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Immunomodulatory Activity and Chemical Characterisation of Sangre de Drago (Dragon's Blood) from Croton lechleri
Abstract
The immunomodulatory activity of the latex from Croton lechleri (sangre de drago) was determined by in vitro assays. Classical (CP) and alternative (AP) complement pathways activities were determined in human serum. Intracellular generation of reactive oxygen species (ROS) by human polymorphonuclear leukocytes (PMNs) and monocytes, and phagocytosis of opsonised fluorescent microspheres were measured by flow cytometry. Free radical scavenging activity was evaluated using 1,1-diphenyl-2-picrylhydrazyl (DPPH). Activity on proliferation of murine lymphocytes was also investigated. In addition, anti-inflammatory activity was assayed in vivo by carrageenan-induced rat paw oedema test. Some of the activities were compared with those of the isolated alkaloid taspine. Sangre de drago from Croton lechleri showed immunomodulatory activity. It exhibited a potent inhibitory activity on CP and AP of complement system and inhibited the proliferation of activated T-cells. The latex showed free radical scavenging capacity. Depending on the concentration, it showed antioxidant or prooxidant properties, and stimulated or inhibited the phagocytosis. Moreover, the latex has strong anti-inflammatory activity when administered i. p. Taspine cannot be considered the main responsible for these activities, and other constituents, probably proanthocyanidins, should be also involved.
Abbreviations
AP:alternative pathway
Con A:concanavalin A
CP:classical pathway
DCFH-DA:2′,7′-dichlorofluorescin diacetate
DPPH:1,1-diphenyl-2-picrylhydrazyl
FSC:forward angle light scatter
HPLC:high-performance liquid chromatography
LB:lymphoid leukaemia
LPS:lipopolysaccharide
NMR:nuclear magnetic resonance
PC:phagocytic capacity
PI:phagocytic index
PKC:protein kinase C
PMA:phorbol-12-myristate-13-acetate
PMNs:polymorphonuclear leukocytes
ROS:reactive oxygen species
SD:standard desviation
SP:estimulation of phagocytosis
SSC:side light scatter
TLC:thin layer chromatography
UV:ultraviolet
... Meanwhile, other researchers also found 74 substances in the essential oil of C. lechleri (Rossi et al. 2011 The chemical peculiarity of this plant led us to suppose that it could be a source of chemical agents capable of acting on multiple pharmacological targets in interaction with the immune system. However, only one immunological study has been performed (Risco et al. 2003), where it was demonstrated the stimulation of phagocytosis in human monocytes by the bark's sap at 5-20 µg/ml and observed the inhibition of phagocytosis activity in human blood monocytes at a higher concentration (50 µg/ml). The immunomodulatory activity of the plant extract was attributed to catechins (monomeric flavan-3-ols) and proanthocyanidins (19)(20)(21)(22)(23). Recently, Shakoor et al. (2021) suggested that polyphenols such as catechins (monomeric flavan-3-ols) and proanthocyanidins could be directly or indirectly involved in the stimulation of the immune response. ...
... The immunomodulatory activity of the plant extract was attributed to catechins (monomeric flavan-3-ols) and proanthocyanidins (19)(20)(21)(22)(23). Recently, Shakoor et al. (2021) suggested that polyphenols such as catechins (monomeric flavan-3-ols) and proanthocyanidins could be directly or indirectly involved in the stimulation of the immune response. These molecules would also be strongly related to antioxidant effects, compared with quercetin and ascorbic acid (De Marino et al. 2008;Risco et al. 2003). In addition, proanthocyanidin fractions revealed a significant inhibitory activity against DNA and RNA viruses, for example, respiratory syncytial virus, influenza A virus, parainfluenza virus, herpesvirus types 1 and 2, and hepatitis A and B virus (Barnard et al. 1993;Ubillas et al. 1994). ...
... This alkaloid showed significant activity at 20 mg/kg/day when compared with the positive control (indomethacin; 1 mg/kg/day) in a carrageenan-induced edema assay (Perdue et al. 1979). Meanwhile, the sap from C. lechleri at 5 mg/ kg i.p. exhibited potent activity during the first 4 h, in comparison with naproxen at 20 mg/kg i.p. (Risco et al. 2003). 3′,4-O-dimethylcedrusin (27) was related to healing, due to its stimulatory actions in wound repair (De Marino et al. 2008). ...
Unlabelled:
The current COVID-19 pandemic, characterized by a highly contagious severe acute respiratory syndrome, led us to look for medicinal plants as an alternative to obtain new drugs, especially those with immunomodulatory abilities, capable of acting against the pulmonary infection caused by coronavirus 2 (SARS-CoV-2). Despite medical advances with COVID-19 drugs and vaccines, plant-based compounds could provide an array of suitable candidates to test against this virus, or at the very least, to alleviate some symptoms. Therefore, this review explores some plants widely used in Peru that show immunomodulatory properties or, even more, contain phytoconstituents potentially useful to prevent or alleviate the COVID-19 infection. More interestingly, the present review highlights relevant information from those plants to support the development of new drugs to boost the immune system. We used three criteria to choose nine vegetal species, and a descriptive search was then conducted from 1978 to 2021 on different databases, using keywords focused on the immune system that included information such as pharmacological properties, phytochemical, botanical, ethnobotanical uses, and some clinical trials. From these literature data, our results displayed considerable immunomodulation activity along with anti-inflammatory, antiviral, antioxidant, and antitumoral activities. Noticeably, these pharmacological activities are related with a wide variety of bioactive phytoconstituents (mixtures or isolated compounds) which may be beneficial in modulating the overt inflammatory response in severe COVID-19. Further scientific research on the pharmacological activities and clinical utilization of these potential plants are warranted.
Supplementary information:
The online version contains supplementary material available at 10.1007/s43450-023-00367-w.
... The sap of Croton lechleri Müll. Arg (Euphorbiaceae) species may be an alternative for the treatment of ulcers in diabetics, since it is already known to have a healing effect (CAI et al., 1991;PHILLIPSON, 1993;PHILLIPSON, 1994;PIETERS et al., 1992), antihemorrhagic (CAI et al., 1991;PHILLIPSON, 1993), antimicrobial (CHEN;PHILLIPSON, 1994) and anti-inflammatory (RISCO, 2003). ...
... Taspine is an alkaloid that assists in the healing of cellular tissues (AZEVEDO et al., 2008). In addition to taspine, other compounds present in sap, such as proanthocyanidins, may be involved in the exposed actions (RISCO et al., 2003). Proanthocyanidin SP-303 is related to the control of diarrhea (FISCHER et al., 2004). ...
... Proanthocyanidin SP-303 is related to the control of diarrhea (FISCHER et al., 2004). The sap has antioxidant and immunomodulatory properties (RISCO et al., 2003). Phenolic compounds, under certain conditions, may promote DNA damage, therefore studies are indicated to ensure the use of this sap (ROSSI et al., 2003). ...
Ulcers development in lower limbs is a potential complication known in Diabetes mellitus patients. Conventional medicines frequently do not show desired efficacy, resulting in adverse effects. In this sense, the seek for natural treatments, effective, easy to obtain and handle and at the same time with low cost, becomes a therapeutic alternatives for the ulcers treatment. The aim of this study was to verify the healing potential of a cream made with Croton lechleri Müll.Arg. sap, when applied in diabetic patients ulcers. It is concluded that the cream made with Croton lechleri Müll.Arg. sap showed healing potential, however, several variables should be evaluated and considered simultaneously, since diabetes is a multifactorial disease.
... Its bark releases by incision a blood-red latex (sap) called 'Sangre de Drago', which constitutes a common household remedy in Latin American countries where is used to stop bleeding, help heal wounds, and treat intestinal ailments (Chen et al. 1994;Jones 2003;Pona et al. 2019). Characteristic secondary metabolites are proanthocyanidins, which account for up to 90% of the dried sap, together with other polyphenols such as catechins (Cai et al. 1991;Risco et al. 2003). Further studies led to the isolation of taspine, a distinctive alkaloid, and 3 0 ,4-Odimethylcedrusin, a lignan (Vaisberg et al. 1989;Chen et al. 1994;De Marino et al. 2008). ...
... The TPC of C. lechleri sap was 713.8 ± 24.9 GAE mg/g, while the TFC was 0.4 ± 0.2 QE mg/g. Figure S4A shows DPPH radical inhibition obtained with the sap in the concentration range of 0.01-100 mg/mL; IC 50 ¼ 2.74 mg/mL. Other authors indicated for the sap an IC 50 of 7.73 mg/mL (Risco et al. 2003). Furthermore, the antiradical activity was detected also with ORAC assay, showing a TEAC of 4798 ± 368 mmol/g ( Figure S4B). ...
... C. lechleri sap at micromolar concentrations decreased both basal and H 2 O 2 -induced ROS production ( Figure S6). These results agree with those of Risco et al. who showed the inhibitory activity of the sap (0.01-1.0 mg/mL) on H 2 O 2 -induced ROS production in human neutrophils (Risco et al. 2003). The protective effect of C. lechleri against ROS production can be due to the high presence of polyphenols, such as catechins and proanthocyanidins, detected in the sap (Risco et al. 2003;Takami et al. 2010). ...
The sap of Croton lechleri M€ ull. Arg. (Euphorbiaceae) is well-known in South American traditional medicine. This research investigated its activity against glycation and oxidative stress (glycoxidation) to estimate its usefulness in ROS-related diseases. The activity of the sap on albumin glycation, LDL oxidation and ROS formation was detected. C. lechleri sap inhibited BSA glycation and exhibited a protective effect against LDL oxidation; at the concentration of 0.8 mg/mL, it extended the Lag phase of almost 60%. Furthermore, the sap was studied on cell viability and ROS production in HUVEC showing valuable free-radical scavenging activity. In detail, the sap (1.0 and 10.0 lg/mL) significantly decreased the baseline level and H 2 O 2-induced ROS production in HUVEC. This research showed for the first time the ability of C. lechleri sap to decrease the albumin glycation, LDL oxidation and ROS formation in HUVEC, supporting its potential in vascular diseases. ARTICLE HISTORY
... The sap of Croton lechleri Müll. Arg (Euphorbiaceae) species may be an alternative for the treatment of ulcers in diabetics, since it is already known to have a healing effect (CAI et al., 1991;PHILLIPSON, 1993;PHILLIPSON, 1994;PIETERS et al., 1992), antihemorrhagic (CAI et al., 1991;PHILLIPSON, 1993), antimicrobial (CHEN;PHILLIPSON, 1994) and anti-inflammatory (RISCO, 2003). ...
... Taspine is an alkaloid that assists in the healing of cellular tissues (AZEVEDO et al., 2008). In addition to taspine, other compounds present in sap, such as proanthocyanidins, may be involved in the exposed actions (RISCO et al., 2003). Proanthocyanidin SP-303 is related to the control of diarrhea (FISCHER et al., 2004). ...
... Proanthocyanidin SP-303 is related to the control of diarrhea (FISCHER et al., 2004). The sap has antioxidant and immunomodulatory properties (RISCO et al., 2003). Phenolic compounds, under certain conditions, may promote DNA damage, therefore studies are indicated to ensure the use of this sap (ROSSI et al., 2003). ...
Ulcers development in lower limbs is a potential complication known in Diabetes mellitus patients. Conventional medicines frequently do not show desired efficacy, resulting in adverse effects. In this sense, the seek for natural treatments, effective, easy to obtain and handle and at the same time with low cost, becomes a therapeutic alternatives for the ulcers treatment. The aim of this study was to verify the healing potential of a cream made with Croton lechleri Müll.Arg. sap, when applied in diabetic patients ulcers. It is concluded that the cream made with Croton lechleri Müll.Arg. sap showed healing potential, however, several variables should be evaluated and considered simultaneously, since diabetes is a multifactorial disease.
... Antioxidant activity was shown by C. celtidifolius (Coutinho et al., 2011), C. lechleri (Marino et al., 2008) and C. zehntneri (Morais et al., 2006). Anti-inflammatory property was found in C. celtidifolius (Nardi et al., 2003), C. crassifolius (Zhao et al., 2012), C. lechleri (Risco et al., 2003) and C. campestris (El Babili et al., 2006). Antinociceptive attributes have been identified in C. crassifolius (Risco et al., 2003), C. nepetaefolius (Abdon et al., 2002), C. celtidifolius (Nardi et al., 2006) and C. zehntneri (Oliveira et al., 2001). ...
... Anti-inflammatory property was found in C. celtidifolius (Nardi et al., 2003), C. crassifolius (Zhao et al., 2012), C. lechleri (Risco et al., 2003) and C. campestris (El Babili et al., 2006). Antinociceptive attributes have been identified in C. crassifolius (Risco et al., 2003), C. nepetaefolius (Abdon et al., 2002), C. celtidifolius (Nardi et al., 2006) and C. zehntneri (Oliveira et al., 2001). Antiviral by C. lechleri (Ubillas et al., 1994) and antileishmaniasis by C. echioides Baill (Novello et al., 2022). ...
The search for compounds with anticancer effects is of paramount importance today due to the high incidence of the disease. The Euphorbiaceae family is known for having compounds with therapeutic properties, one of its genera being Croton. It has several species, which contain compounds already known for their biological activities, presenting anti-inflammatory, antimicrobial and anticancer properties. Thus, the cytotoxicity/antiproliferative activity of semi-purified fractions and compounds isolated from Croton echioides in liver tumor cells of Rattus norvegicus (HTC) was evaluated by the MTT test. The semi-purified fractions showed cytotoxicity at concentrations above 200 µg/mL, at 24, 48 and 72 hours, reaching cell viability of 24.78% [400 µg/mL] at 24 hours, 12.79% [500 µg/mL] at 48 hours and 10.57% [300 µg/mL] at 72 hours. For the isolated compounds, lupeol had a cytotoxic effect in all concentrations (1, 5, 10, 15, 20, 40, 60, 80 and 100 µg/mL) and tested times (24, 48 and 72 hours), reaching minimum viability of 4.37% [100 µg/mL], within 72 hours. The clerodan diterpenes CEH-1 and CEH-4 also showed antiproliferative activity, with minimum viability of 36.19% [100 µg/mL] over 72 hours and 21.33% [100 µg/mL] over 48 hours, respectively. However, the clerodan diterpenes CEH-2 and CEH-3 did not shows a cytotoxic effect for HTC cells. Thus, there is a cytotoxic/antiproliferative potential of C. echioides against tumor cells, with targeted to mitochondrial enzymes, associated with cell proliferation, indicating that this species deserves prominence in the search for new molecules for the treatment of cancer.
... Además de las características antibacterianas sobre cepas bacterianas de cavidad bucal, se ha promovido otro tipo de propiedades de este compuesto como lo aseveran estudios in vitro realizados por Risco et al. 26 ; en cuyas investigaciones demuestran que la sangre de dra-go posee un efecto inmunomodulador, con capacidad para eliminar los radicales libres y dependiendo de la concentración puede poseer propiedades antioxidantes y pro oxidantes; a su vez la capacidad antiinflamatoria es una de las principales características de este compuesto natural. ...
... La sangre de drago ha demostrado una capacidad de inhibición en la vía clásica y alternativa del sistema de complemento, así como también de la proliferación linfocitaria estimulada por mitosis con concavalina A y el crecimiento celular en leucemia linfoide, lo cual resulta en la capacidad de inhibición de las respuestas inmunes mediadas por células, que se puede atribuir a su componente 3',4-O-Dimethylcedrusin, el mismo que posee actividad potencialmente anti proliferativa y antitumoral 26 . ...
Objetivo: El propósito del presente estudio fue determinar la actividad antibacteriana de Croton lechleri (C. lechleri) sobre cepas de S. mutans ATCC 35668. Métodos: Se utilizó concentraciones al 50, 75 y 100% de C. lechleri, como control positivo a la clorhexidina 0,12% y al agua destilada como control negativo. Se midieron los halos de inhibición producidos alrededor de discos embebidos con cada una de las concentraciones de C. lechleri sobre colonias de S. mutans sembradas en Agar Muller Hinton. Resultados: Las concentraciones al 75% y 100% de C. lechleri mostraron actividad antibacteriana in vitro sobre S. mutans, la concentración al 50% no manifestó ninguna actividad. La clorhexidina al 0,12% mostró mayor actividad antibacteriana in vitro que las concentraciones de C. lechleri en los grupos de estudio evaluados. Conclusiones: Croton lechleri puede ser una alternativa natural, accesible y de bajo costo para métodos de prevención en caries dental al utilizarse al 75 y 100%.
... En nuestro país se han encontrado muchas plantas oriundas utilizadas, tradicionalmente, para el tratamiento del dolor e inflamación; dentro de las más usadas se encuentran: Croton lechleri "sangre de drago" (12) ; Chenopodium ambrosioides L. "paico" (13) , Peperomia congona Sodiro "congona" (14) y Perezia coerulescens "mancharisqa" (7) , las cuales son objeto de estudio en esta investigación. ...
... El extracto etanólico de Croton lechleri a las concentraciones de 100 y 200 ug/mL presentó una actividad antinflamatoria similar al fármaco de referencia (dexametasona), por lo que se puede considerar a C. lechleri como una sustancia que no daña la membrana. Esta actividad antiinflamatoria se atribuye a la presencia de metabolitos activos como flavonoides y terpenos, lo que se ha corroborado en estudios previos con concentraciones alrededor de 200 µg/mL (12) . ...
Objetivo. Determinar la actividad antinflamatoria in vitro de los extractos etanólicos de Croton lechleri,Chenopodium ambrosioides L., Peperomia congona Sodiro y Perezia coerulescens, mediante el métodode estabilización de la membrana de glóbulos rojos. Materiales y métodos. Se emplearon muestras desangre humana, donde se evaluaron cuatro diluciones seriadas, 200, 100, 50 y 10 μg/mL de los diferentesextractos, usando una solución isosalina (0,85%, pH 7,2) como medio de dilución, y como fármaco dereferencia dexametasona (200 ug/mL). Se determinaron los porcentajes de hemólisis y protección de lamembrana del glóbulo rojo. Resultados. Se encontraron diferencias significativas entre los promedios deporcentajes de protección y las concentraciones en el caso de Ch. ambrosioides L (p<0,001), P. coerulescens (p<0,001) y C. lechleri (p<0,001). Se encontró correlación lineal entre los porcentajes de protección y la concentración en el caso de Ch. ambrosioides L (R2= 0,795; p<0,001), C. lechleri (R2= 0,631; p<0,001) y P. coerulescens (R2= 0,899; p<0,001). Los extractos de C. lechleri a 100 y 200 ug/mL; y el extracto de P. coerulescens a 200 ug/mL no presentaron diferencias significativas en sus porcentajes de protección en comparación al uso de dexametasona 200 ug/mL (p>0,05) Conclusión. Los extractos etanólicos de P. coerulescens, Ch. ambrosioides L y C. lechleri, presentan actividad antinflamatoria mediante la inhibición de la lisis de la membrana celular en glóbulos rojos. En el caso del extracto de C. lechleri a 100 y 200 ug/mL, así como el extracto de Ch. ambrosioides L a una concentración de 200 ug/mL, mostraron un desempeño similar al fármaco de referencia (dexametasona).
... En referencia a los otros parámetros hematológicos como los leucocitos, linfocitos y neutrófilos, además de que sus variaciones pueden estar relacionadas a los factores antes mencionados, en un estudio anterior de Chen ZP et al. (19) se mostró que el látex de "sangre de drago" presenta actividad antibacteriana y un ligero incremento sobre la proliferación de células endoteliales. Además, se conoce que Croton lechleri Muell. ...
... dérmica por 14 días, y por Chen et al.(19) quienes reportan ausencia de citotoxicidad in vitro de la resina, en un modelo de citotoxicidad, con un IC 50 mayor de 900 mg/mL. Asimismo, Bussmann et al.(27) no encontraron signos de toxicidad en el uso de extracto acuoso en Artemia salina. ...
Objetivo: Determinar si la administración crónica (90 días) del látex liofilizado de Croton lechleri Muell. Arg. “Sangre de drago” modifica los parámetros hematológicos y bioquimicos en Rattus norvegicus var albinus. Materiales y métodos: Se utilizó ratas con un peso corporal (p.c.) entre 150 g a 170 g, distribuidos en Grupo A (control) y Grupos B y C (experimentales), de 20 especímenes cada uno (10 hembras y 10 machos) a las que se administró por vía oral NaCl 0.9% y una dosis diaria de 100 y 200 mg de látex liofilizado/Kg p.c. respectivamente, durante 90 días. Se tomaron muestras de sangre cada 15 días para determinar parámetros hematológicos (hematocrito, linfocitos, leucocitos y segmentados) y bioquímicos (glucosa, urea, creatinina, colesterol total y perfil hepático). Resultados: Todos los valores se encontraron dentro del rango normal. Se encontraron diferencias significativas al comparar los grupos de estudio en los resultados de glucosa (Control vs Grupo I: p<0.001 y Grupo II: p=0.003) y creatinina (Grupo II vs Grupo I: p=0.008 y control: p<0.001). Los valores de bilirrubina total y proteínas totales variaron significativamente durante el tiempo de estudio (p=0.001 y p<0.001, respectivamente). El resto de parámetros no presentaron variaciones significativas por grupos (p>0.05). Conclusión: El látex liofilizado de Croton lechleri Muell. Arg. no generó toxicidad en los parámetros hematológicos y bioquímicos estudiados en Rattus norvegicus var Albinus.
... The latex from C. lechleri also showed immunomodulatory activity in vitro through a potent inhibitory activity on classical and alternate pathways of the complement system, the inhibition of the proliferation of activated T-cells and free radical scavenging capacity. Depending on the concentration, it showed antioxidant or prooxidant properties, and the stimulation or inhibition of phagocytosis (Risco et al., 2003). Moreover, the latex has shown anti-inflammatory, antibacterial and antiviral activities (Ubillas et al., 1994;Jones, 2003;Risco et al., 2003Risco et al., , 2005. ...
... Depending on the concentration, it showed antioxidant or prooxidant properties, and the stimulation or inhibition of phagocytosis (Risco et al., 2003). Moreover, the latex has shown anti-inflammatory, antibacterial and antiviral activities (Ubillas et al., 1994;Jones, 2003;Risco et al., 2003Risco et al., , 2005. ...
Central and South America is a very attractive region for ethnopharmacology. The large diversity of indigenous people still living in highly biodiverse ecosystems makes the scientific study of indigenous medicines in this region extremely interesting. A number of important drugs come from plants of Central and South America, such as quinine, quinidine, (+)-tubocurarine, emetine and pilocarpine. Some of them, such as capsaicin, have led to the development of useful new analogues, like zucapsaicin. Also, a number of herbal drugs from the region are now important elements of phytoterapy worldwide. Among recent developments, two are particularly relevant. In 2012, crofelemer, obtained from the latex of Croton lechleri (dragon's blood), was approved by the US FDA as a medicinal product for the symptomatic treatment of certain cases of secretory diarrhoea. Secondly, a cream containing the essential oil of Cordia verbenacea is the first innovative medicine approved and introduced in the Brazilian marketplace by a Brazilian company. Furthermore, some experiences developed in the region are aimed at giving back to local communities part of the gains obtained from ethnopharmacological research, mainly in order to contribute to their health care. This often requires the integration of indigenous and western medicine through mutual respect and equal recognition. Finally, one of the most popular Central and South American subjects of ethnopharmacological research of the past decades, the hallucinogens, is experiencing a new surge of more carefully carried out research. New clinical evidence seems to suggest that hallucinogens may have a therapeutic role in modern medicine.
... East India Kino or Malabar Kino, Fabaceae). Dragon's blood has been used by different civilizations such as the Greeks, the Romans, and the Arabs. 1 Croton lechleri has several medicinal properties, such as wound healing, 1,2 cicatrizant, 3 immunomodulator, 1,4 analgesic, antiulcer, antidiarrheal, 1 antibacterial, 5 antiviral, 6 antihemorrhagic, 1 antiinflammatory, antioxidant, 1,3 mutagenic and antimutagenic, 1,3,7 antitumor, 1,8 anticancer, 9 and cytotoxic effects. 1,3 Proanthocyanidins are the main chemical constituent of the resin, >90% of the dry weight. ...
... 14e16 Dragon's blood has the immunomodulatory property by influence on complement system. 4 The antioxidant agents from Dragon's blood leaves and fruit, such as phenolic profile and organic acids, are able to protect against free radicals. 17,18 Noteworthy, the anti-inflammatory effect of the alkaloid taspine has been reported. ...
The blood-red sap of Dragon's blood has been used in folk medicine for fractures, wounds, inflammation, gastrointestinal disorders, rheumatism, blood circulation dysfunctions, and cancer. Existing in vitro and in vivo bioactivity of this herb on different mechanisms of healing shows strong potential of this sap in wound healing. This clinical trial study was designated to evaluate the wound healing effect of Dragon's blood on human wounds. Sixty patients, between the ages of 14–65 years, who were referred to remove their skin tag, were assigned to this double-blind, placebo-controlled, randomized clinical trial and received either Dragon's blood or a placebo cream. They were visited on the 3rd, 5th, 7th, 10th, 14th, and 20th day of the trial to check the process of healing and to measure the wound's surface. At the end of trial, there was a significant difference in the mean duration of wound healing between the two groups (p = 0.0001). The phenolic compounds and the alkaloid taspine, which exist in Dragon's-blood resin, are probably the main reasons for the wound healing property of this plant. Being natural accessible, safe, and affordable makes Dragon's blood cream, a good choice for addition to the wound healing armamentarium. Further studies on wounds with different causes and among larger populations are suggested to ensure the effectiveness and safety of Dragon's blood.
... Suarez et al demonstrated that intraperitoneal administration of an aqueous extract of Croton malambo (Euphorbiaceae) resulted in a significant anti-inflammatory effect in a rat model of edema (16). Furthermore, Sangre de Drago (dragon's blood) from Croton lechleri (Euphorbiaceae) inhibits inflammation in vitro and in vivo (17,18). For example, treatment with Sangre de Drago significantly decreased intracellular generation of reactive oxygen species in several cell lines and alleviated paw edema in rats (18). ...
... Furthermore, Sangre de Drago (dragon's blood) from Croton lechleri (Euphorbiaceae) inhibits inflammation in vitro and in vivo (17,18). For example, treatment with Sangre de Drago significantly decreased intracellular generation of reactive oxygen species in several cell lines and alleviated paw edema in rats (18). However, the anti-inflammatory effects of methanol extracts of Euphorbia cooperi (MEC) remain to be elucidated. ...
Numerous Euphorbiaceae plants have been used for the treatment of diseases, including liver diseases, asthma and rheumatism. The present study evaluated the effect of methanol extracts from Euphorbia cooperi (MEC), a member of the Euphorbiaceae plant family, on the production of inflammatory cytokines interleukin (IL)‑6 and tumor necrosis factor (TNF)‑α, nitric oxide (NO) as well as the activation of mitogen‑activated protein kinase and nuclear factor (NF)‑κB signaling. Non‑cytotoxic concentrations of MEC significantly reduced the production of NO and IL‑6, but not TNF‑α, in lipopolysaccharide (LPS)‑stimulated RAW 264.7 macrophages. The decreased production of NO by MEC was due to alleviated expression of inducible NO synthase. Reporter assays with cells treated with MEC demonstrated reduced activator protein‑1 (AP-1) activity, while NF‑κB activity was not reduced. Furthermore, the phosphorylation levels of c‑Jun N‑terminal kinase (JNK) and p38 were suppressed by MEC while phosphorylation levels of inhibitor of κB were not reduced by MEC, suggesting that MEC‑mediated inactivation of JNK and p38 is the underlying regulatory mechanism for inflammatory mediators in LPS‑stimulated RAW 264.7 macrophages.
... In ethnobotany, using dragon's blood canincrease the healing popularity and clinical application when there is a wound [1,2], including antihemorrhagic [3], immunomodulatory [4], antioxidant [5], and active compounds in antimutagenic agents [6]. Chinese herbal medicines have a long history of use in traditional medicine and are still widely used today with high safety and low toxicity [7]. ...
Dragon’s blood (血竭) is a traditional Chinese medicine known for its wound hemostasis, blood circulation, and stasis properties. Recently, it has also been utilized in cosmetics, though its antioxidant capacity remains unclear. This study aims to stabilize the bioactivity of dragon’s blood using various plant extracts. We evaluated single plant extracts and their combinations to identify the conditions that maintained the antioxidant capacity of dragon’s blood the longest. Selected plants included Hibiscus sabdariffa, Clitoria ternatea, Hylocereus sp., Pandanus amaryllifolius, and Camellia sinensis. We used two sources of dragon’s blood: Daemonorops draco and Dracaena cochinchinensis. Extraction conditions were optimized and antioxidant activity was assessed using the free radical scavenging ability of 1,1-diphenyl-2-picrylhydrazyl (DPPH), total anthocyanin concentration (TAC), total polyphenol content (TPC), the free radical scavenging activity of ABTS, and a ferric reducing antioxidant power (FRAP) assay. The results showed that all plant extracts exhibited high antioxidant capacity. Clitoria ternatea had the highest DPPH scavenging ability at 93.81%, with the best combination being green tea and Daemonorops draco at 92.57%. Clitoria ternatea had the highest TPC at 9921 mg GAE/100 g, with the best combination (green tea and Dracaena cochinchinensis) at 10500 mg GAE/100 g. ABTS activity was highest for green tea at 98.3%, with the best combination (Clitoria ternatea and Daemonorops draco) at 93.29%. The FRAP assay showed that green tea had the highest electron-donating potential at 3.85 mg/mL, with the best combination (Daemonorops draco and Dracaena cochinchinensis) at 3.71 mg/mL. This study advances our understanding of the antioxidant properties of these plants and the traditional Chinese medicine dragon’s blood, enhancing the efficacy of dragon’s blood in skincare and cosmetics. Moreover, the application of these extracts could rejuvenate local agriculture, impacting the skincare, cosmetics, and sustainable agriculture sectors.
... El azúcar tiene propiedades higroscópicas con alta osmolaridad, que permite eliminar las bacterias mientras promueve el tejido de granulación, además mejora la migración de macrófagos, reducción de edema y epitelización; su uso se recomienda en forma de pasta por ser más efectiva y fácil aplicación (Pavletic, 2018). De otra parte, el látex de C. lechleri (sangre de grado) tiene propiedades inmunomoduladoras para heridas, capacidad para formar una película que proteja contra la invasión microbiana de heridas, actividad captadora de radicales libres brindadas por las procianidinas, efecto antiinflamatorio, antibacteriano y acción de los polifenoles (Jones, 2003;Risco et al., 2003). ...
A case of severe ulcerative pododermatitis infected with Staphylococcus aureus and Proteus spp in a guinea pig raised in a metal cage is described. A 9-month-old female guinea pig weighing 850 g is taken to consultation for presenting discomfort when walking. Severe ulcerative pododermatitis (grade IV or V) in the hind limbs was diagnosed based on clinical signs, cytology, and radiographs. The animal was removed from the cage and placed on a flat surface. She was treated with a preparation based on 4 g of sugar and 0.5 ml of «dragon’s blood» (Croton lechleri), applying it to the lesion once a day and subsequently bandaging the affected area; in addition, oral prednisolone was used at a dose of 0.8 mg/kg every 24 hours in syrup for 14 days, and subcutaneous gentamicin at a dose of 6 mg/kg every 24 hours for a minimum of 21 days. Weekly clinical and cytology evaluations were made. The patient gradually improved, reducing the lesions, and the number of bacteria and inflammatory cells. The ulcers on the left leg closed on day 20 and on the right leg on day 26 of treatment.
... It has been used in China for more than 1500 years and is known as the "Holy Medicine for Promoting Blood" in the Compendium of Materia Medica [13]. Pharmacological studies have shown that Dragon's Blood has anti-inflammatory [14,15], antibacterial [16], antithrombotic [17], and analgesic effects [18] and immune-enhancing function [19]. Modern medical research has confirmed that Dragon's Blood can act on the microcirculation, relax and soften blood vessels, and can reverse hardening and narrowing of small arteries [20]. ...
During space manned missions, radiation is a serious health risk. Radiation can not only directly cause damage to target organs but also trigger side effects to affect nontarget organs. Dragon’s Blood (DB) is a traditional Chinese Dai medicine that has been proven to exhibit radioprotective effects in our lab previously. It can alleviate brain damage, hematopoietic dysfunction, and gastrointestinal damage caused by radiation in rats, but its mechanism of action is not clear yet. In order to study the effect of brain irradiation on the damage to the liver and the protective effects of Dragon’s Blood, herein, liquid chromatography coupled with a mass spectrometer was used to analyze the total differential protein expression in the rat liver after 30 Gy Co ⁶⁰ γ -ray whole-brain irradiation with/without administration of Dragon’s Blood for 10 days before irradiation. A total of 4557 proteins were identified in the rat liver. A total of 299 coexpressed differential proteins were screened in the RAD/CON group indicating that brain radiation significantly affected the liver’s metabolic system (such as drug and arachidonic acid metabolism), chemical carcinogenesis, and peroxisome process. A total of 85 differential proteins were screened in the DB/RAD group. Results indicated that Dragon’s Blood significantly regulated the expression of 26 proteins to normal levels (Msrb2, Txnrd2, Samm50, Pir, Pex11a, etc.) mainly through regulating the metabolism and redox homeostasis process. The results of molecular docking and network pharmacology found that the main effective radiation protection components in Dragon’s Blood are natural chalcones, flavan, and phenolic derivatives.
... Uma alternativa eficaz é a utilização de plantas medicinais para fins terapêuticos com eficácia no processo de cicatrização e com mínimos efeitos colaterais (BUDOVSKY; YARMOLINSKY; BEN-SHABAT, 2015), como é o caso do C. lechleri, que vem sendo utilizado empiricamente pela população indígena amazônica, desde o México até o Brasil (LORENZI;MATOS, 2008). Os principais constituintes dessa planta são taninos, lignanas e um alcaloide denominado taspina, a que se atribui a propriedade cicatrizante (LORENZI; MATOS, 2008 C. lechleri, planta nativa da região amazônica no Brasil e conhecida popularmente como Sangue de Dragão (GUPTA, 2008), têm em sua seiva uma alternativa para o tratamento de úlceras de diabéticos, pois esse recurso é utilizado em diversos países devido às diferentes ações já relatadas como cicatrizante (CAI et al., 1991;PIETERS et al., 1992;CHEN;PHILLIPSON, 1993;CHEN;PHILLIPSON, 1994;JONES, 2003;AZEVEDO et al., 2008), anti-hemorrágica (CAI et al., 1991;CHEN;PHILLIPSON, 1993), antimicrobiana (CHEN;PHILLIPSON, 1994), anti-inflamatória (RISCO et al., 2003), entre outras. ...
As úlceras de membros inferiores são complicações do Diabetes mellitus que demandam um alto custo para os serviços de saúde. A seiva de Croton lechleri Müll. Arg, planta conhecida como Sangue de Dragão, tem demonstrado um grande potencial para o tratamento de úlceras. O objetivo deste estudo foi acompanhar a evolução de úlceras crônicas nos membros inferiores de pessoas com diabetes, submetidas a um tratamento de três meses com pomada à base de seiva de C. lechleri. É um estudo piloto experimental, com abordagem quantitativa, cuja amostra foi composta por quatro pessoas. Os dados foram coletados por meio de registro fotográfico, exames laboratoriais e um instrumento semiestruturado. Para a análise dos dados foi utilizada estatística descritiva. A pomada não apresentou efeito antimicrobiano, todavia, observou-se uma redução do tamanho médio das úlceras, no entanto são necessárias análises adicionais para determinar a melhor formulação, tempo de tratamento e quantidade de aplicação.
... El azúcar tiene propiedades higroscópicas con alta osmolaridad, que permite eliminar las bacterias mientras promueve el tejido de granulación, además mejora la migración de macrófagos, reducción de edema y epitelización; su uso se recomienda en forma de pasta por ser más efectiva y fácil aplicación (Pavletic, 2018). De otra parte, el látex de C. lechleri (sangre de grado) tiene propiedades inmunomoduladoras para heridas, capacidad para formar una película que proteja contra la invasión microbiana de heridas, actividad captadora de radicales libres brindadas por las procianidinas, efecto antiinflamatorio, antibacteriano y acción de los polifenoles (Jones, 2003;Risco et al., 2003). ...
Se describe un caso de pododermatitis ulcerativa severa infectada con Staphylococcus aureus y Proteus spp en un cuy criado en jaula metálica. Un cuy hembra de 850 g y 9 meses de edad es llevado a consulta por presentar molestias al caminar. Se diagnosticó pododermatitis ulcerativa severa (grado IV o V) en extremidades posteriores basándose en signos clínicos, citología y radiografías. Se retiró al animal de la jaula y fue colocado en superficie plana. Se le trató con un preparado a base de 4 g de azúcar y 0.5 ml de sangre de grado (Croton lechleri), aplicándose en la lesión una vez al día y con posterior vendaje del área afectada; además se utilizó prednisolona oral a dosis de 0.8 mg/kg de p.v. cada 24 horas en jarabe por 14 días, y gentamicina subcutánea a dosis de 6 mg/kg p.v. cada 24 horas por un mínimo de 21 días. Se hicieron evaluaciones clínicas y de citología semanales. La paciente mejoró gradualmente, reduciendo las lesiones, el número de bacterias y de células inflamatorias. Las úlceras de la pata izquierda cerraron en el día 20 y de la pata derecha en el día 26 del tratamiento.
... In Dracaena species (Asparagaceae), dragon's blood is secreted as part of a naturally induced defense mechanism in reaction to pathogen infection, insect attack or mechanical injury (Jura-Morawiec and Tulik, 2016). Specialised metabolites in Dracaena resin have biological activities for clinical applications, and therefore the red resin is widely used in folk medicine due to its analgesic (Peres et al. 1998), anti-inflammatory (Miller et al. 2001), antioxidative (Machala et al. 2001), antiviral (Orozco-Topete et al. 1997), antimicrobial (Gupta and Gupta, 2011), antihemorrhagic (Esmeraldino et al. 2005), antimutagenic (Saffi et al. 2004;Teng et al. 2011), immunomodulatory (Risco et al. 2003), antiulcer (Fischer et al. 2004), and antitumor (Gonzales and Valerio, 2006) activities. ...
... Pokazano jego działanie immunomodulujące [40] oraz przydatność w leczeniu biegunki, stanów zapalnych, infekcji wirusowych [41] i bakteryjnych [42]. Polifenole żywicy mają silne właściwości antyoksydacyjne [43,44]. ...
Przyroda Ameryki Południowej, w tym Peru, to prawdziwa naturalna apteka; uważa się, że ponad 80% rosnących tu roślin ma właściwości lecznicze. Rejonem Andów i dorzeczem Amazonki interesują się zarówno firmy farmaceutyczne jak i ośrodki akademickie na ca-łym świecie. Kilka roślin tego regionu zdobyło już rozgłos w Europie, należą do nich: Cat’s claw (Uncaria tomentosa), Maca (Lepidium meyenii) czy Dragon’s blood (Croton lechleri). Każda z nich ma bardzo długą tradycję stosowania przez Indian w Ameryce Południowej. Jednak popularyzacja tych roślin jako surowców farmaceutycznych czy też roślin uzupeł-niających dietę mieszkańców Europy wymaga przeprowadzenia badań fitochemicznych, biologicznych oraz farmakologicznych.
... Dragon's blood is used for the improvement of blood circulation and reducing pain [12]. Research also indicates that dragon's blood has a variety of pharmacological effects, including immunoregulatory [13], antidiarrheic [14], antibacterial [15], antiviral [16], antioxidant [17], and anticancer [18]. Dragon's blood extracts contain a variety of active ingredients, mainly flavonoids and resin grade. ...
In recent years, an increasing number of natural plant extracts have been determined to be potential drugs for various illnesses. In this study, we investigated the effects of dracorhodin perchlorate (DP) on fibroblast proliferation, which is crucial for wound healing. Cell proliferation assays were performed by different concentrations of DP, and the cell viability was detected by CCK-8 kits. After DP treatment for 24 h, the cell cycle was checked by flow cytometer. EGFR and downstream signaling pathways ERK1/2 and PI3K were examined with DP treatment by western blot. We further determined the effects of the related inhibitors on DP-induced relative protein phosphorylation and cell proliferation. The results showed that 3 μ g/mL of DP promoted cell proliferation most significantly at treatment lengths of 24 h, and the percentage of cells in the S + G2 phase increased compared to those of the control group. In western blot detection, we found that DP significantly upregulated EGFR phosphorylation and activated the downstream ERK/CREB and PI3K/Akt/mTOR signaling pathway. Moreover, the results also showed that AG1478 abolished DP-induced relative protein activation and cell proliferation. When U0126 or LY294002 pretreated cells alone, DP-induced p-ERK or p-PI3K downstream proteins and cell proliferation were suppressed compared to those of the control group, but EGFR was not affected. In addition, ICG001 and BEZ235 collectively eliminated DP-induced fibroblast proliferation. Our findings suggest that DP-promoted fibroblast proliferation is stimulated by p-EGFR-induced activation of the ERK1/2-CREB and PI3K/Akt/mTOR pathways. Our present study explored the mechanism of DP-promoted fibroblast proliferation and provided a new basis for wound healing.
... Uma alternativa eficaz é a utilização de plantas medicinais para fins terapêuticos com eficácia no processo de cicatrização e com mínimos efeitos colaterais (BUDOVSKY; YARMOLINSKY; BEN-SHABAT, 2015), como é o caso do C. lechleri, que vem sendo utilizado empiricamente pela população indígena amazônica, desde o México até o Brasil (LORENZI;MATOS, 2008). Os principais constituintes dessa planta são taninos, lignanas e um alcaloide denominado taspina, a que se atribui a propriedade cicatrizante (LORENZI; MATOS, 2008 C. lechleri, planta nativa da região amazônica no Brasil e conhecida popularmente como Sangue de Dragão (GUPTA, 2008), têm em sua seiva uma alternativa para o tratamento de úlceras de diabéticos, pois esse recurso é utilizado em diversos países devido às diferentes ações já relatadas como cicatrizante (CAI et al., 1991;PIETERS et al., 1992;CHEN;PHILLIPSON, 1993;CHEN;PHILLIPSON, 1994;JONES, 2003;AZEVEDO et al., 2008), anti-hemorrágica (CAI et al., 1991;CHEN;PHILLIPSON, 1993), antimicrobiana (CHEN;PHILLIPSON, 1994), anti-inflamatória (RISCO et al., 2003), entre outras. ...
Inferior members ulcers are complications of Diabetes mellitus that demands a high coast to health’s services. The sap of Croton lechleri Müll. Arg. has demonstrated a huge potential for the treatment of wounds. The objective of this study was go along with chronic ulcers’ evolution in the inferior members in people with diabetes submitted to a three month treatment with ointment based on sap of C. lechleri. Field study, experimental, with quantitative approach, whose sample compound of four people. The data had been collected by means
of photographic registration, laboratorial exams and a semi-structured instrument. For the data analysis, it was used descriptive statistics. The ointment did not present antimicrobial effect; however, it was observed a reduction in the wound’s medium size. Additional analysis are required to determine a better formulation to treat different forms of wounds.
... C. lechleri displayed in vitro inhibition of the classical and alternative complement pathway and active T cell proliferation. C. lechleri suppressed the classical and alternative pathway with an inhibitory concentration (IC 50 ) of 5 and 185 μg/ml, compared to control's IC 50 of 33.7 μg/ml on the classical pathway (Risco et al., 2003). ...
To assess the possible clinical implication of Dragon's Blood in dermatology, a PubMed search was conducted using the keyword “Dragon's Blood,” “Croton lechleri,” and more. Dragon's Blood from C. lechleri is an Amazonian medicinal plant with a characteristic red sap. Its array of phytochemical action in preclinical studies include anti‐inflammatory, antioxidant, antimicrobial, antifungal, and antineoplastic properties. Clinical studies reflect wound healing and antiviral properties. Although its popularity is rising in western medicine, C. lechleri offers limited use in dermatology and further investigation is necessary to gain further insight into its potential clinical implication.
... Estos compuestos se detectaron en muy bajos niveles en las otras dos fracciones que permanecieron inactivas (n-hexano y cloroformo) (Tabla XIX), por lo que el papel de estos compuestos parece determinante en la actividad anticomplementaria evaluada. Este comportamiento de compuestos polifenólicos y flavonólicos ha sido referido para otros extractos de plantas 283,284 . Se ha informado que los grupos hidroxilo de los fenoles y flavonoides pueden actuar como aceptores para las enzimas C3b y C4b. ...
SINTESIS
El tamarindo (Tamarindus indica L.) es reconocido por su utilidad medicinal; sin embargo,
no todos los órganos de la planta han sido estudiados con igual profundidad. Sus hojas son
empleadas en el tratamiento de afecciones hepáticas e infecciosas, aunque no existen
evidencias científicas de su composición química y efectividad terapéutica que respalden
su uso etnobotánico. En el presente trabajo, se desarrolló un estudio fitoquímico de las
hojas de Tamarindus indica L., identificando un total de 35 metabolitos, 21 de los cuales
constituyeron un primer informe a nivel mundial. Las principales familias de compuestos
estuvieron representados por: aceites esenciales, ácidos grasos y compuestos polifenólicos,
principalmente flavonoides. La evaluación de las condiciones de extracción de las
sustancias activas permitió diseñar un método sencillo, económico y eficiente, que
combina la utilización de etanol al 70% como solvente y un tiempo de humectación de 90
minutos, para la obtención de extractos con elevadas concentraciones de metabolitos y una
fracción significativa de minerales, entre ellos el selenio. La caracterización de la
formulación (extracto fluido) preparada en estas condiciones, evidenció diferencias en las
concentraciones de los compuestos mayoritarios en las diversas etapas del ciclo de vida de
la planta, observando la mayor acumulación de metabolitos durante la fructificación. El
extracto fluido se fraccionó en cuatro preparados, de distinta polaridad y naturaleza
química, para la evaluación in vitro de su actividad antioxidante y antimicrobiana. Se
demostró que el extracto fluido posee una buena actividad antioxidante en los modelos in
vitro ensayados, en varios de ellos a concentraciones inferiores a sus fracciones. La
actividad antimicrobiana, por su parte, se asoció a la acción directa de los componentes
presentes en los extractos y no a la estimulación del sistema del complemento. Las dos
actividades farmacológicas estudiadas no dependieron exclusivamente de la concentración
de fenoles y flavonoides, como sugerían trabajos anteriores. Los resultados de la tesis
permiten relacionar por vez primera, el fitocomplejo en cuestión con la actividad
antioxidante y antimicrobiana que sustenta el empleo etnobotánico de las hojas de
Tamarindus indica L.
... 5 Dragon's blood is regarded as a natural medicine for improving blood circulation and reducing pain. 6 Research also showed that Dragon's blood possessed several pharmacological effects, including immunoregulatory, 7 anti-inflammation, 8 antidiarrheic, 9 antibacterial, 10 antiviral, 11 antioxidant, 12 and anticancer, 13 and so on. Interestingly, Dragon's blood can stimulate epithelial regeneration and wound healing by promoting fibroblasts proliferation and collagen synthesis. ...
In recent years, plant-derived extracts are increasing interest from researchers worldwide due to good efficacy and lower side effects. Among the different plant extracts, Dracorhodin perchlorate (DP) is originated from Dragon's blood which has long been used as a natural medicine with various pharmacological activities. In the present study, we have explored the potential regulation of DP on fibroblast proliferation which promotes wound healing both in vitro and in vivo. DP at treatment of 12-24 h significantly induced fibroblast proliferation which is associated with increasing level of phosphorylated-extracellular signal-regulated kinase (ERK). Moreover, if ERK is halted with siRNA, DP cannot induce fibroblast proliferation. In vivo, DP ointment treatment at low- (2.5 μg/mL), medium- (5 μg/mL) and high-(10 μg/mL) doses, rat wounds healed more rapidly compared with the control group. After DP treatment for 7 days, Serpin family H member 1 (SERPINH1) staining confirmed enhanced fibroblast proliferation in the wound tissue. Finally, phosphorylated-ERK in the wound tissue remarkably increased with DP ointment treatment. Therefore, DP may be developed into a potential lead compounds for the treatment of wounds in clinical trials in the near future.
... Our previous studies have demonstrated that DB could protect rat brain and gastrointestinal injury induced by different radiation sources [3-6]. Recent pharmacological researches have shown that DB has antithrombotic [7], anti-cerebral ischemia [8], anti-bacterial [9-11], anti-inflammatory [12][13][14], anti-diabetic [15,16], analgesic [17][18][19] and radio-protective activities [3,4,6], while it is also known to enhance immune function [20], promote blood circulation and stop bleeding [21,22]. ...
... Los resultados obtenidos al realizar el análisis cualitativo de metabolitos secundarios del látex de Croton lechleri, corroboran la presencia predominante de alcaloides, taninos, flavonoides, azúcares reductores y saponinas [39]. ...
The dermal healing activity and acute toxicity of Croton lechleri latex were evaluated using Wistar rats. The observation period to determine the healing activity was 7 days (d) and 14 d for the toxicity. Samples for histological evaluations were prepared 7 d after incised wound. The identification of chemical compounds present in the latex was performed by using gas chromatography coupled to mass spectroscopy. From histopathological analyses, in general, wounds of untreated rats and treated with the commercial cream showed abscesses with granulomatous inflammations, while the skins of rats treated with the latex of C. lechleri exhibited signs of repair. From evaluation of acute dermal toxicity, latex did not cause deaths or signs of toxicity in animals, at doses of 2000 mg/kg, body weight of the rats consistently increased, and no significant differences in mass balances (g/d) were observed between the groups of male and female rats, until the time of treatment with the latex. The latex has an acidic pH that produces an antimicrobial barrier during the healing process, inhibiting the growth of relevant bacterial pathogens. In addition, the organic compounds present in the dichloromethane extract of latex and identified by chromatographic analyses are mostly bioactive as anti-inflammatory, antimicrobial or fibroblast formation stimulation agents and their synergistic combination may explain the healing activity of latex of C. lechleri.
... Phytochemical studies of Croton species have identified the presence of terpenoids (Barreto et al., 2013;, alkaloids (Risco et al., 2003;Araújo-Junior et al., 2004), flavonoids (Zou et al., 2010;Barreto et al., 2013), triterpenes and steroids (Catalán et al., 2003;Maciel et al., 2006). These secondary metabolites are responsible for a wide variety of pharmacological activities against fungi and bacteria (Salatino et al., 2007;Carneiro et al., 2011). ...
... M: vulnerario, tónico, anti-estrés, astringente, antiséptico bucal, cutáneo y vaginal, inmunoestimulante, antiviral, antimicrobiano, antigonorreico, úlceras gastrointestinales, antihemorroidal, antidiarreico, antidisentérico, hepático, antihemorrágico, depurativo, febrífugo, dolencias postparto, afrodisíaco, antianémico, antitumoral, analgésico, E: anticáncer (Gonzales & Valerio, 2006;Montopoli et al., 2012;Alonso-Castro et al., 2013), antimalárico (Gutierrez et al., 2008), vulnerario, antiinflamatorio, antidiarreico (Jones, 2003;Pereira et al., 2010), inmunomodulador, antimicrobiano, antiviral (Williams, 2001;Risco et al., 2003), antioxidante (De Marino et al., 2008), antiulcerogénico (Risco et al., Boletin Latinoamericano y del Caribe de Plantas Medicinales y Aromáticas/217 antirreumático, antiinflamatorio, antialopécico, antidermatósico. 2005), hepatoprotector (Desmarchelier et al., 1999). ...
... M: vulnerario, tónico, anti-estrés, astringente, antiséptico bucal, cutáneo y vaginal, inmunoestimulante, antiviral, antimicrobiano, antigonorreico, úlceras gastrointestinales, antihemorroidal, antidiarreico, antidisentérico, hepático, antihemorrágico, depurativo, febrífugo, dolencias postparto, afrodisíaco, antianémico, antitumoral, analgésico, E: anticáncer (Gonzales & Valerio, 2006;Montopoli et al., 2012;Alonso-Castro et al., 2013), antimalárico (Gutierrez et al., 2008), vulnerario, antiinflamatorio, antidiarreico (Jones, 2003;Pereira et al., 2010), inmunomodulador, antimicrobiano, antiviral (Williams, 2001;Risco et al., 2003), antioxidante (De Marino et al., 2008), antiulcerogénico (Risco et al., Boletin Latinoamericano y del Caribe de Plantas Medicinales y Aromáticas/217 antirreumático, antiinflamatorio, antialopécico, antidermatósico. 2005), hepatoprotector (Desmarchelier et al., 1999). ...
This paper includes 50 taxa (species, subspecies, varieties, cultivars) of plants linked to the Andean context whose products are marketed for food and medicinal purposes in Metropolitan Buenos Aires-La Plata, Argentina. For each taxon its products are indicated, as well as its assigned uses and scientifically studied effects, in order to evaluate their correlation. Also, the products diffusion from the restricted ambit of the Bolivian immigrants segment (‘linked to traditions’ context) to the general commercial circuit (‘not traditional’ context) is discussed. Thereby, the dynamics of local botanical knowledge is assessed through the different products circulation.
... The optical density (OD) of the developed color was read on a microplate reader (Molecular Devices, Sunnyvale, CA, USA) at 570 nm. The results of the lymphocyte proliferation assay are presented as the proliferation index (PI) [PI = 100 · (OD stimulated culture -OD negative control culture )/ OD negative control culture ]. [12][13][14] Statistical analysis ...
Cordyceps militaris is a mushroom traditionally used for diverse pharmaceutical purposes in East Asia, including China, and has been found to be effective for enhancing immunity through various types of animal testing. The aim of this study is to determine the efficacy of C. militaris for enhancing cell-mediated immunity and its safety in healthy male adults. Healthy male adults were divided into the experimental group (n = 39), given 1.5 g/day of ethanol treated C. militaris in capsules, and the control group (n = 40), given the same number of identical placebo capsules filled with microcrystalline cellulose and lactose for 4 weeks from February 13 to March 14, 2012; the natural killer (NK) cell activity, lymphocyte proliferation index (PI), and T-helper cell 1 (Th1) cytokine cluster (interferon [IFN]-γ, interleukin [IL]-12, IL-2, and tumor necrosis factor [TNF]-α) were measured, along with stability test, at weeks 0, 2, and 4. The C. militaris group showed a statistically significant greater increase in NK200 (P = .0010), lymphocyte PI (P ≤ .0001), IL-2 (P = .0096), and IFN-γ (P = .0126), compared with the basal level, than the placebo group. There was no statistically significant adverse reaction. C. militaris enhanced the NK cell activity and lymphocyte proliferation and partially increased Th1 cytokine secretion. Therefore, C. militaris is safe and effective for enhancing cell-mediated immunity of healthy male adults.
... Dragon's blood is widely used as a folk medicine, and possesses antimicrobial (Rao et al., 1982), antiviral (Orozco-Topete et al., 1997), antitumor (Gonzales and Valerio, 2006), antihemorrhagic (Esmeraldino et al., 2005), immunomodulatory (Risco et al., 2003), antiulcer (Fischer et al., 2004), analgesic (Peres et al., 1998), antioxidative (Machala et al., 2001), anti-inflammatory (Miller et al., 2001) and antimutagenic (Saffi et al., 2004;Teng et al., 2011) activities. There are many source plants of dragon's blood, such as Croton, Dracaena, Daemonorops and Pterocarpus (Gupta et al., 2008). ...
Dragon's blood is a famous traditional Chinese medicine produced from source plants under bio- or abio-stress. Dracaena cochinchinensis (Lour.) S.C. Chen xylem (DX) is one of the most important sources of the medicine. In this work, a GC-MS method was developed for analysis of the n-hexane extracts of DX with resin (DXR) and without resin (DXW). The repeatability of the method was also investigated for a metabolite comparative study of the different xylems. About 80 components were detected, 26 of which were identified in both DXR and DXN. Three sesquiterpenes (τ-cadinol, τ-muurolon and α-cadinol) were first discovered in Dracaena cochinchinensis (Lour.) S.C. Chen. The chromatographs of the two plant materials were compared and differences of compounds were found. It showed that phytosterols showed a dramatic rise in content, and sesquiterpenes were found to be synthesized in DXR. Copyright © 2015 John Wiley & Sons, Ltd.
Copyright © 2015 John Wiley & Sons, Ltd.
... The immunomodulatory activity of SD was proposed to involve inhibition of both classical (CP) and alternative (AP) pathways of complement system as well as proliferation of activated T-cells [7], suggesting that SD might be able to inhibit autoimmune diseases. In fact, recent studies have shown that SD is effective in reducing glycemia and increasing insulin sensitivity in diabetic rats [8,9]. ...
Sanguis draxonis (SD), also known as "Dragon's Blood", is a traditional herb medicine that has been used to treat a variety of complications with unknown mechanisms. Recent studies show that SD displays immunosuppressive activities and improves symptoms of type I diabetes in animal models. However, the mechanisms underlying SD's immunosuppressive actions are not completely understood. The voltage-gated Kv1.3 channel plays a critical role in the pathogenesis of autoimmune diseases by regulating the functions of both T cells and B cells. Here we investigated the effect of SD and one of its active components loureirin B (LrB) on Kv1.3. Both SD and LrB inhibited Kv1.3-mediated currents, produced a membrane depolarization, and reduced Ca(2+) influx in Jurkat T cells. In addition, application of LrB inhibited phytohemagglutinin (PHA)-induced IL-2 release from activated Jurkat T cells. Furthermore, point mutations in the selective filter region significantly reduced the inhibitory effect of LrB on Kv1.3. The results of these experiments provide evidence that LrB is a channel blocker of Kv1.3 by interacting with amino acid residues in its selective filter region. Direct inhibition of Kv1.3 in T cells by SD and LrB might be the cellular and molecular basis of SD-mediated immunosuppression.
... Phagocytosis Evaluation by Flow Cytometry. The phagocytosis assay was carried out following a modification of the method described by Risco et al. 27 A suspension (5.5 × 10 7 particles/mL) of fluorescent microspheric hydrophilic particles (2 μm in diameter) of modified carboxylate with a yellow-green fluorescence (505/515 nm), and opsonized using human serum (30 min at 37°C), were used for the phagocytic test. ...
The aim of the present study was to investigate the in vitro activity of fifteen essential oils, four essential oil fractions and three pure compounds (thymol, carvacrol and eugenol) on phagocytosis by human neutrophils and on complement system. Samples were characterized by GC and GC-MS. Most of the oils (nutmeg, clove, niaouli, tea tree, bay laurel, lemon, red thyme, ginger), nutmeg terpenes, eugenol and carvacrol showed mild to moderate inhibition of phagocytosis (25-40% inhibition at doses ranging from 40 µg/mL to 60 µg/mL); highest inhibitory activity was found for thymol (72% at 56 µg/mL), whereas the mixture of bornyl and isobornyl acetates showed a mild stimulating activity (21% at 56 µg/mL). All samples were inactive in the alternative pathway of complement system, whereas on classical pathway, clove oil, eugenol, palmarosa oil, red thyme oil, tarragon oil and carvacrol showed the highest activity, with IC50 ranging from 65 µg/mL to 78 µg/mL.
... The results of the lymphocyte proliferation assay are presented as the proliferation index (PI) [PI = 100 × (OD stimulated culture − OD negative control culture)/OD negative control culture] (Risco et al., 2003;Manosroi et al., 2003). ...
The study of the human immune response to hepatitis B virus (HBV) has been hampered by the lack of an adequate model to evaluate the hepatitis B surface antigen (HBsAg) specific cell response. Thus, this study was conducted to perform an in vitro analysis of the antigenic properties of recombinant HBsAg and demonstrate the influence of variables such as culture time, antigen concentration and cell density on lymphocyte proliferation. Peripheral blood mononuclear cells (PBMCs) were isolated from the venous blood of vaccinated individuals, and in vitro cellular immune responses were evaluated using an HBsAg-specific proliferation assay. Lymphoproliferative responses were detected in culture systems, despite the lack of serum antibodies. Optimal results were obtained when lymphocytes were stimulated at a seeding density of 4×10(6) cells/mL, with 50ng/mL of recombinant HBsAg protein vaccine for 3 days. Data from the present study may contribute to the development of an adequate system to evaluate the cellular immune responses to HBsAg in vaccine recipients.
... The colorimetric method of MTT reduction can be used to measure cytotoxicity, proliferation and even cell activation, since the determination of the activity of mitochondrial dehydrogenase of living cells directly and proportionally represents the number of cells (Mosmann, 1983). The results were presented as a percentage of growth, according to Manosroi, Saraphanchotiwitthaya and Manosroi (2003) and Risco et al. (2003), through equation 1. This indicator eliminates the residual reduction of MTT by cells not exposed to the extract or mitogen, as well as the background color of the methanol extract and the inter-assay variations. ...
A number of natural compounds have been used as immunomodulatory agents, enabling the function of the immune system to be modified by stimulating or suppressing it. There has been increasing interest in the study of therapeutic action of plant extracts regarding their immunomodulatory activity. The aim of this study was to identify and evaluate the action of extracts of the medicinal plants Calophyllum brasiliense, Ipomoea pes-caprae, Matayba elaeagnoides, Maytenus robusta, Rubus imperialis and Vernonia scorpioides on the development of spleen cells from mice, using the in vitro cellular proliferation assay. The cells, obtained by mechanical rupture of mice spleen (5x104 cells/mL), were incubated with methanol extracts (10, 50, 100 and 200 µg/mL) and phytohemagglutinin (PHA, 5 µg/mL). The basal control for proliferation consisted of cells alone, while the positive control consisted of cells and PHA. The cell culture was kept at 37 ºC in 5% CO2 for 72 hours, and cell proliferation was revealed by the blue tetrazolium reduction assay (MTT). The results were expressed as percentage of growth and were analyzed using the Kruskal-Wallis and Mann-Whitney tests. The C. brasiliense, I. pes-caprae and M. elaeagnoides extracts showed dose-dependent induction of cell proliferation, with a significant increase in cell proliferation (p<0.03) and percentage growth of 88.2%, 73.1% and 52.7%, respectively, suggesting T lymphocyte stimulation. By contrast, M. robusta, R. imperialis and V. scorpioides extracts showed significance only with a negative percentage of growth, suggesting inhibition of cell proliferation (p<0.04). Further biomonitoring studies will enable the fractions and isolated substances responsible for the immunomodulatory activities to be identified.
... The pH of the sap from Croton lechleri was 3.9 and the density was 1.08 g/mL according with the literature data (Risco et al., 2003). The chemical characterization has been performed through the determination of the alkaloid taspine as previously reported (Froldi et al., 2009). ...
Ethnopharmacological relevance:
Croton lechleri Mull. Arg. (Euphorbiaceae) is a traditional medicinal plant which produces a red sap, traditionally known as "Sangre de Drago"; it is used in folk medicine externally for wounds, fractures, and haemorrhoids, internally for intestinal and stomach ulcers and also for the empirical cure of cancers.
Materials and methods:
We investigated the effects of Croton lechleri sap and taspine in comparison with taxol and vinblastine on the growth of human cancer cell lines of SK23 (melanoma), LoVo and HT29 (colorectal cancer) using MTT and Trypan blue assays. Further, we studied cell cycle by flow cytometry and detected acetylated-α-tubulin by confocal microscope.
Results:
Croton lechleri inhibited cell proliferation starting from 1 μg/mL in SK23 cells, whereas 10 times higher concentrations were required for growth inhibition of HT-29 and LoVo cell lines. Also taspine (0.1 μg/mL) inhibited the SK23 and HT29 cell proliferation. Further, assay was assessed on SK23 and HT29 cell lines with 24-48 h treatment with sap and taspine. Both sap and taspine inhibited cancer cell proliferation; taspine showed higher activity on SK23 cells, which was significantly increased after 48 h of SK23 treatment. Using confocal microscopy we observed that Croton lechleri (1 μg/mL) caused a loss of microtubule structure, whereas taspine (0.5 μg/mL) caused an increase in acetylated α-tubulin and a modification of cellular morphology, mainly in SK23 cells. Croton lechleri sap 10 and 50 μg/mL influence cell cycle; 50 μg/mL sap caused a dramatic reduction of cells in G(1)/G(0) and S phases with a great increase of subG(0) cells.
Conclusions:
The data showed that Croton lechleri and taspine could inhibit cell proliferation with higher potency against melanoma SK23 cells, supporting the empirical use of the sap as anticancer in ethnomedicine and taspine as a possible anticancer agent.
Objectives This study aimed to evaluate the effect of Croton lechleri on alveolar preservation, focusing on density, dimensions, epithelial regeneration, and pain scale.
Materials and Methods This pilot randomized clinical trial included 20 patients aged 35 to 56, divided into two groups: Group A (experimental) and Group B (control). Both underwent atraumatic dental extractions in the anterior maxilla. Group A received C. lechleri in the alveolus post-extraction, while Group B received no treatment. Patients with <25% buccal wall loss and defects <3 mm were randomized using block randomization via Jamovi software. Assignments were sealed in opaque envelopes and revealed after data collection. Cone-beam computed tomography and clinical analyses were conducted over 4 months.
Statistical Analysis For the statistical analysis of tomographic data, an analysis of variance test for repeated measures was used, followed by a post hoc Tukey test. The clinical data analysis was conducted using a Student's t-test.
Results Exploratory findings from this pilot study revealed a statistically significant effect on bone density (p = 0.03). Although reduced bone loss was noted with the use of C. lechleri extract, the experimental group demonstrated better outcomes in terms of preserving dimensional changes. Furthermore, patients in the experimental group required fewer analgesics during the first 72 hours (p = 0.01), suggesting a significant effect on the clinical pain management protocol and a potential positive effect of C. lechleri on alveolar preservation. In this study, no adverse effects were observed. Regarding the epithelial regeneration parameters, no differences were noted in the color of the scar tissue at 72 hours (p = 1.00). Croton lechleri appears to accelerate the bone repair process, allowing for the formation of higher quality bone in terms of density.
Conclusion This study demonstrates that the use of C. lechleri is viable for improving bone density, providing better pain control, and achieving favorable epithelial healing. However, larger studies are necessary to confirm these findings.
C. lechleri, known as "Sangre de Drago", is an ethnomedicinal resource widely used in the Amazon region, presenting several properties, such as wound healing activity, anti-inflammatory and antitumor effects, among others. However, the scope of its scientific studies carried out in the last 20 years lacks a comprehensive review, in order to inform readers and researchers about the current state of the art on the chemical and pharmacological theme of the species. Using databases such as Scopus and Google Scholar, 33 articles on the themes of phytochemistry and recent pharmacological studies were found, which, in turn, report proanthocyanidins as the main phytochemical group in relative quantity, in addition to the presence of alkaloids, diterpenoids, phytosteroids, saponins, phenolics and polyphenolics as other groups of phytochemical importance. The studies also describe the healing, antitumor, anti-inflammatory, gastrointestinal, and other potential effects of C. lechleri, which demonstrate the notable medicinal importance of the species today.
Phytotherapy is a discipline which rigorously studies the treatment of diseases through the use of medicinal plants or their by-products. Based on this discipline and considering the importance of treating wounds and ulcers, the purpose of our propaedeutic study is to contribute to the development of competencies in the management of medicinal plants in the healthcare’s field. Therefore, our aims are the following ones: (1) to select the most important vulnerary species from a propaedeutic and transdisciplinary vision; (2) to provide a practical comparative overview of the selected species; (3) to consider and value the cultural importance of plants which still are recollected in the country; (4) to select a traditional plant in order to be used by healthcare personnel and (5) describe its scientific evidence, pharmacological action, use and instructions for use. After a comprehensive search in the main databases and academic search engines with information of portals and guides of recognized prestige, the selected species are presented in two blocks. The former is a synthesis of the interesting commercial plants according to the purpose and aims described: the Balsam of Peru, the Shepherd's purse, the Calendula or Pot-Marigold, the Oak, the Sweetbriar rose and the Dragon´s blood according to their pharmacological action. In the second block a descriptive analysis of the St. John's Wort (Hypericum perforatum) is carried out due to its cultural importance as a wound healing plant in the rural communities of a big part of Spain.
Keyboards: Phytotherapy, Ethnomedicine, scientific evidence, ulcer, wounds, Continuing Education for health professionals
Deep vein thrombosis (DVT) is a common complication following traumatic fracture with a 0.5%–1% annual incidence. Low molecular weight heparin (LMWH) is the most commonly used anticoagulation drug for DVT prevention, but treatment with LMWH is invasive. Our aim is to compare the antithrombotic effect of dragon’s blood, an oral botanical anticoagulant medicine approved by the Chinese FDA, with LMWH in patients undergoing hip fracture surgery and to explore the molecular mechanisms of anticoagulation treatment. Our study recruited patients and divided them into LMWH and dragon’s blood treatment group. Coagulation index tests, Doppler ultrasound and mRNA sequencing were performed before and after anticoagulation therapy. There was no significant difference in postoperative DVT incidence between the two groups (23.1% versus 15.4%, P=0.694). D-dimer (D-D) and fibrinogen degradation product (FDP) showed significant reductions in both groups after anticoagulation treatments. We identified SLC4A1, PROS1, PRKAR2B and seven other genes as being differentially expressed during anticoagulation therapy in both groups. Genes correlated with coagulation indexes were also identified. Dragon’s blood and LMWH showed similar effects on DVT and produced similar gene expression changes in patients undergoing hip fracture surgery, indicating that dragon’s blood is a more convenient antithrombosis medicine (oral) than LMWH (hypodermic injection).
Our previous research revealed resin of Dracaena cochinchinensis as a candidate for therapy of neurodegenerative diseases. In the present study, the material basis of Chinese Dragon’s blood and the primary mechanism of the effective components are discussed. Multiple chromatography and spectra analysis were utilized to identify effective constituents. The production of NO was determined using nitrite assay in BV-2 microglial cells stimulated with lipopolysaccharide (LPS). Cell viability was tested using MTT assay. The mRNA level of inducible nitric oxide synthase (iNOS) was investigated by quantitative real-time PCR (qRT-PCR), and the production of IL-6 and TNF-α in the cell supernatants was tested by ELISA. The bioassay-directed separation of the effective extract of D. cochinchinensis afforded two new compounds, a stilbene-flavane dimer (2) and a quinoid flavonoid (11), in addition to 25 known compounds. The evaluation of their anti-neuroinflammatory activities showed that 5, 9, 12, 13, and 14 could exhibit significant anti-neuroinflammatory effects without cytotoxities at the tested concentration, compared to a positive control, minocycline (21.87 ± 2.36 µM). A primary mechanistic study revealed that the effective components could inhibit over-activation of microglial through decreasing the expressions of iNOS, proinflammatory cytokines IL-6 and TNF-α in LPS- induced BV2 microglial cells. Chalcone 9, homoisoflavane 5 and flavone 12–14 are considered to be responsible for the anti-neuroinflammatory effects of Chinese Dragon’s blood. These could inhibit neuroinflammation by reducing the expressions of iNOS, IL-6 and TNF-α in over-activated microglial. Furthermore, the SAR is briefly discussed.
The present study examined the impacts of sodium acetate (SA), sodium acid pyrophosphate (SAPP), and citric acid (CA) on the viability, proliferation, and DNA damage of isolated lymphocytes in vitro. 3‐(4,5‐Dimethylthiazol‐2‐yl)‐2,5‐diphenyl tetrazolium bromide (MTT) and lactate dehydrogenase (LDH) release assays were adopted to evaluate cell viability, while comet assay was employed to assess the genotoxic effects. The cells were incubated with different levels of SA (50, 100, and 200 mM), SAPP (25, 50, and 100 mM/L), or CA (100, 200, and 300 μg/mL). The lymphocytes treated with the tested food additives showed concentration‐dependent decreases in both cell viability and proliferation. A concentration‐dependent increase in LDH release was also observed. The comet assay results indicated that SA, SAPP, and CA increased DNA damage percentage, tail DNA percentage, tail length, and tail moment in a concentration‐dependent manner. The current results showed that SA, SAPP, and CA are cytotoxic and genotoxic to isolated lymphocytes in vitro.
The species Synadenuium umbellatum belongs to the Euphorbiaceae family and is widely found in South America and popularly known in Brazil as “cola-nota”, “avelós”, “cancerola” or “milagrosa”. The latex collected from this plant is empirically used as an aqueous solution for treatment of several purposes including anti-inflammatory and antimicrobial properties. The objective of this study was to investigate the effect of the crude latex in the bacterial culture and in the phagocytic properties of macrophages against yeast Saccharomyces cerevisiae. To evaluate the antimicrobial activity, we tested the effect of crude latex from S. umbellatum against four bacterial strains: Staphylococcus aureus, Escherichia coli, Pseudomonas aeruginosa and Klebsiella pneumoniae. Cytotoxicity assay was performed in peritoneal macrophages by MTT reduction assay. Phagocytic assay was undertaken in macrophages incubated with yeast and latex. After incubation period, the cells were stained and the yeast forms from S. cerevisiae inside macrophages were counted, and the phagocytic index (PI) determined. The results demonstrated that the crude latex was not effective against the bacterial strain tested. When the latex was tested in murine peritoneal macrophages, we observed a time and concentration-dependent cytotoxicity when compared with control. To test the activity to the latex in phagocytosis, we used the concentrations that did not induce toxicity in the macrophages. Interestingly, we observed an improved phagocytic capacity in the cells incubated with three latex titration (LT) (Control, PI=4.9±0,23; LT1:30, PI=9.8±3; LT1:60, LTPI=9.5±3; LT1:120, PI=22.3±1,0; n=4). The results showed that S. umbellatum presents a concentration-dependent cytotoxicity and promotes an improved phagocytic capacity in macrophages. Despite the latex not presenting a direct antibacterial activity against bacterial strains tested, the results suggest that components present in the latex could trigger an improved inflammatory response against infection agents by stimulating the macrophages phagocytic properties. © 2018 International Society for Horticultural Science. All Rights Reserved.
It is estimated that there are as many as 1400 plant species currently used in traditional Peruvian medicine; however, only a few have undergone scientific investigation. In this paper, we make a review of the botanical, chemical, pharmacological and clinical propierties of the most investigated Peruvian medicinal plants. The plant species selected for this review are: Smallanthus sonchifolius (yacon), Croton lechleri (sangre de grado), Uncaria tomentosa/U. guianensis (una de gato), Lepidium meyenii (maca), Physalis peruviana (aguaymanto), Minthostachys mollis (muna), Notholaena nivea (cuti-cuti), Maytenus macrocarpa (chuchuhuasi), Dracontium loretense (jergon sacha), Gentianella nitida (hercampuri), Plukenetia volubilis (sacha inchi) and Zea mays (maiz morado). For each of these plants, information about their traditional uses and current commercialization is also included.
The bioactive ethyl acetate phase obtained from the latex of Croton urucurana Baillon afforded a novel orbitide (1), [1-9-NαC]-crourorb A1, that proved active against NCI-ADR/RES (ovary, multidrug-resistance phenotype) cells with the same potency as doxorubicin (positive control) and inactive up to the highest concentration tested against nontumor NIH/3T3 cells. The structure elucidation was based on 1D and 2D NMR spectroscopy, further supported by HRESIMS data and by application of Marfey's method for determination of the absolute configuration of its amino acid residues. This is the first orbitide obtained from C. urucurana.
The n-hexane extract of the stem bark of Croton anisodontus yielded 2-hydroxy-3,4,6-trimethoxyacetophenone, a well-known substance, but isolated from this species for the first time. The antimicrobial and modulatory activities of the compound towards Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus, Candida albicans, C. krusei and C. tropicalis strains were assessed. Antibiotics such as amikacin, gentamicin and neomycin were used in a sub-inhibitory concentration. Significant activity was observed towards P. aeruginosa and S. aureus 358, with p < 0.001 in association with amikacin. The present results place C anisodontus as an alternative source of 2-hydroxy-3,4,6-trimethoxyacetophenone with antibacterial potential.
Croton membranaceus is used by Ghanaian traditional medical practitioners in the treatment of benign prostatic hyperplasia (BPH). Preparations of the root of this plant have been observed to relieve symptoms of BPH and enhance urination without the accompanying difficulty. There are no observable adverse effects associated with the clinical use of preparations of C. membranaceus. While medicinal significance has generated scientific interest in the plant there is real concern relative to the longer tem availability of this indigenous plant in its natural habitat. The objective of this review is to highlight the prospects of C. membranaceus for prostate health.
Croton caudatus Geiseler is widely used in Manipur, India and its neighbouring areas for the treatment of various ailments including cancer without considering the genotoxic effects. In an attempt to determine whether the aqueous extract of the plant leaves interact with genetic material both somatic and germinal were cytogenetically assayed. Mice which received intraperitoneal injection of the leave extract showed chromosome aberrations, abnormal chromosome behaviour and synaptonemal complex damages indicating their clastogenic potentials.
An offline two-dimensional RP/RPLC system was developed for the separation of components in Dracaena cochinchinensis (Lour.) S.C.Chen xylem containing a resin that is an important raw material in Chinese traditional medicine. In this separation
method, a CN-column was used in the first dimension and a C18-column in the second dimension. Fractions collected from the CN-column were resolved into many additional components, which
indicated that the two-dimensional RP/RPLC system based on the CN- and C18-columns is orthogonal. The method provides higher peak capacity and better resolution. It is suitable for the analysis of
complex samples such as those found in traditional Chinese medicines.
SP-303, a large proanthocyanidin oligomer isolated from the latex of the plant species Croton lechleri (Eupborbiaceae) has demonstrated broad activity against a variety of DNA and RNA viruses. In cell culture, SP-303 exhibits potent activity against isolates and laboratory strains of respiratory syncytial virus (RSV), influenza A virus (FLU-A) and parainfluenza virus (PIV). Parallel assays of SP-303 and ribavirin showed comparable activity against these viruses. SP-303 also exhibits significant inhibitory activity against herpesvirus (HSV) types 1 and 2, including herpesviruses resistant to acyclovir and foscarnet. Inhibition was also observed against hepatitis A and B viruses. The antiviral mechanism of SP-303 seems to derive from its direct binding to components of the viral envelope, resulting in inhibition of viral attachment and penetration of the plasma membrane. Antiviral effects of SP-303 were measured by three distinct methods: CPE, MTT and precursor uptake/incorporation. Cytotoxicity endpoints were markedly greater than the respective antiviral endpoints. SP-303 exhibited activity in RSV-infected cotton rats and African green monkeys, PIV-3-infected cotton rats, HSV-2 infected mice and guinea pigs and FLU-A-infected mice. The most successful routes of SP-303 administration for producing efficacy were: topical application to HSV-2- genital lesions in mice and guinea pigs, aerosol inhalation to FLU-A-infected mice and PIV-3-infected cotton rats, and oral dosage to RSV-infected cotton rats. A variety of toxicological evaluations demonstrated the safety of SP-303, particularly orally, which was predictable, since condensed tannins are a common dietary component. It is notable that the larger proanthocyanidins as a class have high antiviral activity, whereas most of the monomers are inactive. Clinical trials are ongoing to evaluate SP-303 as a therapeutic antiviral agent.
Sangre de grado is an Amazonian herbal medicine used to facilitate the healing of gastric ulcers and to treat gastritis, diarrhea, skin lesions, and insect stings. This study was designed to evaluate the gastrointestinal applications. Gastric ulcers were induced in rats by brief serosal exposure of the fundus to acetic acid (80%). Sangre de grado was administered in drinking water at 1:1,000 and 1:10,000 dilutions from the postoperative period to day 7. Guinea pig ileum secretory responses to capsaicin, electrical field stimulation, and the neurokinin-1 (NK-1) agonist [Sar(9),Met(O(2))(11)]substance P were examined in Ussing chambers. Sangre de grado facilitated the healing of experimental gastric ulcer, reducing myeloperoxidase activity, ulcer size, and bacterial content of the ulcer. The expression of proinflammatory genes tumor necrosis factor-alpha, inducible nitric oxide synthase (iNOS), interleukin (IL)-1beta, IL-6, and cyclooxygenase-2 was upregulated by ulcer induction but reduced by sangre de grado treatment, particularly iNOS and IL-6. In Ussing chambers, sangre de grado impaired the secretory response to capsaicin but not to electrical field stimulation or the NK-1 agonist. We conclude that sangre de grado is a potent, cost-effective treatment for gastrointestinal ulcers and distress via antimicrobial, anti-inflammatory, and sensory afferent-dependent actions.
The antioxidant properties of the wild growing sage species, Salvia reflexa Hornem., were investigated. The presence of superoxide (O(2)(.-)) and hydroxyl ((.)OH) radicals, malonyldialdehyde (MDA), reduced glutathione (GSH) and total flavonoids were observed in the above-ground parts of plant, as well as activities of the antioxidant enzymes superoxide-dismutase (SOD) and peroxidase (P-ase). The potential antioxidant activity of the methanol:water extract has been assessed based on scavenging activity of stable DPPH free radicals. By the means of TLC and LC/MS a screening for secondary plant products was performed. Significant quantities of O(2)(.-), (.)OH and MDA were observed. Thus, this species exhibited high SOD and P-ase activities as well as a content of total flavonoids. The dominant naturally occurring compound was rosmarinic acid. The results obtained suggested a high antioxidant activity of Salvia reflexa Hornem.
Sangre de Drago is a red viscous latex extracted from Croton lechleri (Euphorbiaceae) cortex, renowned in South American popular medicine for its wound-healing properties. The in vitro antiproliferative effects were determined on the human myelogenous leukemia K562 cells line (IC50 = 2.5 +/- 0.3 microg ml(-1)). The mutagenic and antimutagenic activity of C. lechleri sap was examined by means of the Ames/Salmonella test. No mutagenic activity was found on the Salmonella typhimurium strains T98 and T100, either with or without S9 activation. On the other hand, the sap showed an inhibitory effect against the mutagenic activity of the indirectly acting mutagen 2-Aminoanthracene in presence of S9 and a moderate protective activity against directly acting mutagens Sodium Azide and 2-Nitrofluorene. Therefore we suggest that C. lechleri sap interacts with the enzymes of the S9 mix, thereby inhibiting the transformation of 2-Aminoantracene into its active forms.
The wound healing activity of dragon'sblood (Croton spp.), in Spanish 'sangre de drago‛ or 'sangre de grado‛, a traditional South American drug, and some of its constituents, including the alkaloid taspine (1), the dihydrobenzufuran lignan 3',4-O-dimethylcedrusin (2) and proantho-cyanidins, was evaluated in vivo on rats, and compared with the wound healing actitivy of synthetic proanthocyanidins. The beneficial effect of dragon's blood on wound healing was confirmed. Dragon's blood stimulated contraction of the wound, formation of a crust, formation of new collagen, and regeneration of the epithelial layer. 3',4-O-Dimethylcedrusin also improved wound healing in vivo by stimulating the formation of fibroblasts and collagen, but crude dragon's blood was more effective. This was due to the proanthocyanidins, present in dragon's blood, which stimulate contraction of the wound and precipitate with proteins forming a dark crust covering the wound, but which delay wound repair by a decreased formation of new fibroblasts.
The blood-red sap of Croton lechleri was found to contain proanthocyanidins as major constituents which accounted for up to 90% of the dried weight. In addition to (+)-catechin, (−)-epicatechin, (+)-gallocatechin, (−)-epigallocatechin and dimeric procyanidins B-1 and B-4, five novel dimers and trimers were isolated and characterized as catechin-(4α→8)- epigallocatechin, gallocatechin-(4α→8)-epicatechin, gallocatechin-(4α→6)-epigallocatechin, catechin-(4α→8)- gallocatechin-(4α→8)-gallocatechin and gallocatechin-(4α→8)-gallocatechin-(4α→8)-epigallocatechin. Higher oligomers were also obtained. A new procedure combining chemical degradation with 1H NMR spectroscopy has been developed for determination of the composition and molecular size of oligomeric/polymeric proanthocyanidins. The oligomers of the sap were shown to have the mean degree of polymerization of 4,5–6 and 6–7, respectively, and Mr up to 2130. The heterogeneity of the oligomers was clearly indicated by the presence of a variety of flavan-3-ols as extension and terminal units. An exceptionally high content of gallocatechin and epigallocatechin in the oligomers was observed.
Croton lechleri L. (Euphorbiaceae), a plant from the Upper Amazon Valley of Peru, yielded the alkaloid taspine. The anti-inflammatory activity of taspine hydrochloride was studied using the carrageenan-induced pedal edema method, the cotton pellet-induced granuloma method, and the adjuvant polyarthritis model.
Ligaria cuneifolia (R. et P.) Tiegh. is an hemiparasite species used in Argentine folk medicine as a substitute for the European mistletoe (Viscum album L.) based on its putative activity of decreasing high blood pressure. This paper analyzes flavonoid composition, protein constituents and the possible immunomodulatory and antitumoral effects of this species. Micromolecular study disclosed quercetin-free, quercetin-glycosylated and proanthocyanidins corresponding to cyanidin monomers, which implies a particular metabolic pathway. Proteins present in L. cuneifolia extracts analyzed by SDS-PAGE presented multiple bands with molecular weights ranging from 14 to 90 kD. These features contribute to the characterization of the native mistletoe. As V. album is being used in cancer treatment due to its immunomodulatory and antitumoral activity, the action of aqueous L. cuneifolia extracts on murine lymphocytes was investigated. Culture of murine spleen cells alone or stimulated with Concanavalin A or lipopolysaccharide in presence of L. cuneifolia extracts indicated a certain stimulation of splenocytes alone and an inhibition of splenocytes stimulated with Concanvalin A or lipopolysaccharide. An inhibitory effect was also observed on the proliferation of murine leukemia cells. In addition, aqueous extracts increased nitric oxide production by murine macrophages. These results suggest that L. cuneifolia extracts exert an immunomodulatory effect on the mouse immune system.
We developed a simple flow cytometric assay for phagocytosis by human monocytes that is mediated via Fc gamma receptors and the complement receptor CR1 (CD35), using fluorescent latex beads carrying IgG and complement components C4b and C3b. To prepare fluorescent latex beads carrying IgG(BA), BSA-coated latex beads (B) were incubated with diluted rabbit anti-BSA IgG. To bind complement components, BA-particles were incubated with whole human serum pretreated with K-76 monocarboxylic acid (K-76COOH). K-76COOH inhibits the activities of C5 and factor I (12,13), resulting in the deposition of C1,4b,2a,3b on BA-particles (BAC1,4b,2a,3b). Further incubation of BAC1,4b,2a,3b with EDTA-GVB at 37 degrees C gave particles carrying IgG and C4b,C3b (BAC4b,3b). The C3 fragment, C3b, was confirmed to present on BAC1,4a,2a,3b particles by SDS-PAGE and immunoblot, and these particles were calculated to have approximately 25,000-30,000 C3b molecules per particle. To evaluate the particle attachment, the phagocytic assay was performed with 3 microM cytochalasin D treated cells. The percent cells with ingested particles and the number of ingested particles/100 cells for 60 min were estimated, being 5.1% and 5.4 for B, 12.3% and 26.7 for BA, 42.5% and 108.7 for BAC4b,3b, and 42.6% and 112.5 for BAC1,4b,2a,3b, respectively.
A sensitive colorimetric microassay for determining haemolytic complement activity was devised. It is carried out in U-welled microtitre dishes covered with plastic tape, which are incubated in a waterbath and subsequently centrifuged. The supernatant is transferred to flat-bottomed microtitre dishes and haemolysis is estimated by automatic measuring of the absorption using an interference filter of 405 nm in a Titertek Multiskan. Advantages of the method described are saving time and materials, and avoiding the use of radioactive nuclides. This microassay may therefore be a useful substitute for macro and semi-micro tests for colorimetric determination of serum complement activity and for microassays based on the release of a radio-isotope.
It has been shown that low concentrations of E. coli lipopolysaccharides (LPS) greatly and selectively stimulate phagocytosis and related functions in mouse bone marrow-derived macrophages. Culture in the presence of 50 ng/ml LPS induced on average a 10-fold enhancement of phagocytosis of IgG-coated sheep erythrocytes. Activation was in two stages--a small increase observed during the first 8 to 12 hr, and the major increase noted between 16 and 24 hr. Phagocytic activity remained at the maximal level for 24 hr and then declined progressively. Stimulation by LPS was dose-dependent; significant effects could be observed at 0.8 ng/ml and the maximum was reached at 10 ng/ml. LPS-treated cells also showed a markedly increased tendency to form colonies. All these effects could be prevented by the addition of 100 ng/ml polymyxin B together with LPS, indicating that the active principle is lipid A. The LPS-dependent increase in phagocytic activity is probably mediated by increased Fc receptor capacity because both parameters were influenced in parallel by the stimulus. Phagocytosis-related events, such as enhanced hexose monophosphate shunt activity, H2O2 formation, and nitroblue tetrazolium reduction were also stimulated by LPS. By contrast, pinocytosis was unaffected. Measurements of cell-associated enzyme activities showed that lactate dehydrogenase, acid phosphatase, and cathepsin D were significantly increased. Beta-glucuronidase, beta-galactosidase, alkaline phosphodiesterase, and aminopeptidase were unchanged and NAD nucleosidase was markedly decreased after LPS treatment. 5'-Nucleotidase and glucosamine uptake were undetectable both in control and LPS-stimulated cells. LPS treatment induced a significant increase in cell-associated protein, but did not result in cell proliferation or increased cell loss as shown by the DNA content that remained constant. LPS-induced changes were dependent on de novo protein synthesis; cycloheximide prevented enhancement of phagocytosis, Fc receptor capacity, and colony formation.
The phagocytosis of uniform fluorescent latex particles by pulmonary macrophages in the rat was analyzed by flow cytometric methods. The percentage of phagocytic macrophages and the number of particles per cell were determined from cell-size and fluorescence histograms. A comparison of in vivo and in vitro phagocytosis data showed that the percentage of phagocytic lavaged macrophages reflected the availability of instilled particles. With sodium azide used to model phagocytosis inhibition, it was shown that the percentage of phagocytic cells and the number of particles per cell can be determined simultaneously.
Three in-vitro assays have been adopted to examine the cytotoxicity and anti-bacterial activity of the blood-red sap of Croton lechleri from Ecuador, and to examine its effect upon the proliferation of endothelial cells. The sap was found not to be cytotoxic. Several simple phenolic compounds and diterpenes showed a potent anti-bacterial activity. The sap has little effect upon the proliferation of endothelial cells, and no single active ingredient was identified. A mechanism for the wound-healing property of the sap has been proposed.
The phenolic biopolymer SP-303 was evaluated against experimentally induced influenza A (H1N1) virus infections in mice in a series of experiments. When 30, 10 or 3 mg/kg/day of SP-303 were administered intraperitoneally once daily for 8 days beginning either 48 h before or 4 h after virus exposure, only lung consolidation was significantly reduced; extended (p < 0.01) mean day to death was also seen in the late-therapy groups. The high dosage was lethally toxic in this experiment. A small-particle aerosol (SPA) of 10, 5 and 2.5 mg/ml of SP-303, administered for 1 h three times daily for 5 days beginning 4 h after virus exposure, exerted a similar antiviral effect. Twice-daily 1-hour SPA treatments for 3 days beginning 24 h before virus exposure using 4.3 mg/ml of SP-303 resulted in significant increases in mean day to death and reductions of lung consolidation but no inhibition of lung virus titer. Declines in influenza-induced arterial oxygen saturation, as determined by pulse oximetry, were less in all animals treated with SP-303 by SPA, but this reduced decline was significant (p < 0.01) only in the last experiment. Mice receiving SP-303 by SPA exhibited consistent but reversible hypothermia immediately after termination of treatment.
Pluchea sagittalis, (Lam.) Cabr., a popular medicinal herb grown in South America, was studied for anti-inflammatory and antioxidant activities. The anti-edema action of P. sagittalis aqueous extract was assayed in different models of inflammation: 1) the mouse ear edema test induced by arachidonic acid and croton oil; 2) the rat hind-paw edema test produced by several inflammatory inductors: carrageenan, dextran, zymosan, platelet-activating factor (PAF) and arachidonic acid; 3) a subacute model based on the rat carrageenan air-pouch granuloma test. Blood leukocyte free radical production was measured by flow cytometry with 2',7'-dichlorofluorescin diacetate (DCFH-DA) in vivo, in rats with induced air-pouch granuloma, and in a model in vitro. stimulating leukocytes with hydrogen peroxide. The aqueous extract of P. sagittalis showed a marked anti-inflammatory effect in both ear edema tests, dextran and carrageenan hind-paw edemas and carrageenan air-pouch model. It also had a potent antioxidant activity in blood leukocytes, both in vivo and in vitro. Our results correlate the reduction of free radical production with the anti-inflammatory effect of this plant.
The total reactive antioxidant potential (TRAP) of 'Sangre de Drago' from Croton lechleri (Euphorbiaceae) was determined by monitoring the intensity of luminol enhanced chemiluminescence enhanced by peroxyl radicals derived from thermolysis of 2,2'-azo-bis(2-amidinopropane). The TRAP index was calculated as 935.4 +/- 141 microM, measured as equivalents of Trolox concentration. On the other hand, the additive incorporation of lower concentrations yielded an instantaneous increase in chemiluminescence, suggesting a prooxidant activity at these levels. DNA sugar damage induced by Fe(II) salts was also used to determine the capacity of the latex to suppress hydroxyl radical-mediated degradation of DNA. As in the case of luminol enhanced chemiluminescence, Sangre de Drago was highly effective in reducing oxidation of DNA at higher concentrations, but showed an increase in the production of TBARS at lower doses, as compared to the control. Finally, antioxidant activity was tested using hydroperoxide-initiated chemiluminescence in rat liver homogenates, and the latex showed an increase in light emission, suggesting the presence of prooxidant compounds.
Aqueous (AE), ethanol (EE) and dichloromethane (DE) extracts from the whole plant of Anthurium cerrocampanense Croat, endemic to Panama, were assayed for antiinflammatory activity by carrageenan-induced rat paw edema and croton oil-induced mouse ear edema tests. The extracts were administered i.p. and topically, respectively. The best antiinflammatory activity in the carrageenan-induced rat paw edema test, was shown by DE (31% inhibition), which did not show any irritant effect in the peritoneal examination 4 h after administration of the extracts. Furthermore, the highest activity in the croton oil-induced mouse ear edema test was also exhibited by DE (93% inhibition). Since DE was the most effective of the extracts in both tests, it's activity was assessed in various inflammation models in rats. At 100 mg/kg, DE markedly inhibited inflammation produced by dextran (66.6% inhibition) and decreased weakly the edema induced by zymosan A, carrageenan and C16-platelet activation factor (C16-PAF) (33.2, 31.6 and 23.8%, respectively). At 50 mg/kg, DE only significantly reduced the swelling caused by dextran (36.2%). No effect was observed at the same doses in arachidonic acid-induced edema. A clear dose-related antiinflammatory activity of DE was seen in the croton oil-induced mouse ear edema test, and ED50 calculated was found to be 25.5 microg/ear. which was much lower than ED50 obtained for indomethacin (56.1 microg/ear).
A series of dimeric procyanidins (1-9) and some related polyphenols (10-15) were chosen as model compounds in a comparative investigation for various biological activities in order to obtain structure-activity relationships. Antiviral [herpes simplex virus (HSV) and human immunodeficiency virus (HIV)], antibacterial, superoxide radical-scavenging, and complement-modulating properties were assessed. In general, more pronounced activities were seen with epicatechin-containing dimers for anti-HSV, anti-HIV, and radical-scavenging effects, while the presence of ortho-trihydroxyl groups in the B-ring was important in compounds exhibiting anti-HSV and radical-scavenging effects and complement classical pathway inhibition. Double interflavan linkages gave rise to interesting antiviral effects (HSV and HIV) and complement inhibition. The influence of the degree of polymerization or the type of interflavan linkage (4-->6 or 4-->8) differed in the different biological systems evaluated. Only minor or moderate antibacterial effects were observed for the compounds under investigation.
The aim of this study was to investigate the safety and effectiveness of orally administered SP-303 in patients with AIDS and diarrhea.
This is a multicenter, phase II, randomized, double blind, placebo-controlled study. HIV-positive subjects with a history of a CD4 count <200 or an AIDS-defining illness were admitted to an inpatient study unit and screened for diarrhea defined as at least three abnormal (i.e., soft or watery) stools and >200 g of abnormal stool weight over a 24-h period. Subjects discontinued all antidiarrheal agents >24 h before enrollment. Stool samples were studied for routine pathogens. Subjects received 500 mg p.o. of SP-303 or placebo every 6 h for 96 h (4 days). Stool frequency and weights were recorded. Subjects were monitored for symptoms and side effects and were seen 1 wk later in follow-up.
A total of 26 subjects received SP-303, and 25 received placebo. There were no significant demographic differences between treatment arms. A total of 41 subjects (80%) were receiving antiretroviral therapy and 39 subjects (77%) were receiving at least one protease inhibitor. Stool studies revealed no pathogens in 48 of 51 patients (94%). There were no serious adverse events or laboratory abnormalities. The SP-303 treatment group demonstrated a mean reduction from baseline stool weight of 451 g/24 h versus 150 g/24 h with placebo on day 4 of treatment (p = 0.14), and a mean reduction in abnormal stool frequency of three abnormal stools in 24 h versus two in 24 h in the placebo group (p = 0.30). Daily measures analysis over 4 days of treatment demonstrated that SP-303 subjects had a significant reduction in stool weight (p = 0.008) and abnormal stool frequency (p = 0.04) when compared to placebo-treated subjects.
SP-303 is safe and well tolerated. These results suggest that SP-303 may be effective in reducing stool weight and frequency in patients with AIDS and diarrhea.
A series of 19 related dihydrobenzofuran lignans and benzofurans was obtained by a biomimetic reaction sequence involving oxidative dimerization of p-coumaric, caffeic, or ferulic acid methyl esters, followed by derivatization reactions. All compounds were evaluated for potential anticancer activity in an in vitro human disease-oriented tumor cell line screening panel that consisted of 60 human tumor cell lines arranged in nine subpanels, representing diverse histologies. Leukemia and breast cancer cell lines were relatively more sensitive to these agents than were the other cell lines. Compounds 2c and 2d, but especially 2b (methyl (E)-3-¿2-(3, 4-dihydroxyphenyl)-7-hydroxy-3-methoxycarbonyl-2, 3-dihydro-1-benzofuran-5-ylprop-2-enoate), the dimerization product of caffeic acid methyl ester, containing a 3',4'-dihydroxyphenyl moiety and a hydroxyl group in position 7 of the dihydrobenzofuran ring, showed promising activity. The average GI(50) value (the molar drug concentration required for 50% growth inhibition) of 2b was 0.3 microM. Against three breast cancer cell lines, 2b had a GI(50) value of <10 nM. Methylation, reduction of the double bond of the C(3)-side chain, reduction of the methoxycarbonyl functionalities to primary alcohols, or oxidation of the dihydrobenzofuran ring to a benzofuran system resulted in a decrease or loss of cytotoxic activity. Compound 2b inhibited mitosis at micromolar concentrations in cell culture through a relatively weak interaction at the colchicine binding site of tubulin. In vitro it inhibited tubulin polymerization by 50% at a concentration of 13 +/- 1 microM. The 2R, 3R-enantiomer of 2b was twice as active as the racemic mixture, while the 2S,3S-enantiomer had minimal activity as an inhibitor of tubulin polymerization. These dihydrobenzofuran lignans (2-phenyl-dihydrobenzofuran derivatives) constitute a new group of antimitotic and potential antitumor agents that inhibit tubulin polymerization.
Activity of sangre de drago (dragon's blood) on free radicals production in rat and human leukocytes. 44th Annual Congress of the Society for Medicinal Plant Research
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Polyphenolic compounds form Croton lechleri
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Anti-inflammatory activity of Anthurium cerrocampenense Croat in rats and mice
- L Segura
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Segura L, Vila R, Gupta MP, Espósito-Avella M, Adzet T, Caaeigueral S.
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rats and mice. J Ethnopharmacol 1998; 61: 243 ± 8