Discoid Lupus Erythematosus: A Cross-Sectional Study From the Sindh Institute of Skin Diseases, Karachi, Pakistan.

Introduction Discoid lupus erythematosus (DLE) is the most common form of cutaneous lupus erythematosus. It is a chronic, scar-forming, photosensitive autoimmune dermatosis presenting with erythematous and scaly lesions. Predisposed areas include sun-exposed areas like the nose, forehead, and cheeks, as well as the upper body and extremities. The histological findings are typical, with interface dermatitis. Immunoglobulin M (IgM) and immunoglobulin G (IgG) are the most common deposits in the dermoepidermal junction of the involved skin. The most common treatments used are sunscreens, topical corticosteroids, and antimalarials. Immunosuppressive agents, thalidomide, dapsone, and retinoids can be used in refractory cases. The aim of this study was to study the clinicopathologic patterns of DLE in patients presenting to the Institute of Skin Diseases in Sindh, Karachi. Methods A total of 53 consecutive patients with DLE meeting the inclusion criteria were evaluated between February 18, 2018 to March 2, 2019 at the Institute of Skin Diseases. Patients with clinical suspicion of DLE were evaluated and studied prospectively after written informed consent was obtained. Information was then collected from their medical histories, physical examination records, and laboratory investigation reports. Results A total of 53 consecutive patients with clinical and/or histological diagnosis of DLE was included in this study, out of which 75.5% (40) were females with a male to female ratio of 1:3.1. The mean age of the patients at the time of presentation was 36.02 ± 10.04 years, ranging from 14 to 65 years. More than half of the patients (35, 66.0%) were under 40 years of age and 20.8% (11) had a positive family history of DLE. DLE was localized in 36 patients (67.9%) and exposure to the ultraviolet radiation (UVR) was found to be the most frequent induced factor in 46 patients (86.8%), followed by stress which was observed in 14 patients (26.4%). The distribution of commonly affected sites were the face (81.1%), the limbs (71.7%), and the scalp (48.4%) of the patients. Serology antinuclear antibody (ANA) was positive in 56.6% and serology anti-double-stranded deoxyribonucleic acid antibodies (anti-dsDNA) were positive in 45.3% of patients. Smoking, as an induced factor, was more commonly observed among male patients as compared to the female patients with a proportion of 53.8% vs. 2.5%, p < 0.001, while stress was more common among female patients with a proportion of 35% vs. 0%, p = 0.013, respectively. Histopathology with direct immunofluorescence was done in 33 cases which included cases with negative serology or where the diagnosis was in doubt clinically. The main histopathological features observed were periadnexal and perivascular dermal infiltrates, basal cells vacuolization, epidermal atrophy, hyperkeratosis, and follicular plugging. The commonest morphological form observed was the classic discoid plaque form. Conclusion Clinical patterns of DLE in our population comprises of female dominance. Exposure to UVR was the leading inducing factor. The face and limbs were the most commonly involved sites, and the majority of the patients had localized DLE with positive ANA in more than half of those patients. The importance of limiting ultraviolet radiation exposure and toxins (drugs and smoking) should be emphasized in our population.

2-[(2-Meth-oxy-benzyl-idene)amino]-phenol.

In the title compound, C(14)H(13)NO(2), the azomethine double bond adopts an E conformation and the benzene rings form a dihedral angle of 77.70 (7)°. In the crystal, mol-ecules are linked by O-H⋯N and C-H⋯O hydrogen bonds and arranged in a zigzag fashion, forming infinite chains parallel to the c axis, resulting in a graph-set R(2) (2)(9) motif.

{2-[(3-Bromo-benzyl-idene)amino]-5-chloro-phen-yl}(phen-yl)methanone.

In the title compound, C(20)H(13)BrClNO, the azomethine double bond [C=N = 1.246 (4) Å] adopts an E conformation. The bromo- and chlorophenyl rings are inclined to one another by 13.70 (11)°, and form dihedral angles of 76.68 (10) and 74.24 (7)°, respectively, with the phenyl ring. In the crystal, mol-ecules are linked by C-H⋯O hydrogen bonds to form double stranded chains propagating along the b-axis direction.

17-(Pyrimidin-2-yl)-8,16-dioxa-17-aza-tetra-cyclo-[7.7.1.0.0]hepta-deca-2,4,6,10,12,14-hexa-ene.

In the title compound, C(18)H(13)N(3)O(2), the benzene rings form a dihedral angle of 78.49 (9)°. The dihedral angles between the benzene rings and the pyrimidine ring are 76.53 (10) and 27.73 (11)°. The two cis-fused six-membered heterocyclic rings adopt half-chair confirmations. In the crystal, mol-ecules are linked by C-H⋯O hydrogen bonds, forming chains parallel to the b axis.

{5-Chloro-2-[(4-nitro-benzyl-idene)amino]-phen-yl}(phen-yl)methanone.

The mol-ecule of the title Schiff base compound, C(20)H(13)ClN(2)O(3), assumes an E configuration about the C=N bond. The aromatic rings of the nitro-benzene and chloro-benzene groups are twisted by 13.89 (13)° and form dihedral angles of 76.38 (13) and 84.64 (13)°, respectively, with the phenyl ring. In the crystal, mol-ecules are linked into chains parallel to the b axis by C-H⋯π inter-actions.

{5-Chloro-2-[(2-hy-droxy-benzyl-idene)amino]-phen-yl}(phen-yl)methanone.

The title Schiff base compound, C(20)H(14)ClNO(2), adopts an E configuration about the azomethine bond. The phenol and chloro-benzene rings form dihedral angles of 84.71 (9) and 80.70 (8)°, respectively, with the phenyl ring and are twisted by 15.32 (8)° with respect to one another. The mol-ecular conformation is stabilized by an intra-molecular O-H⋯N hydrogen bond, which forms an S(6) ring motif. In the crystal, mol-ecules are linked by C-H⋯O hydrogen bonds, forming columns parallel to the a axis.

Understanding the magnitude of still birth in Mymensingh Medical College Hospital.

To understand the incidence and causes of still-births occurred in Mymensingh Medical College Hospital, we conducted a retrospective record review study in Department of Gynaecology of the hospital. The study population were the cases of still births occurred the months of January and December 2007. We administered a structured questionnaire to all the Medical Officers working in the department. They were requested to provide information on the still-births they noticed during the study period. They review their personal log books and hospital records to complete the questionnaire. We also reviewed the hospital records to obtain the service statistics. In total 11,146 patients were admitted to seek obstetric care during the study period and of them 7,069(63%) sought delivery care. During this period there were 735(10%) still births. The incidences of still births were more during December and January. The pre-existing maternal diseases that were frequently associated with still births were Antepartum Haemorrhage (APH) 38% and hypertension (27%). The frequently reported direct causes of the still births were obstructed labour (42%), misuse of oxytocin (28%) and foetal distress (20%). In many cases the loss is completely unexpected. Hospital based surveillance and issuing of still-birth certificates may increase the awareness of the problem among the obstetricians and in the community.

Lipoxygenase inhibitory tetraketones: potential Remedial source for inflammation and asthma / Las tetracetonas inhibidoras de la lipoxigenasa: fuente potencial Remedial para la inflamación y el asma

OBJETIVE: A series of tetraketones has been synthesized by way of a one pot synthesis and screened for inhibitory activity against the enzyme lipoxygenase. METHOD: An efficient and high yielding one pot synthesis to tetraketones [2-22] has been developed by way of tetraethyl ammonium bromide (Et4N+Br-) mediated condensation of cyclohexane-1, 3-dione [1] with a variety of aldehydes. Lipoxygenase enzyme solution was prepared so that enzyme concentration in reaction mixture was adjusted to give rates of 0.05 absorbance/minute. The test compounds were prepared in methanol of concentrations 50, 25, 12.5, 6.25 and 3.125 µM. The reaction mixture contained 160 µL (100 mM) sodium phosphate buffer (pH 8.0), 10µL of test-compound solution and 20µL of lipoxygenase solution. The contents were mixed and incubated for 10 minutes at 25ºC. The reaction was then initiated by the addition of 10µL substrate solution (linoleic acid, 0.5 mM, 0.12% w/v tween 20 in the ratio of 1:2), with the formation of (9Z,11E)-(13S)-13-hydroperoxyoctadeca-9,11-dienoate, the change of absorbance at 234 nm was followed for 6 minutes. The concentrations of the test compounds that inhibited the lipoxygenase activity by 50% (IC50) were determined by monitoring the effect of increasing concentrations of these compounds in the assays on the degree of inhibition. The IC50 values were calculated by means of the EZ-Fit Enzyme-Kinetics Program (Perrella Scientific Inc., Amherst, USA). RESULT: The tetraketones [2-22] were synthesized in high yields (91-98%) using mild reaction conditions. Most of these compounds showed significant inhibitory activity against the enzyme lipoxygenase. It was found that the presence of substituents which increase delocalization of electrons enhances the inhibitory activity. CONCLUSION: It is concluded that the study is likely to lead to the discovery of therapeutically efficient agents against important disorders such as inflammation and asthma.

OBJETIVO: Una serie de tetracetonas han sido sintetizadas mediante síntesis de varios pasos en un solo reactor (one-pot), y examinadas en relación con su actividad inhibitoria frente a la enzima lipoxigenasa. MÉTODO: Una síntesis one-pot de un rendimiento alto y eficiente para la obtención de tetracetonas (2-22) ha sido desarrollada mediante bromuro amónico tetraetílico (Et4N+Br-) - de ciclohexano-1,3-diona, con una variedad de aldehídos. La solución de enzima lipoxigenasa fue preparada de modo que la concentración de la enzima en las mezcla de la reacción fue ajustada para que diera tasas de 0.05 absorbancia/minuto. Los compuestos de la prueba fueron preparados en metanol de concentraciones (50, 25, 12.5, 6.25 y 3.125 µM). La mezcla de reacción contenía 160 µL (100 mM) de un tampón (buffer) de fosfato de sodio (pH 8.0), 10µL de solución de compuesto de prueba, y 20µL de solución de lipoxigenasa. Los contenidos fueron mezclados e incubados por 10 minutos a 25ºC. La reacción fue iniciada entonces por la adición de 10µL de solución substrato (ácido linoleico, 0.5 mM, 0.12% p/v tween 20 en proporción de 1:2), con la formación de (9Z, 11E)-(13S)-13-hidroperoxioctadeca-9,11-dienoato, el cambio de absorbancia a 234 nm fue seguido por 6 minutos. Las concentraciones de los compuestos de prueba que inhibían la actividad de la lipoxigenasa en un 50% (IC50) fueron determinadas monitoreando el efecto del aumento de las concentraciones de estos compuestos en los ensayos sobre el grado de inhibición. Los valores IC50 fueron calculados mediante el Programa Cinética de la Enzima EZ-Fit (Perrella Scientific Inc., Amherst, USA). RESULTADOS: Las tetracetonas (2-22) se sintetizaron con elevados rendimientos (91-98%) usando condiciones de reacción leve. La mayoría de estos compuestos mostraron una actividad inhibitoria significativa frente a la enzima lipoxigenasa. Se halló que la presencia de sustituyentes que aumentan la deslocalización de los electrones contribuye a mejorar la actividad inhibitoria. CONCLUSIÓN: Se concluye que es probable que el estudio conduzca al descubrimiento de agentes terapéuticamente eficientes frente a trastornos importantes tales como la inflamación y el asma.

Lipoxygenase inhibitory tetraketones: potential remedial source for inflammation and asthma.

OBJECTIVE: A series of tetraketones has been synthesized by way of a one pot synthesis and screened for inhibitory activity against the enzyme lipoxygenase. METHOD: An efficient and high yielding one pot synthesis to tetraketones [2-22] has been developed by way of tetraethyl ammonium bromide (Et4N+Br-) mediated condensation of cyclohexane-1, 3-dione [1] with a variety of aldehydes. Lipoxygenase enzyme solution was prepared so that enzyme concentration in reaction mixture was adjusted to give rates of 0.05 absorbance/minute. The test compounds were prepared in methanol of concentrations 50, 25, 12.5, 6.25 and 3.125 microM. The reaction mixture contained 160 microL (100 mM) sodium phosphate buffer (pH 8.0), 10 microL of test-compound solution and 20 microL of lipoxygenase solution. The contents were mixed and incubated for 10 minutes at 25 degrees C. The reaction was then initiated by the addition of 10 microL substrate solution (linoleic acid, 0.5 mM, 0.12% w/v tween 20 in the ratio of 1:2), with the formation of (9Z, 11E)-(13S)-13-hydroperoxyoctadeca-9,11-dienoate, the change of absorbance at 234 nm was followed for 6 minutes. The concentrations of the test compounds that inhibited the lipoxygenase activity by 50% (IC50) were determined by monitoring the effect of increasing concentrations of these compounds in the assays on the degree of inhibition. The IC50 values were calculated by means of the EZ-Fit Enzyme-Kinetics Program (Perrella Scientific Inc., Amherst, U.S.A.). RESULT: The tetraketones [2-22] were synthesized in high yields (91-98%) using mild reaction conditions. Most of these compounds showed significant inhibitory activity against the enzyme lipoxygenase. It was found that the presence of substituents which increase delocalization of electrons enhances the inhibitory activity. CONCLUSION: It is concluded that the study is likely to lead to the discovery of therapeutically efficient agents against important disorders such as inflammation and asthma.

Natamycin treatment of experimental Candida albicans induced keratomycosis in rabbits

Objective: The efficacy of topical natamycin 5% was studied using a reproducible model of keratomycosisproduced by Candida albicans in the rabbits. Method: Candida albicans was isolated from infected human eye and 4 x 105 cells of the Candida albicans was injected into the corneal stroma of the eyes of 15 rabbits. All eyes developed a corneal ulcer without pretreatment with immunosuppressive agents. Forty-eight hours after inoculation, the animals were divided into two groups: test group I, 10 eyes receiving natamycin drops in a 5% suspension; control group II, five eyes receiving 0.9% normal saline solution. The rabbits¡¯ corneas were removed for Candida albicans recovery and placed in 1 ml of sterile 0.9% normal saline solution, minced within two hours with scalpel and thoroughly homogenized with a piston and mortar. Serial dilutions of this corneal solution from 10-1 ¨C 10-4 were made in 0.9% sterile saline solution and 100 ¦Ìlaliquots were plated onto tryptic soy agar. All cultures of cornea from the treated eyes were negative after seven days of inoculation while five cultures were still positive in the control eyes at the end of the experiment. Result: It was found that 5% natamycin was effective in treating experimental Candida albicans induced keratomycosis in rabbits. Conclusion: It is concluded that natamycin has a significant effect (p < 0.01) against Candida albicansin treating experimental keratomycosis.

Objetivo: La eficacia de la natamicina tópica al 5% fue estudiada usando un modelo reproducible de queratomicosis producida por Candida albicans en conejos. Método: Candida albicans fue aislada de una infección ocular humana y 4 x 105 células de Candida albicans fueron inyectadas en el estroma córneo de los ojos de 15 conejos. Todos los ojos desarrollaron una úlcera córnea sin pre-tratamiento con agentes inmunosupresores. Cuarenta y ocho horas después de la inoculación, los animales fueron divididos en dos grupos: un grupo experimental I, en el que diez (10) ojos recibieron gotas de natamicina en suspensión al 5%; y un grupo control II, en el que cinco(5) ojos recibieron solución salina normal al 0.9%. Las córneas de los conejos fueron extraídas para recuperar Candida albicans y colocadas en 1 ml de solución salina normal estéril, para ser luego desmenuzadas a las dos horas con un escalpelo, y homogeneizadas completamente con un mortero. Sehicieron diluciones seriadas de esta solución córnea de 10-10 -10-4 en solución salina al 0.9% y 100 mlde alícuotas fueron colocadas en placas con agar de soya tríptico. Todos los cultivos de corneas de los ojos tratados, resultaron negativos luego de siete días de inoculación, mientras que 5 cultivos eran todavía positivos al final del experimento en los ojos del control.Resultado: Se halló que la natamicina al 5% era efectiva en el tratamiento de la queratomicosis inducida experimentalmente mediante Candida albicans en conejos. Conclusión: Se concluyó que la natamicina surte efecto (p < 0.01) sobre Candida albicans en eltratamiento experimental de la queratomicosis.

Natamycin treatment of experimental Candida albicans induced keratomycosis in rabbits.

OBJECTIVE: The efficacy of topical natamycin 5% was studied using a reproducible model of keratomycosis produced by Candida albicans in the rabbits. METHOD: Candida albicans was isolated from infected human eye and 4 x 10(5) cells of the Candida albicans was injected into the corneal stroma of the eyes of 15 rabbits. All eyes developed a corneal ulcer without pretreatment with immunosuppressive agents. Forty-eight hours after inoculation, the animals were divided into two groups: test group I, 10 eyes receiving notamycin drops in a 5% suspension; control group II, five eyes receiving 0.9% normal saline solution. The rabbits' corneas were removed for Candida albicans recovery and placed in 1 ml of sterile 0.9% normal saline solution, minced within two hours with scalpel and thoroughly homogenized with a piston and mortar Serial dilutions of this corneal solution from 10(-1) - 10(-4) were made in 0.9% sterile saline solution and 100 microl aliquots were plated onto tryptic soy agar. All cultures of cornea from the treated eyes were negative after seven days of inoculation while five cultures were still positive in the control eyes at the end of the experiment. RESULT: It was found that 5% natamycin was effective in treating experimental Candida albicans induced keratomycosis in rabbits. CONCLUSION: It is concluded that natamycin has a significant effect (p < 0.01) against Candida albicans in treating experimental keratomycosis.

Triterpenes from Mimusops elengi.

Pentacyclic triterpenes (1) and (2) have been isolated from Mimusops elengi and assigned structures 3beta,6beta,19alpha,23-tetrahydroxy-urs-12-ene and 1beta-hydroxy-3beta-hexanoyllup-20 (29)-ene-23, 28-dioic acid, respectively, on the basis of spectroscopic studies including 2D-NMR. The compound 1 showed moderate inhibiting activity against beta-glucuronidase enzyme

A new withanolide glycoside from physalis peruviana

A new withanolide glycoside, 17beta-hydroxy-14, 20-epoxy-1-oxo-[22R]-3beta-[O-beta-D-glucopyranosyl]-witha-5, 24-dienolide (1), has been isolated from the whole plant of Physalis peruviana. Its identity was determined using a combination of spectroscopic data including 2D NMR techniques and chemical transformations.