The extraordinary transformation of traditional Chinese medicine: processing with liquid excipients.

Context: The Chinese medicinal materials originate from animals, plants, or minerals must undergo appropriate treatment before use as decoction pieces. Processing of Chinese medicines with liquid excipients is a pharmaceutical technique that transforms medicinal raw materials into decoction pieces which are significantly different from the original form. During processing, significant changes occur in chemical constituents, which inevitably affects clinical efficacy. At present, the liquid materials in processing mainly involve wine, vinegar, honey, saline water, ginger juice, herbal juice, etc.Objective: This review introduces the typical methods of liquid excipients processing, summarizes the influence on chemical composition, pharmacological efficacy, and expounds the ways and mechanisms of liquid excipients to change the properties of drugs, enhance the efficacy, eliminate or reduce toxicity and adverse reaction.Methods: English and Chinese literature from 1986 to 2020 was collected from databases including Web of Science, PubMed, Elsevier, Chinese Pharmacopoeia 2015, and CNKI (Chinese). Liquid excipients, processing, pharmacological effects, synergism, chemical constitution, traditional Chinese medicine (TCM) were used as the key words.Results: Liquid excipients play a key role in the application of TCM. Processing with proper liquid excipients can change the content of toxic or active components by physical or chemical transformation, decrease or increase drug dissolution, alter drug pharmacokinetics, or exert their own pharmacological effects. Thus, processing with liquid excipients is essential to ensure the safety and efficacy of TCM in clinic.Conclusion: This article could be helpful for researchers who are interested in traditional Chinese herbs processed with liquid excipients.

An easy access to topical gels of an anti-cancer prodrug (5-fluorouracil acetic acid) for self-drug-delivery applications.

An easy access to topical gels (both hydro- and organogels) derived from an anti-cancer prodrug namely 5-fluorouracil acetic acid (5-FuA) achieved by exploiting a simple salt formation strategy is reported for the first time. Nearly 85% of the salts synthesized were gelators. Single crystal structures of some of the gelator salts revealed an intriguing hydrogen bonding network including double stranded 1D chains stabilized through uracil-uracil complementary interactions and the crystal structures of the gelator salts corroborated well with the hypothesis based on which the gelators were designed. Studies indicated that both the hydrogel and the methyl salicylate gel of the gelator salt FuA-15 were suitable for self-drug-delivery application.

Synthesis and insecticidal activity of acridone derivatives to Aedes aegypti and Culex quinquefasciatus larvae and non-target aquatic species.

A serious Mosquito borne yellow fever is one of the grave diseases which affect the major population. Since there is no specific treatment for yellow fever, there is a necessity to develop an effective agent. The series of acridinone analogues 3 to 5 were synthesized with help of non-conventional microwave heating and confirmed by respective spectral characterization. 5c and 3b showed highest activity to kill 90% of larvae against A. aegypti and C. quinquefasciatus, respectively. Also the active products were treated to check the mortality of non-target aquatic species. Through the reports of the larvicidal bioassay, compounds 3b against C. quinquefasciatus whereas 5c against A. aegypti were found to be more active. By keeping this as a platform, further extension of the work can be done to find out a valuable drug for controlling disease vectors.

Efeito da suplementação de cobre e selênio na dieta de novilhos Brangus sobre o desempenho e fermentação ruminal / The effects of copper and selenium supplementation in the diet of Brangus steers on performance and rumen fermentation

Vinte e oito bovinos Brangus foram usados para determinar o efeito da suplementação de cobre e selênio no desempenho e na fermentação ruminal. Os animais foram divididos em: 1) C(Controle) - sem a suplementação de cobre e selênio; 2) Se - 2mg Se/kg de matéria seca na forma de selenito de sódio; 3) Cu - 40mg Cu/kg de matéria seca na forma de sulfato de cobre; 4) Se/Cu - 2mg Se/kg de matéria seca na forma de selenito de sódio e 40mg Cu/kg de matéria seca na forma de sulfato de cobre. As pesagens dos animais foram feitas em intervalos de 28 dias, após jejum completo de 18 horas. Foram colhidas amostras de líquido ruminal para análises de ácidos graxos voláteis e pH. O ganho de peso diário aumentou com a suplementação de Se (P<0,05). A ingestão de matéria seca não foi alterada pelos tratamentos (P>0,05). Os animais submetidos à suplementação com Cu apresentaram menor pH ruminal quando comparado com a suplementação Se/Cu (P<0,05). Os animais suplementados com Se/Cu apresentaram maior proporção de ácido acético quando comparado com o controle (P<0,05). Para o ácido propiônico e butírico, não houve diferenças significativas (P>0,05) entre os tratamentos. Apesar do pouco efeito na fermentação ruminal, as suplementações de selênio, cobre e selênio/cobre proporcionaram uma melhor eficiência alimentar.

Twenty-eight Brangus cattle were used to determine the effect of copper and selenium supplementation on performance and rumen fermentation. The animals were divided in: 1) (Control) - without supplementation of copper and selenium; 2) Se - 2mg Se/kg of dry matter as sodium selenite; 3) Cu - 40mg Cu/kg of dry matter as copper sulphate; 4) Se/Cu - 2mg Se/kg of dry matter as sodium selenite and 40mg Cu/kg of dry matter as copper sulphate. Animal weighing was performed in 28 day intervals, after 18 hours of fasting. Samples of rumen liquid were collected for analysis of volatile fatty acid and pH. The daily weight gain increased with selenium supplementation (P<0.05). The dry matter intake was not altered by treatments (P>0.05). The animals that received copper supplementation had lower pH rumen compared with selenium/copper supplementation (P<0.05). The animals supplemented with selenium/copper had a high proportion of acetic acid when compared to control (P<0.05). For propionic and butyric acid, there was no difference (P>0.05) among treatments. Despite the little effect on rumen fermentation, the supplementations of selenium, copper and selenium/copper provided better feed efficiency.

Relative effectiveness of pretreatments on performance of Rhizomucor miehei lipase in nonpolar reaction media.

Enzymes can be used in nonpolar reaction media to modify water-insoluble substrates. A variety of pretreatments, applied to the enzyme prior to introduction to the nonpolar media, can improve enzyme activity. However, the various pretreatments have not been studied using directly comparable conditions, nor have they been applied simultaneously to test for interactive effects. This work evaluates pretreatment of lipase with various classes of additives. The pretreated lipase is used to catalyze esterification between citronellol and acetic acid in a medium of n-hexane. The effectiveness of a particular pretreatment is presented in terms of relative performance (RP), which is equal to the number of times faster the pretreated lipase catalyzes the reaction relative to untreated lipase. The individual and interactive effects of the pretreatment factors were studied and compared. Buffer salts had a much stronger performance-enhancing effect than nonbuffer salts; pretreatment with 90% (w/w) sodium phosphate yielded lipase with an RP of approx 64. A strong interaction was found between the treatments with sodium phosphate and pH adjustment. These treatments may mitigate the inhibitory effect of acetic acid. Activating effects of phase interfaces and active-site protectants are shown to be complementary to other treatments, demonstrating that they likely act by distinct mechanisms.