings, the ethanolic fractionated extract of Caesalpinia sappan (F-EtOH) has high activity against Streptococcus mutans, the most severe cariogenic bacteria. The present study was aimed to isolate and identify the active compound of F-EtOH and compare its inhibitory activity against the biofilm of S. mutans as well as the cytotoxicity to oral fibroblast cells with F-EtOH. Compound isolation was done by column chromatography. The active compound was identified using liquid chromatography-mass spectrometry with electrospray ionization and nuclear magnetic resonance spectroscopy. It was found that the major compound of F-EtOH is brazilin. F-EtOH and brazilin were compared for inhibitory potential on the biofilms of three strains of S. mutans. The results exhibited that both F-EtOH and brazilin had potential on inhibiting biofilm formation and eradicating the preformed biofilms and their activity was dose dependent. F-EtOH showed significantly less toxic to normal periodontal ligament fibroblast than brazilin. At low concentration of 1- and 2-MBC, F-EtOH showed higher effective than brazilin. The results of our study suggest that the antibacterial activity of F-EtOH is according to the synergistic effects of the existing compounds including brazilin in F-EtOH.

Objective: The present investigation was undertaken to assess the hypoglycemic potential of ethanolic (ECB) and aqueous extracts (ACB) of root bark of Caesalpinia bonducella using various in vitro techniques., Method: The ethanolic and aqueous extracts of root bark of C. bonducella were studied for their effects on glucose adsorption capacity, in vitro glucose diffusion, in-vitro amylolysis kinetics and glucose transport across membrane of yeast cells., Result: It was observed that the extracts under study adsorbed glucose and the adsorption of glucose increased remarkably with an increase in glucose concentration. The results of amylolysis kinetic experimental model revealed that the rate of glucose diffusion was found to be increased with time from 30 to 180min and both the extracts demonstrated significant inhibitory effects on movement of glucose into external solution across dialysis membrane as compared to control. Also, the extracts under study promoted glucose uptake by the yeast cells. It was observed that the enhancement of glucose uptake was dependent on both the sample and glucose concentration. Ethanolic extract of C. bonducella extract exhibited significantly higher (P≤0.05) activity than the aqueous extract at all concentrations., Conclusion: The results of the study verified the hypoglycemic activity of the extracts of root bark of C. bonducella. However, the observed effects need to be confirmed by using different in vivo models and clinical trials for its effective utilization as a therapeutic agent in effective management of diabetes mellitus., (Copyright © 2017 Académie Nationale de Pharmacie. Published by Elsevier Masson SAS. All rights reserved.)

The aim of this study was to investigate the antioxidant activity of Caesalpinia sappan aqueous extract (CE) and its potential on synthesis of silver nanoparticles (AgNPs). The antioxidant activity of CE was investigated using ferric reducing antioxidant power (FRAP) assay and two radical scavenging methods using 2,20-azinobis-(3-ethylbenzothiazoline-6-sulfonic acid) diammonium salt (ABTS) and 1,1-diphenyl-2-picrylhydrazyl (DPPH) as free radicals. Silver nitrate (AgNO3) was used as precursor for the synthesis of AgNPs. Effects of AgNO3 concentration, reaction temperature, and duration of reaction were investigated. The obtained AgNPs was characterized using UV-Vis and photon correlation spectrophotometers. The antimicrobial activity of AgNPs was studied by means of diffusion method. The results from FRAP demonstrated that CE had high reducing property of 78.7 ± 2.4 mM Fe 2+ /mg. The trolox equivalent antioxidant capacity of CE determined by ABTS was 64.8 ± 4.2 µM/mg. The concentration of CE that can inhibit 50% of DPPH radicals (IC50) was 51.2 ± 3.2 µM. These results indicated that CE possesses strong antioxidant and reducing activities. The present study also showed that CE can act as reducing agent to produce AgNPs. The concentration of AgNO3, reaction temperature, and reaction time play an important role on the particles size and zeta potential of the obtained AgNPs. The antimicrobial activity of the AgNPs against Escherichia coli, Candida albicans, and Streptococcus mutants was stronger than against Staphylococcus aureus.

Caesalpinia pulcherrima flower extract mediated synthesis of silver nanoparticles was attempted in the present work including optimization of some procedure parameters. Characterization of synthesized silver nanoparticles was done by various spectral analyses. The size of synthesized silver nanoparticles was 12 nm and they were spherical in shape. The green synthesized silver nanoparticles were further evaluated for antimicrobial, antioxidant, cytotoxic, and genotoxic activities; they showed good antimicrobial, antioxidant, and cytotoxic effects. Genotoxic study revealed non-toxic nature at lower concentration. Overall results suggest that the synthesized silver nanoparticles have pronounced applicability in pharmaceutical and biomedical field.

One new cassane diterpene possessing an unusual N bridge between C-19 and C-20 named caesalsappanin R ( 1 ), as well as another new diterpene caesalsappanin S ( 2 ), were isolated from the seeds of Caesalpinia sappan with methanol extract. Their structures were determined by spectroscopic analysis and examined alongside existing data from prior studies. Their biological activities were profiled by their antiplasmodial activity., Competing Interests: There is no conflict of interest associated with the authors of this paper.

Seeds of tropical legumes posses a repertoire of proteinase inhibitors (PI) and the current study highlights some structural/functional features of a strong serine PI from the seeds of Caesalpinia bonduc (CbTI-2). Following purification, N-terminal sequence of CbTI-2 revealed over 40% similarity with a few serine PIs of Caesalpinioideae subfamily. Upon exposure to metal ions and ionic/non ionic surfactants, CbTI-2 showed immense variation in the levels of antitryptic activity. Exposure of CbTI-2 to 1,4-Dithiothreitol, Guanidinium HCl, H 2 O 2 and Dimethyl sulfoxide led to a steady loss of inhibitory activity. Chemical modification of amino acids suggested an arginine as the active site residue. Circular Dichroism spectrum of native CbTI-2 revealed an unordered state. Secondary structure composition of CbTI-2 following exposure to extreme conditions (heat, acidic/alkaline environment, Guanidine hydrochloride and DTT) showed considerable perturbations that caused severe loss of antiproteolytic activity. DLS studies yielded a hydrodynamic radius of ∼2.2nm for CbTI-2 and also reconfirmed 1:1 stoichiometry for the trypsin-CbTI-2 complex. Initial studies indicated CbTI-2 to be a potent antiplasmodial agent by being highly toxic towards growth, schizont rupture process and erythrocytic invasion of Plasmodium falciparum., (Copyright © 2017 Elsevier B.V. All rights reserved.)

Responsible for nearly 1.5 million deaths every year, the infectious disease tuberculosis remains one of the most serious challenges to global health. The emergence of multidrug-resistant tuberculosis and, more recently, extensively drug-resistant tuberculosis poses a significant threat in our effort to control this epidemic. New drugs are urgently needed to combat the growing threat of antimicrobial resistance. To achieve this goal, we screened approximately 500 species of medicinal plant methanol extracts and their solvent partitioned fractions for potential inhibitors of Mycobacterium tuberculosis growth. Using microdilution screening, the ethyl acetate solvent partitioned fraction from the heartwood of Caesalpinia sappan exhibited strong antitubercular activity. We isolated the active compound and identified it as 3-deoxysappanchalcone. The extracted 3-deoxysappanchalcone possessed activity against both drug-susceptible and drug-resistant strains of M. tuberculosis at MIC 50 s of 3.125-12.5 μg/mL in culture broth and MIC 50 s of 6.25-12.5 μg/mL inside macrophages and pneumocytes. 3-Deoxysappanchalcone was also found to act in partial synergy with streptomycin/ethambutol against M. tuberculosis H37Rv. 3-Deoxysappanchalcone had no cytotoxicity against the A549 cell line up to a concentration of 100 μg/mL (selectivity index > 8-32). Further studies are warranted to establish the in vivo effect and therapeutic potential of 3-deoxysappanchalcone. Copyright © 2017 John Wiley & Sons, Ltd., (Copyright © 2017 John Wiley & Sons, Ltd.)

This study contributes to the continual discovery of lifespan-extending compounds from plants, using the Caenorhabditis elegans model system. An ethyl acetate soluble fraction of methanol extract from the heartwood of Caesalpinia sappan showed a significant lifespan-extending activity. Subsequent activity-guided chromatography of the ethyl acetate-soluble fraction led to the isolation of brazilin. Brazilin showed potent 2,2-diphenyl-1-picrylhydrazyl radical scavenging and superoxide anion quenching activities and also revealed a lifespan-extending activity in C. elegans under normal culture conditions. Brazilin also exhibited the protective effects against thermal, oxidative and osmotic stress conditions to improve the survival rate of the nematode. Furthermore, brazilin elevated superoxide dismutase (SOD) activity and decreased intracellular reactive oxygen species accumulation in C. elegans. Further studies showed that brazilin-mediated increased stress tolerance of worms could be due to increased expressions of stress resistance proteins such as heat shock protein (HSP-16.2) and superoxide dismutase (SOD-3). Besides, there were no significant, brazilin-induced changes in aging-related factors, including progeny production, food intake, and growth, indicating brazilin influences longevity activity independent of affecting these factors. Brazilin increased the body movement of aged worms, indicating brazilin affects the healthspan and lifespan of nematode. These results suggest that brazilin contributes to the lifespan of C. elegans under both normal and stress conditions by increasing the expressions of stress resistance proteins.

Ethnopharmacological Relevance: Decoctions of the leaves of M. benthamianum Baill. are used by traditional healers in Guinea to treat malaria and this use was validated by a preliminary clinical assay., Aim of the Study: To evaluate the in vitro antiplasmodial activity and to identify active compounds from extracts of M. benthamianum leaves., Material and Methods: Antiplasmodial activity of extracts, fractions and pure compounds was evaluated in vitro against a chloroquine-sensitive strain of Plasmodium falciparum (3D7) using the measurement of the plasmodial lactate dehydrogenase activity. Selectivity of extracts and purified compounds for Plasmodium parasites was evaluated by using WST-1 test on HeLa human cells. Compounds were isolated using normal phase silica gel column chromatography and prepHPLC and their structures elucidated using extensive spectroscopic analysis., Results: Hydroethanolic extracts (70% v/v) of M. benthamianum leaves showed a moderate in vitro activity against P. falciparum 3D7, with IC 50 in the range 22.5 - 32.6µg/mL, depending on the batch; while a dark precipitate formed during ethanol evaporation showed higher activity (IC 50 =6.5µg/mL). The fractionation was performed on this most active fraction and was followed by in vitro antiplasmodial assay. Active compounds (5, 7, 8) belong to several phytochemical classes, contributing together to the global antiplasmodial activity of the hydroethanolic extract against P. falciparum parasite. This study finally allowed the isolation of three diterpenes including two new compounds named Mezobenthamic acids A (1) and B (2) and neocaesalpin H (3), as well as quercetin (4), kaempferol (7), resveratrol (6), gallic acid (9) and its ethylester (5), β-sitosterol glucoside (10) and 13b-hydroxy-pheophorbide a (8)., Conclusion: This study gives some concrete evidence to support the ethnopharmacological use of Mezoneuron benthamianum leaves extract in the management of malaria. The active compounds can be further studied for their antiplasmodial potential, as well as their suitability to be used as quality markers for the standardization of this herbal drug from the Guinean traditional pharmacopeia., (Copyright © 2017 Elsevier Ireland Ltd. All rights reserved.)

Plant-derived natural products have been the highly significant sources of novel antitumor agents. The cassane-type diterpenes of genus Caesalpinia have been reported to bear antiproliferative activities toward different types of cancer cells. In this study, we evaluated the antineoplasmic activities of 16 natural origin cassane-type diterpenes isolated from the CHCl 3 extract of the seeds of C. minax in pituitary adenomas cells and identified caesalpin G (CAG) showed the strongest cytotoxicity. Moreover, we further investigated the structure-activity relationship and molecular mechanism of these derivatives systematically. The results confirmed the unsaturated lactone-type ring, hydroxyl at C-7, and alkenyl at C-11 or C-14 functionality as critical for anticancer activity in this family of natural products. In addition, the mechanism experiments also demonstrated unfolded protein response and ER stress and Wnt/β-catenin pathway were involved in the CAG-induced apoptosis.

Caesalpinia coriaria ( C. coriaria ), also named cascalote, has been known traditionally in México for having cicatrizing and inflammatory properties. Phytochemical reports on Caesalpinia species have identified a high content of phenolic compounds and shown antineoplastic effects against cancer cells. The aim of this study was to isolate and identify the active compounds of a water:acetone:ethanol (WAE) extract of C. coriaria pods and characterize their cytotoxic effect and cell death induction in different cancer cell lines. The compounds isolated and identified by chromatography and spectroscopic analysis were stigmasterol, ethyl gallate and gallic acid. Cytotoxic assays on cancer cells showed different ranges of activities. A differential effect on cell cycle progression was observed by flow cytometry. In particular, ethyl gallate and tannic acid induced G2/M phase cell cycle arrest and showed interesting effect on microtubule stabilization in Hep3B cells observed by immunofluorescence. The induction of apoptosis was characterized by morphological characteristic changes, and was supported by increases in the ratio of Bax/Bcl-2 expression and activation of caspase 3/7. This work constitutes the first phytochemical and cytotoxic study of C. coriaria and showed the action of its phenolic constituents on cell cycle, cell death and microtubules organization.

Ethno-Pharmacological Relevance: Pattanga is botanically equated as Caesalpinia sappan Linn. (Family: Caesalpiniaceae) and is used in Ayurveda system of medicine since ages. According to Ayurveda, useful part is Heartwood, which is bitter, astringent and acrid and is useful in vitiated conditions of vata and pitta, burning sensation, wounds, ulcers, leprosy, skin diseases, menorrhagia, leucorrhea, and diabetes. It is used as a major ingredient in Ayurvedic formulations and preparations like Patrangasava, Chandanadya Thalia, and Karpuradyarka., Aim of the Study: The present study is planned to evaluate the gastroprotective activity of the selected Ayurvedic drug using three different in vivo gastric ulcer models, so as to provide scientific evidence for the Ayurvedic claims., Materials and Methods: For this study, Wistar albino rats fasted overnight were selected. The hydroalcoholic extract of Caesalpinia sappan heartwood at the dose level 250 and 500mg/kg body weight was selected and administered orally before necrotizing agents. Antioxidant and antiulcer parameters were evaluated and the stomach samples were subjected for histopathological studies. In addition, PGE2 estimation and protein expressions of COX-1, COX-2 and iNOS were analyzed by Western blot. The plant extract was subjected to LCMS/MS analysis. In addition, Cytoprotective effect in isolated gastric mucosal cells, TUNEL Assay, Acid neutralizing capacity assay, H + /K + ATPase inhibitory assay were performed., Results: The ulcer protection was found to be 92%, 86% and 64% against ethanol, NSAID and pylorus ligation induced ulcer respectively. The hydro-alcoholic extract of C. sappan heartwood exhibited cytoprotective effect with 76.82% reduction against indomethacin-induced cytotoxicity at the concentration of 25µg/ml. C. sappan showed 63.91% inhibition in H + /K + ATPase inhibitory assay at the concentration 500µg/ml., Conclusions: Our results depict that Caesalpinia sappan heartwood possesses gastroprotective activity, possibly mediated through cytoprotection and antioxidant mechanisms. The data obtained in the present study provides scientific support for the traditional use of Caesalpinia sappan in the management of peptic ulcer., (Copyright © 2016 Elsevier Ireland Ltd. All rights reserved.)