Ethylenediammonium-Dicarboxylate Salts and Co-Crystallization for Biological and Pharmaceutical Applications

Several ammonium type salts and co-crystals have been used in drug formulations to increase or decrease solubility, to improve stability, toxicity and also reducing the hygroscopicity of the products. Basically, a wide range of chemically diverse acidsand bases with different pKa, solubilities , molecular weight and other properties have been used for the purpose for a very long timein both drug and food formulations. In the present study, six ethylenediamminium salts containing thiocyanate and the anion derivedfrom diprotic acids namely oxalic (I), adipic (2), fumaric(3), succinic (4), azelaic (5) and sebacic (6) respectively, have been synthesized and characterized including their molecular structures. The difference in the pKa values of the acids unable the salt formation to be generalized. The molar conductivities of the salts are between 218 and 453 ohm-1cm2mol-1 with maximum value of 453 for salt (I). All the salts showed low activity against some selected bacteria and fungi and low toxicity against vero cell. The molecular structure of the salts will be presented and the biological activity will be compared with other ammonium salts

Leishmanicidal Activity of Films Containing Paromomycin and Gentamicin Sulfate both In Vitro and In Vivo

Background: Based on the efficacy of paromomycin ointment and recent ongoing clinical trials of combination of paromomycin and gentamicin, a new physical form of films of the paromomy­cin and gentamicin was prepared and anti-Leishmania activities of the prepared films were as­sessed in vitro and in vivo.Methods: Paromomycin 15% and gentamicin 0.5% was incorporated in a film using ethyl cellu­lose and HPMC (Hydroxyl Propyl Methyl Cellulose). In order to assess the drug release and anti-Leishmania activities of the preparation, a clone L. major parasite was established using a set of modified NNN medium without overlay liquid layer. Therapeutic effects of the films were evalu­ated using Balb/c mice model. The mice were inoculated with 2×106 L. major promastigotes (MRHO/IR/75/ER) and then when the lesions developed the mice were randomly divided in 3 groups, 10 mice per group, and treated with either perpetrated films or placebo for 28 days or left untreated.Results: Growth inhibition of cloned promastigotes showed that the films have enough releasing capacity and in vivo system, the films containing paromomycin and gentamicin was able to re­duce the lesion size and induced complete cure in 80% of the mice but relapse was seen in 60% of the cured mice and overall 50% cure rate was seen during 20 weeks period of the study.Conclusion: It seems that the prepared films might be further used in human clinical trials

Let's talk about varying G

It is possible that fundamental constants may not be constant at all. There is a generally accepted view that one can only talk about variations of dimensionless quantities, such as the fine structure constant $\alpha_{\rm e}\equiv e^2/4\pi\epsilon_0\hbar c$. However, constraints on the strength of gravity tend to focus on G itself, which is problematic. We stress that G needs to be multiplied by the square of a mass, and hence, for example, one should be constraining $\alpha_{\rm g}\equiv G m_{\rm p}^2/\hbar c$, where $m_{\rm p}$ is the proton mass. Failure to focus on such dimensionless quantities makes it difficult to interpret the physical dependence of constraints on the variation of G in many published studies. A thought experiment involving talking to observers in another universe about the values of physical constants may be useful for distinguishing what is genuinely measurable from what is merely part of our particular system of units.Comment: 6 pages, Gravity Research Foundation essa

Ethyl­enediaminium hemioxalate thio­cyanate

In the title compound, C2H10N2 2+·0.5(C2O4)2−·NCS−, the ethyl­enediaminium dication adopts a (+)-synclinal conformation with an N—C—C—N torsion angle of 62.64 (15)°. The oxalate dianion lies across an inversion centre. In the crystal structure, the ions are linked through N—H⋯N, N—H⋯O and C—H⋯S hydrogen bonds, leading to the formation of a three-dimensional network

2,4-Diamino-6-methyl-1,3,5-triazin-1-ium hydrogen oxalate

The title compound, C4H8N5 +·C2HO4 −, was obtained from the reaction of oxalic acid and 2,4-diamino-6-methyl-1,3,5-triazine. The protonated triazine ring is essentially planar with a maximum deviation of 0.035 (1) Å, but the hydrogen oxalate anion is less planar, with a maximum deviation of 0.131 (1) Å for both carbonyl O atoms. In the crystal, the ions are linked by inter­molecular N—H⋯O, N—H⋯N, O—H⋯O and C—H⋯O hydrogen bonds, forming a three-dimensional network. Weak π–π [centroid–centroid distance = 3.763 Å] and C—O⋯π inter­actions [O⋯centroid = 3.5300 (16) Å, C—O⋯centroid = 132.19 (10)°] are also present

The decrease in NKG2D+ Natural Killer cells in peripheral blood of patients with metastatic colorectal cancer

Background: Natural killer (NK) cells play important roles in the immune defense against tumors such as colorectal cancer. In humans, NKG2D is an activating immune receptor constitutively expressed in most cytotoxic lymphocytes including NK and CD8+ T cells. In this study, the expression of NKG2D molecule was investigated in peripheral blood NK cells from colorectal cancer patients and compared with healthy subjects. Methods: We studied 21 non-metastatic (low-grade), 17 non-metastatic (high-grade), 16 metastatic colorectal cancer patients, and 24 healthy controls. Peripheral blood samples were obtained to isolate peripheral blood mononuclear cells (PBMCs) and the percentage of peripheral blood NKG2D+CD3-CD56+ NK cells was analyzed by flow cytometry. The expression of NKG2D at mRNA level was also measured by real-time PCR in both, patients and control subjects. Results: The results showed a significant reduction in the percentage of NKG2D+NK cells as well as NKG2D mRNA expression in peripheral blood of metastatic colon cancer patients. Conclusion: This result suggests that decreased expression of activating NKG2D receptor in metastatic colorectal cancer might compromise NK cell function and allow tumor to evade immunity (Tab. 3, Fig. 4, Ref. 33). Text in PDF www.elis.sk