Kalanchoe laciniata and Bryophyllum pinnatum: an updated review about ethnopharmacology, phytochemistry, pharmacology and toxicology

Abstract The species Kalanchoe laciniata (L.) DC. and Bryophyllum pinnatum (Lam) Pers. are native from Brazil and Madagascar, respectively. Both belonging to the Crassulaceae family and being widely used by population as a natural anti-inflammatory agent. These species have similar leaf morphology and for this reason, they are known by the same popular name as " saião " or " coirama ". Several studies have been published involving different parts and preparations of these species. Therefore, this review aims to provide an update overview about the traditional uses, chemical constitution, pharmacology and toxicology of K. laciniata and B. pinnatum species. An extensive literature review was conducted in different scientific databases. Various chemical constituents have been identified in extracts from different parts of K. laciniata and B. pinnatum , being flavonoids the major compounds. They have been traditionally used to treat inflammation, microbial infection, pain, respiratory diseases, gastritis, ulcers, diabetes and cancer tumors. Non-clinical in vitro assays evaluated mainly the antimicrobial and antioxidant activities, while in vivo assays evaluated the leishmanicide, anti-inflammatory and immunomodulatory activities. Regarding toxicity, few studies have been conducted for the two species. The information reported in this work might contribute to the recognition of the importance of K. laciniata and B. pinnatum species, as well as to direct further studies. (AU)

Mecanismos de ação relacionados à atividade antiúlcera de Kalanchoe pinnata (Lam.) Pers. (Crassulaceae) / Mechanisms of action underlying antiulcer activity of Kalanchoe pinnata (Lam.) Pers. (Crassulaceae).

Kalanchoe pinnata (Lam.) Pers. (Crassulaceae) é uma espécie muito empregada na medicina tradicional no Brasil e em outras partes do mundo, especialmente Índia, países da África e China. É indicada popularmente para diversos fins incluindo o tratamento de úlceras gástricas. A análise fitoquímica revelou a presença de vários constituintes, em especial os flavonoides. O tratamento de úlcera gástrica convencional apresenta diversos efeitos colaterais e, na maioria das vezes, não evita a recidiva da lesão. Dessa maneira, é interessante encontrar uma terapêutica mais segura e efetiva. Com o objetivo de avaliar a segurança, foi realizado ensaio de citotoxicidade do extrato bruto, in vitro, com valor de IC50 igual a 0,926 mg/mL, sendo possível predizer um valor de LD50 (1341,46 mg/kg). Já em relação ao ensaio de citotoxicidade, in vitro, da fração acetato de etila não foi encontrado um valor de IC50. Resultados de fototoxicidade, in vitro, mostraram que o extrato bruto e fração acetato de etila de K. pinnata não possuem potencial fototóxico. A contagem microbiana na droga vegetal para bactérias aeróbias/mesófilas foi de 6,9 x 104 UFC/g e a contagem de bolores e leveduras foi de 2,4 x 103 UFC/g, ambos valores dentro do limite estabelecido pela OMS. Análise de endotoxinas também foi realizada para o extrato bruto (<4,0.105 UE/kg) e fração acetato de etila (<2,7.105 EU/kg) de K. pinnata. Referente à fitoquímica, diversos flavonoides foram identificados no extrato bruto e fração acetato de etila de K. pinnata. Paralelamente ao estudo fitoquímico foi verificado que a atividade gastroprotetora do extrato bruto envolve a ação das prostaglandinas e grupamentos sulfidrila. Já o mecanismo de gastroproteção da fração acetato de etila é dependente de prostaglandinas e óxido nítrico. A atividade cicatrizante do extrato bruto de K. pinnata também foi avaliada. De acordo com os resultados macroscópicos, as doses de 200mg/kg e 400 mg/kg reduziram a área de lesão, com uma taxa de 33% e 39%, respectivamente, após 7 dias de tratamento (p<0,05). Análise histológica dos grupos tratados com o extrato bruto (200 e 400 mg/kg) indicou melhor recuperação da lesão, verificada pela regeneração da mucosa gástrica e pelo restabelecimento da arquitetura glandular. As enzimas antioxidantes (catalase, superóxido dismutase e glutationa peroxidase) e a expressão de VEGF foram avaliadas no mecanismo de cicatrização de úlceras gástricas. Os resultados mostraram que a atividade antiulcerogênica foi mediada pela ação antioxidante da enzima SOD. Não foi evidenciado in vivo o aumento da expressão de VEGF e nem o sequestro do radical peroxil nos animais tratados com o extrato bruto. Os resultados dos ensaios in vitro (ORAC) mostraram uma maior capacidade de sequestro de radicais peroxil da fração acetato de etila (1192,35 ± 112,61 µmol equivalente de Trolox/g de amostra seca) quando comparado com o extrato bruto (431,32 ± 7,17 µmol equivalente de Trolox/g de amostra seca). A atividade anti Helicobacter pylori também foi avaliada, no entanto, o extrato bruto não apresentou atividade anti H.pylori. Ademais, o extrato bruto demonstrou um potencial anti-inflamatório, pois foi observada uma redução nos níveis de TNF-α e L-selectina, após o tratamento em neutrófilos estimulados com LPS. Analisando os resultados sugere-se que K. pinnata possui um potencial terapêutico no combate de úlceras gástricas e possivelmente, anti-inflamatório, sendo que os flavonoides podem estar relacionados com o efeito biológico observado.

Kalanchoe pinnata (Lam.) Pers. (Crassulaceae) is a commonly used species in traditional medicine in Brazil and in other parts of the world, especially India, Africa and China, for the treatment of various diseases, including gastric ulcers. Phytochemical analysis revealed the presence of several constituents in this plant, especially flavonoids. The available pharmaceutical products to treat peptic ulcer have several side effects and, in most cases, do not prevent recurrence of the gastric lesions. Therefore, it is important to find a safer and more effective therapy. In order to evaluate safety, the in vitro cytotoxicity assay of crude extract from K. pinnata was performed. The IC50 value was 0,926 mg/mL corresponding to LD50 value (1341, 46 mg/kg). It was not determined IC50 value in vitro cytotoxicity assay for ethyl acetate fraction from K. pinnata. Neither the crude extract nor ethyl acetate fraction from K. pinnata showed phototoxicity. Microbial counting was performed on the K. pinnata-based drug in order to investigate microbiological contamination. The microbial count for aerobic / mesophilic bacteria was 6.9 x 104 CFU/g, and yeast count was 2.4 x 103 CFU/g, both values in agreement with the limits established by WHO. Endotoxin analysis was also performed for the crude extract (<4,0.105 UE/kg) and for ethyl acetate fraction (<2,7.105 UE/kg) from K. pinnata. In the phytochemical analysis several flavonoids were identified in the crude extract and ethyl acetate fraction of K. pinnata. In parallel to the phytochemical study, it was verified that the gastroprotective activity of the crude extract of K. pinnata involved prostaglandins and sulfhydril compounds. On the other hand, the mechanism of gastroprotection of the ethyl acetate fraction of K. pinnata is dependent on prostaglandins and nitric oxide. The healing activity of the crude extract of K. pinnata was also evaluated. According to the macroscopic results the dose of 200 mg/kg and 400mg/kg reduced the injury area, with a rate of 33% and 39%, respectively, after 7 days of treatment (p <0.05). Histological analysis showed regeneration of the gastric mucosa and re-establishment of the glandular architecture in groups treated with the crude extract (200 and 400 mg/kg). Antioxidant enzymes (catalase, superoxide dismutase and glutathione peroxidase) and VEGF expression were evaluated in the mechanism of gastric ulcer healing. The results showed that the antiulcerogenic activity was mediated by SOD. It was not demonstrated an increase in VEGF expression and nor in the in vivo sequestration of the peroxyl radical in the animals treated with crude extract. The results of in vitro assay (ORAC) showed a greater sequestering of peroxyl radical to the ethyl acetate fraction (1192,35 ± 112,61 µmol equivalent of Trolox/g of ethyl acetate fraction) when compared to the crude extract (431,32 ± 7,17 µmol equivalent of Trolox/g of crude extract) of K. pinnata. The anti Helicobacter pylori activity was also evaluated; however, the crude extract did not show anti H. pylori activity. However, the crude extract of K. pinnata demonstrated an anti-inflammatory potential, because TNF-α and L-selectin levels were reduced after treatment in LPS-stimulated neutrophils. The analysis of the results suggests that K. pinnata has a therapeutic potential against gastric ulcers and possible anti-inflammatory properties, and the flavonoids may be linked to the biological effect.

Flavonoid Compounds from the Leaves of Kalanchoe prolifera and Their Cytotoxic Activity against P-388 Murine Leukimia Cells

Seven flavonoid compounds, kaempferol (1), quercetin (2), quercetin-3-O-β-D-glucopyranoside (3), kaempferol-3-O-β-D-glucopyranoside (4), kaempferol-3-O-α-L-rhamnoside (5), quercetin-3-O-sophoroside (6) and quercetin-3-O-rutinoside (7), were isolated from the methanolic extract of leaves of Kalanchoe prolifera. Compounds 1-7 were isolated for first time from this plant. These compounds were evaluated their cytotoxic activity against P-388 murine leukimia cells in vitro. Among those compounds kaempferol (1) and quercetin (2) showed strongest cytotoxic activity with IC₅₀ values of 4.45 ± 0.05 and 6.28 ± 0.02 µg/mL, respectively.

Research progress of alternative production approaches of salidroside / 中国中药杂志

Salidroside, one of the active components of Rhodiola plants, is a phenolic glycoside with significant biological activities. The investigation and development of alternative production approaches of salidroside is of high academic and application values due to the limited resource of Rhodiola plants, and from which the low yield of salidroside. This review summarized the research progress and perspective of the alternative production approaches of salidroside including both chemosynthetic and biosynthetic methods and pathways.

[New species of Lebanon and redescription endemic species]

In this note, the authors give a brief description of 12 wild plants not observed previously in Lebanon [of which a tree] or species considered extinct in this country since more than 50 years. They add new details to the description of 2 endemic plants of Lebanon Senecio mouterdei, abundant in Wadi-Johannam and Orobanche astragali parasite living in altitude

Plantas empleadas en odontalgias I / Plants used for toothache

En la consulta estomatológica, las odontalgias son padecimientos frecuentes, los cuales por su magnitud disminuyen la capacidad y rendimiento del individuo. Para tratar dichas alteraciones se emplean fármacos de diversa naturaleza, aunque desde tiempos remotos diversas plantas también han sido empleadas. Nuestra flora medicinal es una de las más diversas del mundo y por supuesto incluye algunas utilizadas con la misma finalidad. En este estudio, se presentan 51 especies que corresponden a 29 familias botánicas reportadas como utilizadas en odontalgias en diferentes países, principalmente en México y que son usadas por la medicina tradicional. Dichas plantas elaboran, entre otros, metabolitos secundarios con posible actividad biológica: aceites esenciales, alcaloides, cardenólidos, ciclitoles, glucósidos-iridoides, heterósidos cianogenéticos, mucílagos, resinas, saponinas, sesquiterpenos, taninos y triterpenos. Las partes de los vegetales empleadas son muy variadas e incluyen en algunos casos a la planta entera fresca. Las formas de uso más frecuentemente reportadas fueron las infusiones y los cocimientos. La vía de administración es local, tópica o por medio de enjuagues, o bien ingiriendo la infusión o el cocimiento, aunque algunas plantas se aplican en forma de cataplasma.

Odontalgia is a very common disorder, frequently observed in patients visiting the dentist office. Due to its severity, odontalgia may significantly reduce the performance capability of the subject. At present, many drugs from different origins are being used for the odontalgia treatment. However, from ancient times, several plants have also been used. As our medicinal flora has one of the greatest diversity in the world, it certainly includes some plants that can be employed for such purpose. This study includes 51 species, belonging to 20 botanical families, which have been reported as useful for odontalgia treatment by traditional medicine in several countries, mainly in Mexico. Such plants produce several secondary metabolites with probable biologic activity, among them: essential oils, alkaloids, cardenolides, ciclitols, glycoside-iridoids, heterosides, cyanogenics, mucilages, resins, saponines, sesquiterpenes tannins and triterpenes. The parts of the plant that might be used for the odontalgia control are diverse; sometimes even the whole fresh plant can be used. The most frequently reported methods of preparation are infusion and concoction. The administration is mainly local (topic) or as mouthwash, or by drinking the infusion or decoction. Some of the plants can be prepared and applied as poultice.

Pharmacokinetics of hylotelephin in Beagle dogs / 药学学报

<p><b>AIM</b>To investigate the pharmacokinetics of hylotelephin in Beagle dogs and obtain the main pharmacokinetic parameters.</p><p><b>METHODS</b>An HPLC method with UV detection was developed to study the pharmacokinetics of hylotelephin in dogs by joining an internal standard (anthracene). Benzoyl chloride was used to the pre-column derivatization of hylotelephin and methanol-water (64:36) was used as the mobile phase. According to the 3P97 pharmacokinetic program, the main parameters were calculated.</p><p><b>RESULTS</b>The hylotelephin pharmacokinetics conforms to a two-compartment open model after a single iv dose of hylotelephin 10.6 or 21.3 mg x kg(-1) in Beagle dogs. The parameters of two groups were as follows: T(1/2) alpha were 2.3 and 2.1 min, T(1/2) beta were 1.9 and 2.0 h, K12 were 0. 12 and 0.11 min, K21 were 0.17 and 0.21 min, K10 were 0.011 and 0.0094 min, Vc were 0.54 and 0.54 L x kg(-1), AUC were 1.8 and 4.1 g x min x L(-1), CL were 0.0048 and 0.0056 L x kg(-1) x min(-1), MRT were 2.10 and 2.4 h, respectively.</p><p><b>CONCLUSION</b>The pharmacokinetics of hylotelephin after iv administration showed a rapid distribution and elimination process in Beagle dogs and was of first order kinetics.</p>

Morfoanatomia de folhas de bálsamo: Sedum dendroideum Moc. et Sessé ex DC, Crassulaceae / Leaf morpho-anatomy of Sedum dendroideum Moc. et Sessé ex DC, Crassulaceae

Sedum dendroideum Moc. et Sessé ex DC, Crassulaceae é uma espécie suculenta, conhecida popularmente como bálsamo. Na medicina tradicional, suas folhas são empregadas para tratar inflamações de pele, contusões e problemas gástricos, em razão das ações emoliente e cicatrizante. Com o objetivo de fornecer subsídios morfológicos e taxonômicos, realizou-se estudo morfoanatômico das folhes. Observou-se que as folhas são simples, sésseis e alternas e apresentam formato oboval, levemente assimétrico, com ápice obtuso, base decurrente e margem lisa. A epiderme é uniestratificada e possui células com paredes anticlinais delgadas e onduladas. Os estômatos são anisocíticos, estando presentes em ambas as faces. Mesofilo homogêneo e numerosos idioblastos com conteúdo fenólico foram evidenciados.