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1.
Animals (Basel) ; 12(23)2022 Nov 26.
Artículo en Inglés | MEDLINE | ID: mdl-36496822

RESUMEN

Sexual intercourse in the animal kingdom functions to enable reproduction. However, we now know that several species of non-human primates regularly engage in sex outside of the times when conception is possible. In addition, homosexual and immature sex are not as uncommon as were once believed. This suggests that sex also has important functions outside of reproduction, yet these are rarely discussed in sex-related teaching and research activities concerning primate behaviour. Is the human sexual experience, which includes pleasure, dominance, and communication (among others) unique, or do other primates also share these experiences to any extent? If so, is there any way to measure them, or are they beyond the rigour of scientific objectivity? What would be the evolutionary implications if human-like sexual experiences were found amongst other animals too? We comment on the evidence provided by our close relatives, non-human primates, discuss the affective and social functions of sex, and suggest potential methods for measuring some of these experiences empirically. We hope that this piece may foster the discussion among academics and change the way we think about, teach and research primate sex.

2.
Cell Genom ; 2(6): None, 2022 Jun 08.
Artículo en Inglés | MEDLINE | ID: mdl-35711737

RESUMEN

Knowledge on the population history of endangered species is critical for conservation, but whole-genome data on chimpanzees (Pan troglodytes) is geographically sparse. Here, we produced the first non-invasive geolocalized catalog of genomic diversity by capturing chromosome 21 from 828 non-invasive samples collected at 48 sampling sites across Africa. The four recognized subspecies show clear genetic differentiation correlating with known barriers, while previously undescribed genetic exchange suggests that these have been permeable on a local scale. We obtained a detailed reconstruction of population stratification and fine-scale patterns of isolation, migration, and connectivity, including a comprehensive picture of admixture with bonobos (Pan paniscus). Unlike humans, chimpanzees did not experience extended episodes of long-distance migrations, which might have limited cultural transmission. Finally, based on local rare variation, we implement a fine-grained geolocalization approach demonstrating improved precision in determining the origin of confiscated chimpanzees.

3.
PLoS One ; 16(8): e0256654, 2021.
Artículo en Inglés | MEDLINE | ID: mdl-34428261

RESUMEN

As the number of female forest landowners (FFLs) in the United States continues to rise, there is an increasing need to understand the perceptions of stakeholder groups about opportunities and challenges faced by FFLs in the context of sustainable forestland management. This study utilizes the technique of SWOT-AHP (Strengths, Weaknesses, Opportunities, and Treats-Analytical Hierarchy Process) to understand the perceptions of four stakeholder groups (FFLs, private foresters, government representatives, and non-profits) in Georgia-a significant forestry state located in the Southern United States. Sixteen factors (four under each SWOT category) were selected through a comprehensive literature review and detailed interviews with individuals from the identified stakeholder groups. A survey was created using these factors that asked stakeholders to compare them in their respective SWOT categories. An additional survey was created for each stakeholder group where survey participants compared the highest-ranking factors in each SWOT category. We found that all stakeholder groups prioritized weaknesses over the other SWOT categories. Results showed a significant need for relevant educational outreach programs that cater specifically to FFLs. Additionally, researchers found a need to promote the interest of future generations in forestland management as all stakeholder groups felt that limited interest from future generations was the most important threat. This study will directly feed into regional, national, and international attempts to increase the participation of minority family forest landowners in sustainable forest management through integrated forest policy development.


Asunto(s)
Conservación de los Recursos Naturales , Participación de los Interesados/psicología , Femenino , Bosques , Georgia , Humanos , Entrevistas como Asunto , Formulación de Políticas , Encuestas y Cuestionarios
4.
Am J Primatol ; 83(10): e23320, 2021 10.
Artículo en Inglés | MEDLINE | ID: mdl-34402081

RESUMEN

Paleoclimate reconstructions have enhanced our understanding of how past climates have shaped present-day biodiversity. We hypothesize that the geographic extent of Pleistocene forest refugia and suitable habitat fluctuated significantly in time during the late Quaternary for chimpanzees (Pan troglodytes). Using bioclimatic variables representing monthly temperature and precipitation estimates, past human population density data, and an extensive database of georeferenced presence points, we built a model of changing habitat suitability for chimpanzees at fine spatio-temporal scales dating back to the Last Interglacial (120,000 BP). Our models cover a spatial resolution of 0.0467° (approximately 5.19 km2 grid cells) and a temporal resolution of between 1000 and 4000 years. Using our model, we mapped habitat stability over time using three approaches, comparing our modeled stability estimates to existing knowledge of Afrotropical refugia, as well as contemporary patterns of major keystone tropical food resources used by chimpanzees, figs (Moraceae), and palms (Arecacae). Results show habitat stability congruent with known glacial refugia across Africa, suggesting their extents may have been underestimated for chimpanzees, with potentially up to approximately 60,000 km2 of previously unrecognized glacial refugia. The refugia we highlight coincide with higher species richness for figs and palms. Our results provide spatio-temporally explicit insights into the role of refugia across the chimpanzee range, forming the empirical foundation for developing and testing hypotheses about behavioral, ecological, and genetic diversity with additional data. This methodology can be applied to other species and geographic areas when sufficient data are available.


Asunto(s)
Pan troglodytes , Refugio de Fauna , Animales , Biodiversidad , Clima , Ecosistema , Variación Genética , Filogeografía
5.
mSystems ; 6(3): e0126920, 2021 Jun 29.
Artículo en Inglés | MEDLINE | ID: mdl-34156289

RESUMEN

Understanding variation in host-associated microbial communities is important given the relevance of microbiomes to host physiology and health. Using 560 fecal samples collected from wild chimpanzees (Pan troglodytes) across their range, we assessed how geography, genetics, climate, vegetation, and diet relate to gut microbial community structure (prokaryotes, eukaryotic parasites) at multiple spatial scales. We observed a high degree of regional specificity in the microbiome composition, which was associated with host genetics, available plant foods, and potentially with cultural differences in tool use, which affect diet. Genetic differences drove community composition at large scales, while vegetation and potentially tool use drove within-region differences, likely due to their influence on diet. Unlike industrialized human populations in the United States, where regional differences in the gut microbiome are undetectable, chimpanzee gut microbiomes are far more variable across space, suggesting that technological developments have decoupled humans from their local environments, obscuring regional differences that could have been important during human evolution. IMPORTANCE Gut microbial communities are drivers of primate physiology and health, but the factors that influence the gut microbiome in wild primate populations remain largely undetermined. We report data from a continent-wide survey of wild chimpanzee gut microbiota and highlight the effects of genetics, vegetation, and potentially even tool use at different spatial scales on the chimpanzee gut microbiome, including bacteria, archaea, and eukaryotic parasites. Microbial community dissimilarity was strongly correlated with chimpanzee population genetic dissimilarity, and vegetation composition and consumption of algae, honey, nuts, and termites were potentially associated with additional divergence in microbial communities between sampling sites. Our results suggest that host genetics, geography, and climate play a far stronger role in structuring the gut microbiome in chimpanzees than in humans.

6.
Commun Biol ; 4(1): 283, 2021 03 05.
Artículo en Inglés | MEDLINE | ID: mdl-33674780

RESUMEN

Much like humans, chimpanzees occupy diverse habitats and exhibit extensive behavioural variability. However, chimpanzees are recognized as a discontinuous species, with four subspecies separated by historical geographic barriers. Nevertheless, their range-wide degree of genetic connectivity remains poorly resolved, mainly due to sampling limitations. By analyzing a geographically comprehensive sample set amplified at microsatellite markers that inform recent population history, we found that isolation by distance explains most of the range-wide genetic structure of chimpanzees. Furthermore, we did not identify spatial discontinuities corresponding with the recognized subspecies, suggesting that some of the subspecies-delineating geographic barriers were recently permeable to gene flow. Substantial range-wide genetic connectivity is consistent with the hypothesis that behavioural flexibility is a salient driver of chimpanzee responses to changing environmental conditions. Finally, our observation of strong local differentiation associated with recent anthropogenic pressures portends future loss of critical genetic diversity if habitat fragmentation and population isolation continue unabated.


Asunto(s)
Conducta Animal , Evolución Molecular , Variación Genética , Componentes Genómicos , Repeticiones de Microsatélite , Pan troglodytes/genética , Migración Animal , Animales , Ecosistema , Interacción Gen-Ambiente , Genética de Población , Pan troglodytes/psicología , Filogenia , Especificidad de la Especie
8.
Mol Ecol Resour ; 21(3): 745-761, 2021 Apr.
Artículo en Inglés | MEDLINE | ID: mdl-33217149

RESUMEN

Noninvasive samples as a source of DNA are gaining interest in genomic studies of endangered species. However, their complex nature and low endogenous DNA content hamper the recovery of good quality data. Target capture has become a productive method to enrich the endogenous fraction of noninvasive samples, such as faeces, but its sensitivity has not yet been extensively studied. Coping with faecal samples with an endogenous DNA content below 1% is a common problem when prior selection of samples from a large collection is not possible. However, samples classified as unfavourable for target capture sequencing might be the only representatives of unique specific geographical locations, or to answer the question of interest. To explore how library complexity may be increased without repeating DNA extractions and generating new libraries, in this study we captured the exome of 60 chimpanzees (Pan troglodytes) using faecal samples with very low proportions of endogenous content (<1%). Our results indicate that by performing additional hybridizations of the same libraries, the molecular complexity can be maintained to achieve higher coverage. Also, whenever possible, the starting DNA material for capture should be increased. Finally, we specifically calculated the sequencing effort needed to avoid exhausting the library complexity of enriched faecal samples with low endogenous DNA content. This study provides guidelines, schemes and tools for laboratories facing the challenges of working with noninvasive samples containing extremely low amounts of endogenous DNA.


Asunto(s)
Exoma , Genómica , Hibridación de Ácido Nucleico , Animales , Heces , Biblioteca de Genes , Secuenciación de Nucleótidos de Alto Rendimiento , Pan troglodytes/genética , Análisis de Secuencia de ADN
9.
Nat Commun ; 11(1): 4451, 2020 09 15.
Artículo en Inglés | MEDLINE | ID: mdl-32934202

RESUMEN

Large brains and behavioural innovation are positively correlated, species-specific traits, associated with the behavioural flexibility animals need for adapting to seasonal and unpredictable habitats. Similar ecological challenges would have been important drivers throughout human evolution. However, studies examining the influence of environmental variability on within-species behavioural diversity are lacking despite the critical assumption that population diversification precedes genetic divergence and speciation. Here, using a dataset of 144 wild chimpanzee (Pan troglodytes) communities, we show that chimpanzees exhibit greater behavioural diversity in environments with more variability - in both recent and historical timescales. Notably, distance from Pleistocene forest refugia is associated with the presence of a larger number of behavioural traits, including both tool and non-tool use behaviours. Since more than half of the behaviours investigated are also likely to be cultural, we suggest that environmental variability was a critical evolutionary force promoting the behavioural, as well as cultural diversification of great apes.


Asunto(s)
Conducta Animal , Pan troglodytes/psicología , Animales , Ecosistema , Ambiente , Femenino , Bosques , Masculino , Pan troglodytes/fisiología , Comportamiento del Uso de la Herramienta
11.
Nat Hum Behav ; 4(9): 910-916, 2020 09.
Artículo en Inglés | MEDLINE | ID: mdl-32451479

RESUMEN

Human ethnographic knowledge covers hundreds of societies, whereas chimpanzee ethnography encompasses at most 15 communities. Using termite fishing as a window into the richness of chimpanzee cultural diversity, we address a potential sampling bias with 39 additional communities across Africa. Previously, termite fishing was known from eight locations with two distinguishable techniques observed in only two communities. Here, we add nine termite-fishing communities not studied before, revealing 38 different technical elements, as well as community-specific combinations of three to seven elements. Thirty of those were not ecologically constrained, permitting the investigation of chimpanzee termite-fishing culture. The number and combination of elements shared among individuals were more similar within communities than between them, thus supporting community-majority conformity via social imitation. The variation in community-specific combinations of elements parallels cultural diversity in human greeting norms or chopstick etiquette. We suggest that termite fishing in wild chimpanzees shows some elements of cumulative cultural diversity.


Asunto(s)
Diversidad Cultural , Conducta Social , Animales , Pan troglodytes
12.
Science ; 363(6434): 1453-1455, 2019 Mar 29.
Artículo en Inglés | MEDLINE | ID: mdl-30846610

RESUMEN

Chimpanzees possess a large number of behavioral and cultural traits among nonhuman species. The "disturbance hypothesis" predicts that human impact depletes resources and disrupts social learning processes necessary for behavioral and cultural transmission. We used a dataset of 144 chimpanzee communities, with information on 31 behaviors, to show that chimpanzees inhabiting areas with high human impact have a mean probability of occurrence reduced by 88%, across all behaviors, compared to low-impact areas. This behavioral diversity loss was evident irrespective of the grouping or categorization of behaviors. Therefore, human impact may not only be associated with the loss of populations and genetic diversity, but also affects how animals behave. Our results support the view that "culturally significant units" should be integrated into wildlife conservation.


Asunto(s)
Conservación de los Recursos Naturales/métodos , Pan troglodytes/psicología , Conducta Social , Animales , Conjuntos de Datos como Asunto , Humanos
13.
J Ethnopharmacol ; 229: 233-245, 2019 Jan 30.
Artículo en Inglés | MEDLINE | ID: mdl-30336303

RESUMEN

ETHNOPHARMACOLOGICAL RELEVANCE: Rheumatoid arthritis (RA) is a chronic inflammatory and destructive joint disease that affects the worldwide population. Alpinia officinarum Hance (Zingiberaceae), rhizomes are widely used ethnobotanically as an anti-inflammatory, analgesic, and antioxidant agent in traditional medicine. AIM: To investigate the efficacy and possible mechanism of isolated phytoconstituent from the methanol extract of A. officinarum (MEAO) rhizomes against Freund's complete adjuvant (FCA)-induced arthritis in rats. Furthermore, molecular docking was performed to study the binding mode of this compound into the active site of TNF-α. MATERIALS AND METHODS: Diarylheptanoid was isolated from MEAO, well characterized (HPTLC, 1H NMR, 13C NMR, and ESI-MS) and evaluated for its antiarthritic activity in female Wistar rats (170-200 g). Diarylheptanoid (5, 10 and 20 mg/kg, p.o.) was administered starting from day 12. Various behavioral, biochemical, molecular and histopathology parameters were evaluated. Molecular docking study was performed using Glide module integrated into Schrodinger molecular modeling software. RESULTS: The structure and molecular weight of the isolated compound (diarylheptanoid) were confirmed by 1D and mass spectral data and characterized as 1-phenyl-5-hydroxy-7- (4''-hydroxy-3''-methoxyphenyl) heptane-3-one (i.e., 5-HPH) with molecular formula C20H24O4. Administration of 5-HPH (10 and 20 mg/kg) significantly inhibited (p < 0.05) FCA induced increases in paw volume, joint diameter, thermal hyperalgesia and tactile allodynia. It also significantly decreased oxido-inflammatory markers (SOD, GSH, MDA, and TNF-α). FCA induced a histological alteration in ankle joint also attenuated by 5-HPH. Its Glide docking score was found to be -9.702 with binding energy (Glide energy) of -37.033 kcal/mol. CONCLUSION: 5-HPH may exhibit its anti-arthritic potential via inhibition of elevated oxido-inflammatory markers thus restoring the elevated hyperalgesia, allodynia and reducing destruction in synovial membrane and cartilage. Therefore, 5-HPH is a potential moiety bearing antioxidant and with anti-inflammatory properties to inhibit FCA-induced arthritis in rats. The results of the present investigation should enable the design of potent small-molecule inhibitors that inactivate TNF-α with high affinity and specificity.


Asunto(s)
Alpinia , Antiinflamatorios/farmacología , Artritis Experimental/metabolismo , Diarilheptanoides/farmacología , Factor de Necrosis Tumoral alfa/metabolismo , Animales , Articulación del Tobillo/efectos de los fármacos , Articulación del Tobillo/patología , Antiinflamatorios/uso terapéutico , Artritis Experimental/tratamiento farmacológico , Artritis Experimental/patología , Diarilheptanoides/uso terapéutico , Femenino , Metanol/química , Simulación del Acoplamiento Molecular , Fitoterapia , Extractos Vegetales , Ratas Wistar , Solventes/química , Factor de Necrosis Tumoral alfa/sangre
14.
Am J Phys Anthropol ; 166(3): 510-529, 2018 07.
Artículo en Inglés | MEDLINE | ID: mdl-29989158

RESUMEN

OBJECTIVES: We investigated occurrences and patterns of terrestrial nocturnal activity in wild chimpanzees (Pan troglodytes) and modelled the influence of various ecological predictors on nocturnal activity. METHODS: Data were extracted from terrestrial camera-trap footage and ecological surveys from 22 chimpanzee study sites participating in the Pan African Programme: The Cultured Chimpanzee. We described videos demonstrating nocturnal activity, and we tested the effects of the percentage of forest, abundance of predators (lions, leopards and hyenas), abundance of large mammals (buffalos and elephants), average daily temperature, rainfall, human activity, and percent illumination on the probability of nocturnal activity. RESULTS: We found terrestrial nocturnal activity to occur at 18 of the 22 study sites, at an overall average proportion of 1.80% of total chimpanzee activity, and to occur during all hours of the night, but more frequently during twilight hours. We found a higher probability of nocturnal activity with lower levels of human activity, higher average daily temperature, and at sites with a larger percentage of forest. We found no effect of the abundance of predators and large mammals, rainfall, or moon illumination. DISCUSSION: Chimpanzee terrestrial nocturnal activity appears widespread yet infrequent, which suggests a consolidated sleeping pattern. Nocturnal activity may be driven by the stress of high daily temperatures and may be enabled at low levels of human activity. Human activity may exert a relatively greater influence on chimpanzee nocturnal behavior than predator presence. We suggest that chimpanzee nocturnal activity is flexible, enabling them to respond to changing environmental factors.


Asunto(s)
Conducta Animal/fisiología , Pan troglodytes/fisiología , Sueño/fisiología , Vigilia/fisiología , Animales , Antropología Física , Evolución Biológica , Ecosistema , Humanos , Temperatura
15.
Int Immunopharmacol ; 52: 110-118, 2017 Nov.
Artículo en Inglés | MEDLINE | ID: mdl-28888779

RESUMEN

BACKGROUND: Inflammation activated by oxidative stress can cause various diseases, such as asthma, rheumatoid arthritis, cancer, diabetes, etc. Plant constituents with sesquiterpene lactones possess antioxidant and anti-inflammatory properties. AIM: To determine the antioxidant and anti-inflammatory potential of isolated phytoconstituent from Cyathocline purpurea Buch-Ham ex D (CP). Don in laboratory animals. Furthermore, to understand the interactions involved in the binding of this compound to cyclooxygenase-2 (COX-2) via computational docking. METHODS: Phytoconstituent was isolated, purified and well characterized (using IR, NMR, and MS) from ethyl acetate fraction of CP methanolic extract. It was then evaluated for its in-vitro antioxidant activity against 1,1-diphenyl-2-picrylhydrazyl (DPPH), hydrogen peroxide (H2O2) and hydroxyl (OH) radical assays as well as in-vivo anti-inflammatory potential against carrageenan-induced paw edema model in rats. The molecular docking study was performed against the crystal structure of COX-2 to evaluate the binding potential of phytoconstituent towards this enzyme. RESULTS: The isolated compound 6α-hydroxy-4 [14], 10 [15]-guainadien-8α, 12-olide (HGN) showed significant (p<0.001) antioxidant activity with IC50 values of 76µg/mL. Administration of HGN (10 and 20mg/kg) significantly (p<0.001) reduced the increased paw volume after subplantar administration of carrageenan. It also exhibits good binding affinity towards with COX-2 with a docking score of -8.98 and Glide binding energy of -36.488kcal/mol shedding light on the potential mechanism of anti-inflammatory action. CONCLUSIONS: The presence of hydroxyl group in HGN provides a credential to its in-vivo anti-inflammatory and in-vitro antioxidant activities. Furthermore, the good binding affinity of HGN for the active site of COX-2 may open novel vistas in therapeutic option with natural antioxidants like Cyathocline purpurea to treat various inflammatory disorders.


Asunto(s)
Antiinflamatorios/uso terapéutico , Antioxidantes/uso terapéutico , Ciclooxigenasa 2/metabolismo , Edema/tratamiento farmacológico , Inflamación/tratamiento farmacológico , Fitoterapia/métodos , Sesquiterpenos de Guayano/uso terapéutico , Animales , Asteraceae/inmunología , Compuestos de Bifenilo/inmunología , Carragenina/toxicidad , Células Cultivadas , Edema/inducido químicamente , Femenino , Humanos , Peróxido de Hidrógeno/metabolismo , Masculino , Ratones , Estrés Oxidativo/efectos de los fármacos , Picratos/inmunología , Ratas , Ratas Wistar
16.
Sci Rep ; 6: 22219, 2016 Feb 29.
Artículo en Inglés | MEDLINE | ID: mdl-26923684

RESUMEN

The study of the archaeological remains of fossil hominins must rely on reconstructions to elucidate the behaviour that may have resulted in particular stone tools and their accumulation. Comparatively, stone tool use among living primates has illuminated behaviours that are also amenable to archaeological examination, permitting direct observations of the behaviour leading to artefacts and their assemblages to be incorporated. Here, we describe newly discovered stone tool-use behaviour and stone accumulation sites in wild chimpanzees reminiscent of human cairns. In addition to data from 17 mid- to long-term chimpanzee research sites, we sampled a further 34 Pan troglodytes communities. We found four populations in West Africa where chimpanzees habitually bang and throw rocks against trees, or toss them into tree cavities, resulting in conspicuous stone accumulations at these sites. This represents the first record of repeated observations of individual chimpanzees exhibiting stone tool use for a purpose other than extractive foraging at what appear to be targeted trees. The ritualized behavioural display and collection of artefacts at particular locations observed in chimpanzee accumulative stone throwing may have implications for the inferences that can be drawn from archaeological stone assemblages and the origins of ritual sites.


Asunto(s)
Conducta Animal , Pan troglodytes , África Occidental , Animales , Geografía
17.
Int Immunopharmacol ; 33: 8-17, 2016 Apr.
Artículo en Inglés | MEDLINE | ID: mdl-26849772

RESUMEN

BACKGROUND: Inflammation triggered by oxidative stress can cause various ailments, such as cancer, rheumatoid arthritis, asthma, diabetes etc. In the last few years, there has been a renewed interest in studying the antioxidant and anti-inflammatory action of plant constituents such as flavonoids and diarylheptanoids. AIM: To evaluate the antioxidant, anti-inflammatory activity and the total phenolic content of isolated compounds from Alpinia officinarum rhizomes. Furthermore, molecular docking was performed to study the binding mode of these compounds into the active site of cyclooxygenase-2 (COX-2). METHODS: A. officinarum rhizomes were extracted by maceration, using methanol. This extract was further fractionated by partitioning with hexane, chloroform and ethyl acetate and these fractions on further purification resulted in isolation of five pure compounds. Characterization was carried out by using (1)H NMR, (13)C NMR and MS. They were further evaluated for antioxidant and anti-inflammatory activity using carrageenan-induced paw edema model in rats. Molecular docking study was performed using Glide module integrated in Schrodinger molecular modeling software. RESULTS: The compounds were identified as 1,7-diphenylhept-4-en-3-one (1), 5-hydroxy-1,7-diphenyl-3-heptanone (2), 3,5,7-trihydroxyflavone (Galangin, 3), 3,5,7-trihydroxy-4'-methoxyflavone (Kaempferide, 4) and 5-hydroxy-7-(4″-hydroxy-3″-methoxyphenyl)-1-phenyl-3-heptanone (5). The compound-3 and compound-5 (10mg/kg) showed significant (p<0.001) antioxidant and anti-inflammatory potential. Moreover, total phenolic content was detected as 72.96 mg and 51.18 mg gallic acid equivalent respectively. All the five isolates were found to be good binders with COX-2 (average docking score -9.03). CONCLUSIONS: Galangin and 5-hydroxy-7-(4″-hydroxy-3″-methoxyphenyl)-1-phenyl-3-heptanone exhibited anti-inflammatory and in-vitro antioxidant activity which may be due to presence of phenolic content in it. The molecular docking study revealed that these compounds have affinity towards COX-2 active site which can further be explored as selective COX-2 inhibitors. The results obtained in this work justify the use of A. officinarum in the treatment of inflammatory disorders like rheumatoid arthritis and inflammatory bowel diseases.


Asunto(s)
Alpinia/inmunología , Antiinflamatorios/farmacología , Antioxidantes/farmacología , Inhibidores de la Ciclooxigenasa 2/farmacología , Extractos Vegetales/farmacología , Animales , Antiinflamatorios/aislamiento & purificación , Antioxidantes/aislamiento & purificación , Ciclooxigenasa 2/metabolismo , Inhibidores de la Ciclooxigenasa 2/aislamiento & purificación , Femenino , Flavonoides/aislamiento & purificación , Ácidos Heptanoicos/aislamiento & purificación , Espectroscopía de Resonancia Magnética , Espectrometría de Masas , Chaperonas Moleculares/metabolismo , Extractos Vegetales/aislamiento & purificación , Unión Proteica/efectos de los fármacos , Ratas , Ratas Wistar , Rizoma
18.
Inflamm Allergy Drug Targets ; 13(6): 393-405, 2015.
Artículo en Inglés | MEDLINE | ID: mdl-25675406

RESUMEN

We have reported the synthesis, characterization, in vitro release profile and preliminary pharmacological investigations of an antioxidant mutual prodrug of diacerein with thymol in our earlier communication. The present work reports the results of in vivo release studies and extensive pharmacological evaluation of this prodrug in collagenase- induced osteoarthritis and monosodium iodoacetate- induced hyperalgesia in Wistar rats. In vivo release was thoroughly studied in Wistar rats upon oral administration of the prodrug. In rat blood, release of 92.7% of diacerein and 20.5% of thymol was observed. From these studies we hypothesized that activation of prodrug could be mediated by physiological pH of blood (7.4) and serum esterases. Pharmacological screening of prodrug in collagenase and monoiodoacetate-induced osteoarthritis at a dose of 6.8 mg/kg, (BID) exhibited significant reduction in knee diameter (p<0.001), increase in paw withdrawal latency (p<0.001), and locomotor activity (p<0.001) with significantly higher anti-inflammatory and anti-osteoarthritic activities as compared to parent drug. The biochemical studies indicated a significant step-up in glucosaminoglycan level (p<0.001) and reduction in the C-reactive protein (p<0.001) and sulfated alkaline phosphatase levels (p<0.001). The histopathological and radiological studies confirmed the additive anti-osteoarthritic effect of prodrug as compared to plain diacerein. Antioxidant potential of prodrug was significantly more (p<0.001) while ulcer index was significantly lower (p<0.01) than diacerein. Interestingly, the diarrhea observed in diacerein- treated animals was not evident in animalstreated with prodrug, thymol and their physical mixture. Our findings indicate promising potential of this antioxidant prodrug to be used for long-term and safer management of OA.


Asunto(s)
Antraquinonas/farmacología , Antiinflamatorios/farmacología , Osteoartritis/tratamiento farmacológico , Profármacos , Timol/farmacología , Animales , Antraquinonas/química , Antraquinonas/uso terapéutico , Antiinflamatorios/química , Antiinflamatorios/uso terapéutico , Antiinflamatorios no Esteroideos/farmacología , Antiinflamatorios no Esteroideos/uso terapéutico , Antioxidantes/farmacología , Colagenasas , Evaluación Preclínica de Medicamentos , Concentración de Iones de Hidrógeno , Yodoacetatos , Articulaciones/patología , Masculino , Actividad Motora/efectos de los fármacos , Osteoartritis/inducido químicamente , Osteoartritis/patología , Dimensión del Dolor/efectos de los fármacos , Ratas , Ratas Wistar , Úlcera Gástrica/inducido químicamente , Timol/química , Timol/uso terapéutico
19.
Int J Ayurveda Res ; 1(3): 159-62, 2010 Jul.
Artículo en Inglés | MEDLINE | ID: mdl-21170207

RESUMEN

OBJECTIVE: To study the efficacy of Kumbhajatu in reducing the cholesterol levels and as an antioxidant in hypercholesterolemic rats. MATERIALS AND METHODS: Hypercholesterolemia was induced in normal rats by including 2% w/w cholesterol, 1% w/w sodium cholate and 2.5% w/w coconut oil in the normal diet. Powdered form of Kumbhajatu was administered as feed supplement at 250 and 500 mg/kg dose levels to the hypercholesterolemic rats. Plasma lipid profile, hepatic superoxide dismutase (SOD) activity, catalase activity, reduced glutathione and extent of lipid peroxidation in the form of malondialdehyde were estimated using standard methods. RESULTS: Feed supplementation with 250 and 500 mg/kg of Kumbhajatu resulted in a significant decline in plasma lipid profiles. The feed supplementation increased the concentration of catalase, SOD, glutathione and HDL-c significantly in both the experimental groups (250 and 500 mg/kg). On the other hand, the concentration of malondialdehyde, cholesterol, triglycerides, LDL-c and VLDL in these groups (250 and 500 mg/kg) were decreased significantly. CONCLUSION: The present study demonstrates that addition of Kumbhajatu powder at 250 and 500 mg/kg level as a feed supplement reduces the plasma lipid levels and also decreases lipid peroxidation.

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